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Cedrón, Juan Carlos. "Capsaicin." Revista de Química, 2013. http://repositorio.pucp.edu.pe/index/handle/123456789/99655.
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Pica, nos hace ponernos rojos, pero también alivia el dolor. La capsaicina es el componente principal del ají, ingrediente de tantas comidas en nuestro país.It is spicy, it makes us blush, but it also relieves pain. Capsaicin is the main component of chili pepper, an ingredient in so many dishes in our country.
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Hughes, G. A. "Novel, potent antagonists of capsaicin." Thesis, University College London (University of London), 2005. http://discovery.ucl.ac.uk/1445556/.
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The aim of this project was to explore and refine the conformational rationale for the activity of capsazepine (CPZ) as a blocker of the ion channel TRPV1 (transient receptor potential vanilloid type 1), by the synthesis and biological evaluation of further conformational constrained capsaicin analogues. The resolution of the stereoisomers of Af-(4-chlorophenethylthiocarbamoyl)-6,7-dihydroxy-1-methyl-1,2,3,4-tetrahydroisoquino-line 29, Af-(4-chlorophenethylthio-carbamoyl)-6,7-dihydroxy-3-methyl-1,2,3,4-tetra-hydroisoquinoline 30 and N-(4-chlorophenethylthiocarbamoyl)-6,7-dihydroxy-1,3-dimethyl-1,2,3,4-tetrahydroiso-quinoline 31 by stereoselective synthetic methodology is described, and some of the more unusual and interesting mechanisms are discussed. The novel asyrnmetric chemistry described includes the separation of the enantiomers of 2-(3,4-dimethoxyphenyl)-l-methylethylamine 38 by crystallisation with the enantiomers of mandelic acid, the use of sodium triacetoxyborohydride in the stereoselective reduction of 6,7-dimethoxy-l,3-dimethyl-3,4-dihydroiso-quinoline 171, to give the cw-diastereomers of 6,7-dimethoxy-1,3-dimethyl-1,2,3,4-tetrahydroisoquinoline 44, and the novel stereoselective route to the trans-diastereomers of 6,7-dimethoxy-l,3-dimethyl-l,2,3,4-tetrahydroisoquinoline 44 from the enantiomers of 2-(3,4-dimethoxyphenyl)-l-methylethylamine 38 by the Michael addition of A-benzyl-2-(3,4-dimethoxyphenyl)-l-methylethylamine 155 to ethynyl-4-tolylsulfone 150, followed by TFA-mediated cyclisation, single electron reductive desulfonylation and palladium-catalysed hydrogenolysis. The results of investigations into the conformational behaviour of the resolved stereoisomers of 29, 30 and 31 by techniques of NMR spectroscopy and molecular modelling, the evaluation of their biological activity at the rat and human orthologues of the ion channel TRPV1, and the attempted correlation of the two sets of data, with respect to the published conformational rationale for the activity of CPZ, are also described.
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Ziglio, Analine Crespo. "Uso da capsaicina como preservante de madeiras ao ataque de fungo apodrecedor." Universidade de São Paulo, 2010. http://www.teses.usp.br/teses/disponiveis/88/88131/tde-16082010-143912/.
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Nesse estudo, utilizamos a oleoresina de capsaicina, extraído da pimenta Malagueta (Capsicum frutensens) e da pimenta Dedo-de-moça (Capsicum baccatum), para a preservação de amostras de madeira contra o ataque do fungo Paecilomyces variotti. Os preservantes naturais foram aplicados em corpos de prova de madeiras do gênero Pinus sp. e Hymenae sp. (Jatobá) com as dimensões 5,0 x 3,0 x 1,0 (cm). A seguir, esses corpos de prova foram expostos ao fungo para o acompanhamento do seu desenvolvimento. As análises mostraram que o preservante natural retardou o crescimento do fungo, sendo a oleoresina de capsaicina extraído da pimenta Malagueta a mais eficiente se comparada à oleoresina extraída da pimenta Dedo-de-moça e ao óleo de linhaça. A partir da medida de ângulo de contato observou-se que o preservante de oleoresina da pimenta Malagueta proporcionava uma maior molhabilidade para as duas espécies de madeiras. A técnica de FTIR-ATR indicou que os preservantes não modificaram a estrutura das madeiras e a análise de raios X revelou que o desenvolvimento do fungo provocou uma perda de estabilidade e periodicidade nas estruturas das madeiras. Através do teste de proporção utilizado para a análise do desenvolvimento do fungo, comprovou-se estatisticamente que o seu crescimento foi menor para as amostras com os preservantes das pimentas. Pelo MEV foi possível visualizar as estrutura de hifas do fungo sobre a madeira. E a perda de massa para ambas as espécies de madeiras foram menores quando foram utilizados os preservantes, sendo o Pinus a espécie que sofreu maior degradação.In this study, were used the oleoresin capsaicin, extracted from Capsicum frutensens and Capsicum baccatum, for the preservation of wood samples against the attack of the Paecilomyces variotti fungus. The natural preservatives were applied to Pinus sp. and Hymenaea sp. (Jatobá) specimens with the dimensions 5.0 x 3.0 x 1.0 (cm). Subsequently, these specimens were exposed to fungus and their development was monitored. . Analyses showed that the natural preservative slowed the growth of the fungus. Action of the oleoresin capsaicin extracted from Chilli pepper is the most efficient when compared to pepper oleoresin extracted from Capsicum frutensens and Capsicum baccatum and also with the linseed oil. The contact angle measured showed that the preservative of Oleoresin Chilli Pepper offered a higher wettability for both wood species. FTIR-ATR technique indicated that the preservatives did not change wood structure and X-ray analysis revealed that the development of the fungus caused a loss of stability and periodicity in the wood structures. At proportion test to analyze the development of the fungus, it was shown statistically that their growth was lower for the samples with preservatives peppers. It was possible to visualize the hyphae structure by scanning electronic microscopy technique. Mass loss of both wood specie was lower when preservative was used, and Pine species was more degraded.
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Tablas, Mariana Baptista. "Efeitos da capsaicina na etapa de promoção/progressão da carcinogênese química de colón em ratos." Botucatu, 2018. http://hdl.handle.net/11449/180429.
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Orientador: Luís Fernando BarbisanResumo: A capsaicina (8-metil-N-vanilil-trans-6-nonamida) é uma substância alcaloide de natureza lipofílica, responsável pela pungência de pimentas e pimentões. Apresenta propriedades anti-inflamatória, antimicrobiana e antioxidante bem descritas na literatura científica. Assim, este projeto teve como objetivo investigar se a capsaicina apresenta efeito quimioprotetor quando administrada na etapa de promoção/progressão da carcinogênese de cólon induzida pela 1,2-dimetilhidrazina (DMH). Ratos Wistar machos foram alocados em seis grupos experimentais com 10 a 15 animais cada. Os animais dos grupos 1-3 receberam quatro injeções subcutâneas (s.c) do carcinógeno DMH (40mg/kg, duas doses/semana) e os animais do grupo 4-6 receberam quatro injeções s.c de solução de EDTA .Os grupos 2 e 4 receberam por gavagem 5mg/kg p.c e os grupos 3 e 5 receberam 50mg/kg p.c de capsaicina diluída em óleo de milho até o final da 24ª semana do experimento. Após a eutanásia dos animais, os cólons distal, medial e proximal foram corados com azul de metileno a 2% para detecção de focos de criptas aberrantes (FCA). Após a análise de FCAs, os cólons foram processados para análise histológica e classificação de tumores. As amostras congeladas foram utilizadas para análise de expressão de gênica pela técnica Taqman® Low Density Array (TLDA). Os níveis séricos de ALT (p=0,346) e creatinina (p=0,854) foram semelhantes entre os grupos, mostrando que as doses de capsaicina utilizadas não apresentaram ação citotóxica par... (Resumo completo, clicar acesso eletrônico abaixo)
Abstract: Capsaicin (8-Methyl-N-vanillyl-(trans)-6-nonenamide) is a lipophilic alkaloid, responsible for the pungency in pepper. Its antiinflamatory, antimicrobial and antioxidant properties are well described in the scientific literature. Thus, the objective of this study was to investigate whether capsaicin exerts a chemoprotective effect when administered during 1,2-dimethylhydrazine (DMH)-induced colon carcinogenesis promotion/progression in rates. Male Wistar rats were allocated into six groups of 10-15 animals each. Groups 1-3 received 4 subcutaneous injections of DMH (40 mg/kg bw, 2 doses/week), while groups 4-6 received EDTA solution (DMH vehicle, 2 doses/week), followed by intragastric 5mg/kg bw capsaicin diluted in corn oil (G2, G4) or 50mg/kg bw (G3, G5) for 24 weeks (3 doses/week). After sacrifice, blood samples were drawn by heart puncture for the assessment of serum alanine aminotransferase (ALT) and creatinine levels, and the colon was removed. A segment of distal colon and colon tumor samples were frozen in liquid nitrogen at -80ºC. Distal, medial and proximal colon samples were stained with 2% methylene blue for the detection of aberrant crypt foci (ACF).After ACF analysis, colon tumors were processed for histological analysis and tumor classification. The frozen samples were used for the analysis of gene expression by Taqman® Low Density Array (TLDA). Serum ALT (p=0.346) and creatinine (p=0.854) levels were similar among groups, indicating that the capsaicin doses use... (Complete abstract click electronic access below)
Doutor
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Ziglio, Analine Crespo. "Oleoresina de capsaicina como preservante natural de madeira de Pinus sp. contra a ação de fungos de podridão branca e de podridão mole." Universidade de São Paulo, 2015. http://www.teses.usp.br/teses/disponiveis/18/18158/tde-27082015-101533/.
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Neste trabalho, avaliou-se a eficácia do uso da oleoresina de capsaicina, extraído das pimentas Malagueta, Red Savina e Bhut Jolokia, no tratamento da superfície de madeiras do gênero Pinus sp. com teores de umidade de equilíbrio de 12% e 0%. Os corpos de prova foram submetidos ao ataque de fungos Paecilomyces variotti e Pycnoporus sanguineus. Foi utilizado um preservante sintético conhecido comercialmente como stain para se comparar com a eficiência de preservantes naturais à base de oleoresina de capsaicina. A partir de medidas de ângulo de contato das superfícies das madeiras tratadas com o óleo de capsaicina, observou-se que a pimenta Bhut Jolokia e o preservante stain proporcionavam menor molhabilidade para a espécie de madeira estudada em ambos teores de umidade. O tratamento preservante fez com que a energia de superfície diminuísse se comparada aos valores de amostras de madeiras sem o tratamento preservante devido às contribuições polares e dispersivas. A análise estatística dos resultados, pelo método de Tukey, mostrou que não existe um grupo de resultados estatisticamente equivalente aos obtidos com a amostra testemunha (sem tratamento). As amostras de Pinus sp. a um teor de umidade 0% mostrou-se mais protegida superficialmente quando modificada com a oleoresina extraída da pimenta Bhut Jolokia e o mesmo efeito foi observado estatisticamente para o preservante stain. A técnica de Langmuir foi utilizada para melhor compreender as interações capsaicina/ergosterol, capsaicina/DPPG (dipalmitoil fosfatidil glicerol) e capsaicina/DPPG/ergosterol. A isotermas de pressão de superfície vs área por molécula se mostraram mais expandidas quando a subfase continha oleoresina de capsacina e quando comparada com as de lipídio puro (DPPG), indicando assim, a inserção da capsaicina na monocamada. Em linhas gerais, oleoresina de capsaicina extraída da pimenta Bhut Jolokia mostrou-se mais eficiente em todos os aspectos se comparada com as pimentas Red Savina e Malagueta, marcando, assim, uma potencialidade para uso como preservante natural de madeiras.The present study evaluated the effectiveness of capsaicin oleoresin extracted from Malagueta, Red Savina and Bhut Jolokia peppers in the surface treatment of Pinus sp. with moisture contents of 12% and 0%. The samples were submitted to the attack of Paecilomyces variotti and Pycnoporus sanguineus fungus. A synthetic wood preservative, that is commercially known as stain, was used to compare the effectiveness of natural preservatives based on capsaicin oleoresin. From contact angle measurements for wood surfaces treated with capsaicin oleoresin, it was obtained that Bhut Jolokia pepper and stain preservatives have provided worse wettability for wood samples at both moisture contents. The preservative treatment caused a decrease in the surface energy when compared to the samples without preservative treatment due to polar and dispersive contributions. Statistical analysis for the results by using the Tukey method showed that there is not a group of results that are statistically equivalent to those obtained for the control samples (without treatment). Pinus sp. samples at a moisture content of 0% showed to be more surface protected after being modified with the oleoresin extracted from Bhut Jolokia; the same effect was observed statistically for stain. The Langmuir technique was used to better understand interactions among capsaicin/ergosterol, capsaicin/DPPG (dipalmitoyl phosphatidyl glycerol) and capsaicin/DPPG/ergosterol. Surface pressure vs. area per molecule isotherms appeared to be even more extended when the subphase contained capsaicin oleoresin instead of pure lipid (DPPG), thus indicating the inclusion of capsaicin into the monolayer. In general, the capsaicin oleoresin extracted from Bhut Jolokia proved to be more efficient in all the aspects of characterization when compared to Red Savina and Malagueta highlighting its potential for use as a natural wood preservative.
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Bhatta, Puspanjali. "Protective effect of capsaicin against cisplatin ototoxicity." OpenSIUC, 2014. https://opensiuc.lib.siu.edu/theses/1579.
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Cisplatin is a widely used chemotherapeutic drug for the treatment of solid tumors. However, the drug accumulates in the cochlea, and damages inner ear structures, resulting in bilateral andpermanent hearing loss. Previous data from our laboratory indicate that activation of the transient receptor potential vanilloid 1 (TRPV1) receptor (by capsaicin) increases the NOX3 isoform of NADPH oxidase, leading to the generation of reactive oxygen species (ROS) in the cochlea, transient cochlear inflammation and transient hearing loss. We also demonstrated that the transient inflammation was produced by ROS-mediated activation of signal transducer and activator of transcription 1 (STAT1). Surprisingly, over time, this response desensitizes and capsaicin was subsequently able to protect against cisplatin ototoxicity. The goal of this study was to determine the mechanism of otoprotection against cisplatin ototoxicity following the administration of capsaicin. For this study we utilize both an immortalized organ of Corti outer hair cells and rat cochlea. Capsaicin (2.5 µM) increased both Ser727 p-STAT1 and Tyr705 p-STAT3 implicating its role in inflammation. Expression of cannabinoid receptors were observed in UB/OC-1 cells as well as rat outer hair cells (OHCs). However, inhibition of CB2 receptors (by AM630) reduced capsaicin-mediated Tyr705 p-STAT3, but had little effect on Ser727 STAT1. Capsaicin protected UB/OC-1 cells against cisplatin-induced apoptosis. This protection was reversed by CB2 antagonist but potentiated by TRPV1 inhibition. Significant cell death was observed following treatment of UB/OC-1 cells with AM630 alone, underscoring the importance of CB2 receptors in survival of these cells. CB2 agonist, JWH, significantly increased the protective signal, STAT3. Furthermore, capsaicin-mediated protection was reversed by the inhibition of STAT3, implicating STAT3 in otoprotection. In animal studies, oral administration of capsaicin (0.5% solution) induced transient inflammation but led to a long term recovery. Animals pre-treated with oral capsaicin were protected against cisplatin-induced hearing loss as compared to vehicle-treated animals, suggesting protection against hearing loss. Capsaicin increased the expression of both CB1 and CB2 receptors in the organ of Corti, which might confer the long term protective actions of this agent against hearing loss. In rats pretreated with AM630, the protective action of capsaicin was abolished. We conclude that otoprotection mediated by capsaicin is produced by activation of CB receptors in the cochlea which are coupled to both STAT1 and STAT3 activation. However, our data support the conclusion that activation of STAT3 confers the otoprotective action of capsaicin. In contrast, activation of STAT1 by capsaicin could contribute to the transient inflammatory response previously observed in vivo. The net protective action of capsaicin could result from an increase in the STAT3/STAT1 ratio of cells in the cochlea, which antagonizes the ability of cisplatin lower this ratio and promote cell death.
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Saffran, Alexander. "Activation of TRPV1 by Capsaicin Regulates ENaC." VCU Scholars Compass, 2018. https://scholarscompass.vcu.edu/etd/5544.
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ENaC is a constitutively open heterotrimeric channel which regulates Na+ transport in tight epithelia of the kidney, lungs, colon and anterior tongue containing fungiform taste buds. The amiloride-sensitive ENaC is comprised of aβg subunits. Humans express an additional subunit, the d subunit. Therefore, humans contain both aβg-ENaC and dβg-ENaC functional channels. Relative to aβg-ENaC, the dβg-ENaC is 10-fold less sensitive to amiloride. In the mammalian anterior tongue, ENaC is expressed in fungiform salt sensing taste receptor cells and is the Na+-specific salt taste receptor. In mammals, salt elicits an inverted U shaped behavioral response. Lower concentrations of salt are appetitive while high salt concentrations are aversive. The appetitive salt concentrations are sensed via ENaC. Thus, modulating ENaC activity in fungiform taste receptor cells will, in turn, regulate salt intake. The aim of this project is to investigate the effect of a common food ingredient, capsaicin, on ENaC expression and function in two cell lines, HEK293 cells and cultured adult human fungiform taste bud cells (HBO cells). Capsaicin, a TRPV1 agonist was chosen because in previous studies, it modulated chorda tympani taste nerve responses to NaCl in a dose-dependent manner. Most importantly, capsaicin and other agonists of TRPV1 were effective in modulating human salt taste perception. It is likely that the effect of capsaicin is due to its interactions with TRPV1, because TRPV1 and ENaC subunits are co-expressed in cortical collecting duct cells (CCD) and in a subset of human taste bud cells. In support of this hypothesis, TRPV1 has been shown to regulate ENaC expression and function in CCD cells of rats and mice. Using immunohistochemical techniques, our results demonstrate that TRPV1 is co-localized with the d-ENaC subunit in HBO cells. Additionally, the results in HEK-293 cells suggest that the activation of TRPV1 via capsaicin has a modulatory effect on d-ENaC mRNA and protein expression as well ENaC channel function measured as Na+ flux.
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Liapi, Anastasia. "Cloning of the vanilloid-like receptor VR-L and investigation of its interaction with members of the transient receptor potential family of receptors." Thesis, University College London (University of London), 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.270624.
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Tavares, Mauricio Temotheo. "Candidatos a novos agentes antineoplásicos: síntese e avaliação da atividade antitumoral de análogos sulfonatos e sulfonamídicos da capsaicina." Universidade de São Paulo, 2014. http://www.teses.usp.br/teses/disponiveis/9/9138/tde-29102014-153643/.
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O câncer é o segundo grupo de doenças que mais mata em todo o mundo, atrás apenas das doenças cardiovasculares. No Brasil, esse panorama é preocupante devido ao período de acentuada tendência de envelhecimento, fase etária de maior incidência do câncer. Neste contexto, a atual terapia antineoplásica continua apresentando diversos vieses quanto à toxicidade e seletividade. Muitos dos fármacos empregados na clínica médica são de origem natural, ou tiveram em suas etapas iniciais de desenvolvimento, correlação com produtos naturais, enaltecendo a importância de fontes naturais no desenvolvimento de novos compostos bioativos. A capsaicina, substância responsável pela pungência apresentada pelos frutos de pimenteiras do gênero Capsicum, tem se mostrado um importante agente natural com atividade citotóxica à diversas linhagens neoplásicas, porém, sua ação pungente e baixa estabilidade físico-química, limitam seu emprego terapêutico. Com isso, a capsaicina apresenta grande potencial em servir como arcabouço para o planejamento de novas entidades químicas bioativas, análogas à mesma, para emprego no tratamento do câncer. Este trabalho propôs-se a planejar e sintetizar análogos sulfonamídicos e sulfonatos da capsaicina, promovendo variações moleculares no núcleo estrutural capsaicinóide. Após síntese em única etapa, os análogos foram obtidos e caracterizados por faixa de fusão, RMN 1H/13C e análise elementar. Posteriormente os compostos foram submetidos a ensaio de citotoxicidade nas linhagens tumorais: MDA-MB-231 e MCF-7 (de câncer de mama), B16-F10 (melanoma murino) e sobre linhagens sadias de fibroblasto (3T3), pelo método de avaliação da viabilidade celular por biorredução do sal de tetrazólio, o MTT. Quatro compostos apresentaram atividade biológica interessante, em concentrações micromolares (µM) iferiores à atividade apresentada pela capsaicina, destacando-se os compostos RPF-101 e RPF-151, os mais ativos e que tiveram seus mecanismos de indução de morte investigados. Estudos teóricos subsequentes realizados com os análogos de maior atividade (RPF-101 e RPF-151), revelaram que as modificações moleculares promovidas nas estruturas dos mesmos conferiram maior caráter hidrofílico e maior momento de dipolo, o que pode estar relacionado com o incremento na atividade biológica de ambos. A avaliação dos compostos ativos frente às propriedades constantes na Regra dos Cinco de Lipinski (RO5) revelou que estes respeitam todos os parâmetros da regra, enaltecendo assim o caráter druglikeness dos mesmos, em serem ativos via administração oral, visto que o RPF151 não apresentou ação pungente in vivo. A obtenção dos compostos RPF-101 e RPF-151 indicam o sucesso alcançado com a otimização estrutural promovida no arcabouço capsaicinóide, e enaltece o potencial destes análogos em inspirar o planejamento de novas estruturas, ainda mais otimizadas, que possuam maior potência e menor toxicidade associada.Cancer is the second most lethal group of diseases all over the world, just behind cardiovascular diseases. This scenery is worrying in Brazil due the pronounced aging trend observed, that presents the higher incidence of cancer. In this context, the current anticancer therapy still have several biases regarding toxicity and selectivity. Many current medicines correlate to natural products, even in its early stages of development, which highlight the importance of natural sources in the design of new bioactive compounds. Capsaicin is the substance responsible for the pungency of Capsicum genus\' chili peppers. Capsaicin has been shown as an important natural agent because of its cytotoxic activity against several tumor cell lines. However, the pungency and poor stability presented by capsaicin restricts its therapeutic employments. Thus, the capsaicinoid scaffold has a great potential to inspire the design of new bioactive analog entities to be employed in anticancer therapy. This project aimed at designing and synthesizing sulfonamide and sulfonate analogues of capsaicin, performing molecular changes on capsaicinoid core. After a single step synthesis, the analogues were purified and characterized by melting point, 1H/13C NMR and elementary analysis. Subsequently, cytotoxicity assays were performed by MTT method on tumor cell lines MDA-MB-231 and MCF-7 (breast cancer), B16-F10 (murine melanoma) and on healthy fibroblast (3T3). Four compounds showed interesting biological activity at micromolar concentrations (µM) and their IC50 were lower than that presented by capsaicin. The most active compounds, RPF-101 and RPF-151, had their death induction mechanisms investigated. In silico subsequent studies with the most active compounds (RPF-101 and RPF-151) showed that molecular changes promoted on each one increased their hydrophilicity and raised their dipole moment, which may be related to the improvement on biological activity of both. The evaluation of active compounds for Lipinski´s Rule of Five (RO5) properties revealed that they respect all properties presenting its druglikeness for oral administration since RPF151 did not presented in vivo pungency. The RPF-101 and RPF-151 indicate the success obtained by the structural optimization promoted on capsaicinoid scaffold and emphasizes the potential of these analogues to inspire the designing of new future optimized structures, with greater potency and less associated toxicity.
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NASCIMENTO, Patrícia Lins Azevedo do. "Atividade antioxidante e antimicrobiana da pimenta malagueta (Capsicum frutescens)." Universidade Federal Rural de Pernambuco, 2013. http://www.tede2.ufrpe.br:8080/tede2/handle/tede2/4651.
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Pimenta malagueta (Capsicum frutescens) as it is known in Brazil, is one of the pepper species most used in cooking and in Brazilian folk medicine. Antioxidant and antimicrobial activities, total phenolic compounds and capsaicin, dihydrocapsaicin and crisoeriol content were analyzed. The content of capsaicin, dihydrocapsaicin and crisoeriol found was 9.2, 4.0 and 2.1 mg/g extract, respectively. The minimal inhibitory concentration was determined against six bacteria strains and Candida albicans but for all of them were necessary concentrations higher than 1000 μg/ml. The total phenolic content was 9.1 mg GAE/g extract. The ethanolic extract of C. frutescens had an effective DPPH and ABTS + scavenging (CE50 of 302.3 and 82.6 g/ml respectively) and percentage of antioxidant activity by β-carotene/linoleic acid assay that ranged from 15 to 47%. The main groups of compounds extracted from plants with biological properties are essential oils, alkaloids, glycosides, phenolic compounds, terpenoids and flavonoids. Our results suggest that C. frutescens contains a potential antimicrobial and antioxidant that can be associated with its phenolic, capsaicinoids and flavonoid contents.
Pimenta malagueta (Capsicum frutescens), como é conhecida no Brasil, é uma das espécies de pimenta mais usadas na culinária e na medicina popular brasileira. Foram analisadas as atividades antioxidante e antimicrobiana, o teor de fenólicos totais, capsaicina, dihidrocapsaicina e crisoeriol. O teor de capsaicina, dihidrocapsaicina e crisoeriol encontrado foi de 9,2, 4,0 e 2,1 mg/g de extrato respectivamente. A concentração inibidora mínima foi determinada frente seis linhagens de bactérias e da levedura Candida albicans, mas para todos os micro-organismos testados foram necessárias concentrações superiores a 1000 μg/mL. O teor de fenólicos totais foi de 9,1 mg equivalentes de ácido gálico/g de extrato. O extrato etanólico de C. frutescens apresentou atividade eficiente frente aos radicais DPPH e ABTS + (CE50 de 302,3 e 82,6 μg/mL, respectivamente) e porcentagem de atividade antioxidante pelo ensaio β-caroteno/ácido linoleico que variou de 15 a 47%. Os principais grupos de compostos extraídos de plantas com propriedades biológicas são os óleos essenciais, alcaloides, glicosídeos, compostos fenólicos, terpenoides e flavonoides. Os nossos resultados sugerem que C. frutescens contém um potencial antimicrobiano e antioxidante que pode estar associado com o seu teor de fenólicos, capsaicinoides e flavonoides.
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Fong, Genevieve May. "Mechanisms of neuroprotection by capsaicin, a red pepper extract." Thesis, The University of Sydney, 2017. http://hdl.handle.net/2123/18042.
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Background: Capsaicin is a natural compound isolated from red peppers that is currently used in the management of pain due to its ability to desensitise TRPV1 channels to further noxious stimuli following high or repeated doses (De Silva et al. 2011; Derry et al. 2013; Sharma et al. 2013). Recent studies have shown that capsaicin can also upregulate expression of the neuroprotective protein neuroglobin (Ngb), activate cell survival signalling pathways and diminish oxidative stress and inflammation (Kim et al. 2003; Dairam et al. 2008; Guo et al. 2008; Luqman et al. 2011; Lee et al. 2012). Therefore, it was hypothesised that capsaicin pre-treatment could protect neurons in a model of Parkinson’s Disease (PD). Aim: To test whether capsaicin prevents neuronal loss and restores motor function in a 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP) model of PD. Methods: Male C57BL/6J mice were pre-treated with vehicle or capsaicin (1 mg/kg) prior to saline or MPTP (25 mg/kg/day) treatment over two consecutive days. Gait was assessed on a subset of mice six days after the onset of treatment. Serum and various organs were harvested for biochemical and histological analyses that assessed dopaminergic neuron (DN) counts, apoptosis and necrosis (using caspase-3/7 and LDH assays, respectively), alterations in kinase signalling (PI3K/Akt, ERK, mTOR and p38 MAPK), markers of inflammation (IL-1β, IL-6, TNF-α, IFN-γ and MCP-1), antioxidant activity (SOD, GPx and CAT) and oxidative damage (3-nitrotyrosine (3-NT)). The ability for capsaicin to cross the blood-brain barrier (BBB) and accumulate within the brain was also assessed by matrix assisted laser desorption/ionisation imaging mass spectrometry (MALDI-IMS). Results: The major daughter fragment (m/z 137.03 a.m.u.) of capsaicin appeared abundantly in capsaicin-treated brains and predominantly accumulated in the cerebral cortex. Mice exposed to MPTP experienced a 25% loss in DN viability with a concomitant increase in xi | P a g e caspase-3/7 activity. MPTP treatment also induced phosphorylation of Akt, ERK and p38 while mTOR remained unchanged. MPTP treatment increased SOD and decreased CAT activity and elevated 3-NT expression in the substantia nigra (SN). Cerebral levels of the pro-inflammatory markers TNF-α, IFN-γ, IL-1β and MCP-1 and expression of leukocytes markers, CD45 and Iba-1, were also elevated in MPTP-treated mice. In contrast, capsaicin pre-treatment elevated Akt and ERK phosphorylation and reduced p38 activation. Capsaicin pre-treatment also reversed the MPTP-induced increase in SOD and decrease in CAT activity and concomitantly reduced 3-NT expression. Furthermore, capsaicin pre-treatment reversed the MPTP-induced increase in pro-inflammatory cytokine expression, however no obvious improvement in neuronal viability was observed. Conclusions: Capsaicin was able to cross the BBB and accumulate within the brain. Although capsaicin pre-treatment did not improve neuronal viability in this MPTP model of PD, it did reverse the MPTP-induced increase in pro-inflammatory cytokine expression and decrease in antioxidant activity. Capsaicin-mediated protection may involve both TRPV1-dependent and -independent mechanisms and activation of various kinase signalling pathways, such as PI3K/Akt and p38 MAPK. Further studies are required to elucidate the precise mechanism of capsaicin-mediated protection but should also consider the possibility that capsaicin may generate toxic metabolites under oxidative stress.
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Marchie, Alfonse. "Sex differences in the perception of capsaicin-induced pain." Thesis, McGill University, 2003. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=79045.
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Previous research has demonstrated that although women may find post-operative pain more intense than men, males are more disturbed than females by low levels of pain that last over time. In these studies, females had a tendency to rate the intensity of pain higher than males, but males had stronger affective responses following the surgical placement of intra-oral implants. However, these findings have not been investigated in an experimental setting. This experiment examined the pain responses of 20 healthy subjects (10 males, 10 females), who were subjected to capsaicin-induced pain on the face and ankle (on separate sessions). During the experiment, all subjects rated their pain intensity, unpleasantness, and anxiety on visual analog scales (VAS). In addition, throughout the experiment, heart rate was monitored every five minutes and mood was assessed once before and after the experiment. Finally, subjects also completed the McGill Pain Questionnaires (MPQ) once at the end of every session. Results revealed that although there were generally no statistically significant sex differences in the pain ratings during the experiment, there was a sex * time interaction with males displaying increasing anxiety scores over time with the capsaicin patch on the face while the anxiety scores of females decreased over time with the capsaicin patch on the face (F = 1.64, P = 0.02). Also, there was a tendency for the relative unpleasantness (unpleasantness/intensity ratio) to be greater for males than females over time on the face (F = 3.43, P = 0.08). Males and females did not differ in both the mean number of words chosen and the pain rating index of the MPQ for all categories. In addition, there were no sex differences for heart rate and mood for both the ankle and face regions throughout the experiment. Taken together, these results replicate previous findings that men may find low levels of pain more disturbing than women.
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Lambert, Joseph Walter. "Molecular Study of Capsaicin in Aqueous and Hydrophobic Environments." Thesis, Virginia Tech, 2006. http://hdl.handle.net/10919/33495.
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Anyone who has eaten spicy foods has experienced the adverse effects of capsaicin, the pungent chemical found in hot chili that causes a burning sensation. The specific action of capsaicin occurs by the activation of receptors in sensory neurons. This thesis investigates the interaction of capsaicin with model cell membranes representing the structure of neurons. In particular, we are interested in the changes induced by capsaicin to the structure and dynamics of membranes. Molecular dynamics simulations are used to study the molecular interactions. The first part of this study evaluates different molecular representations for capsaicin in an 1-octanol/water system. This inhomogeneous system is commonly used to determine the partition of compounds between hydrophilic and hydrophobic environments, as that found in biological membranes. The results of these simulations validate the OPLS united-atom force field as a reasonable molecular representation of capsaicin, as it describes the behavior of capsaicin both quantitatively and qualitatively in 1-octanol/water mixtures. In the second part, simulations are performed for capsaicin and model cell membranes consisting of dipalmitoylphosphatidylcholine and dipalmitoylphosphatidylethanolamine, two of the most commonly found lipids. Simulations investigated capsaicin in the aqueous and lipid phases. The results provide insight into the changes to the bilayers caused by capsaicin. Bilayers containing dipalmitoylphosphatidylethanolamine showed lower permeabilities to capsaicin than those composed of pure dipalmitoylphosphatidylcholine. Temperature is found to be an important factor in the permeability of capsaicin in the bilayer. Capsaicin in the bilayer concentrated in a region beneath the lipid/water interface, in which favorable hydrophilic and lipophilic interactions occur. The structure of the bilayer is not significantly changed at the concentrations of capsaicin considered. One important result from the simulations indicates that the interfacial density decreases with increasing capsaicin concentration in the bilayer, supporting the experimental observations of increased permeability in bilayers exposed to capsaicin.Master of Science
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Kim, Kyung-Mi. "Increase in swimming endurance capacity of mice by capsaicin." Kyoto University, 1998. http://hdl.handle.net/2433/182408.
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Kyoto University (京都大学)0048
新制・課程博士
博士(農学)
甲第7502号
農博第1014号
新制||農||768(附属図書館)
学位論文||H10||N3195(農学部図書室)
UT51-98-U169
京都大学大学院農学研究科食品工学専攻
(主査)教授 伏木 亨, 教授 松野 隆一, 教授 大東 肇
学位規則第4条第1項該当
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Sadofsky, Laura Rachel. "Molecular pharmacology of the capsaicin receptor (TRPV1) in the airways." Thesis, University of Hull, 2005. http://hydra.hull.ac.uk/resources/hull:8630.
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The capsaicin receptor (vanilloid receptor I, transient receptor potential vanilloid 1 or TRPV I) is a member of the transient receptor potential (TRP) family of proteins. This cation channel is sensitive to a range of inflammatory mediators such as some lipoxygenase products, as well as the tussive agents capsaicin, resiniferatoxin and protons. It has been proposed that TRPV I is a cough receptor and may be important in airways inflammation. Rat TRPVI (rTRPVI) and human TRPVI (hTRPVl) permanently expressing cell lines were generated and successfully characterised by agonist triggered changes in intracellular calcium levels. Thapsigargin and/or removal of extracellular calcium revealed that, both rTRPVI and hTRPVI are not only expressed on the cell surface but on thapsigargin sensitive and insensitive intracellular stores respectively. Citric acid, an agent routinely used in the clinic for inhalation cough challenges, was investigated for its ability to activate TRPVl permanently expressed in a cell line. rTRPV I was activated by citric acid in a concentration and pH dependent manner. Citric acid activation of TRPVI was inhibited by iodoresiniferatoxin but not capsazepine. Mutation of the TRPVI putative proton binding site (E648 to A648) abolished citric acid activation of the channel without reducing the capsaicin evoked response. Thus, citric acid activates rTRPV I by a proton dependent mechanism. The role of N-linked glycosylation and sialylation on rTRPVI and hTRPVI was investigated. Treatment of rTRPVl with neuraminidase or tunicamycin dramatically reduced the channels' maximal responses to capsaicin. In addition mutation of the rTRPVI N-linked glycosylation site (N604 to Q604) or expression ofrTRPVI in the glycosylation mutant cell line, Lec2, also resulted in a striking reduction in the receptors' maximal calcium response to capsaicin. Flow cytometry data indicated that these differences in TRPVI function were unlikely to be linked to differences in receptor cell surface expression. Human TRPV I also displayed significant reductions in responsiveness to capsaicin following either neuraminidase or tunicamycin treatment. Thus, receptor sialylation regulates TRPVI activation by capsaicin. Finally, TRPVI expression on human primary bronchial fibroblasts (HPBF) was investigated. Negligible endogenous TRPVI expression was detected in HPBF. Interestingly, the inflammatory mediators tumour necrosis factor (TNF-a), lipopolysaccharide (LPS) and interleukin Ia (IL-Ia) all induced TRPVI expression in HPBF, as assessed by RT-PCR, flow cytometry and calcium signalling. TRPVI functional expression was observed as early as 6 hrs (for TNF-a) post challenge and remained elevated upto the final time point tested (96 hrs for IL-Ia). Thus, TRPVI may play an important role in the inflammatory process. In conclusion, TRPV I may play an important role in conditions where cough and inflammation have been implicated.
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Paule, Cleoper. "Molecular bases underlying the sensitivity of the capsaicin receptor TRPV1." Thesis, Imperial College London, 2010. http://hdl.handle.net/10044/1/6144.
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Individual human beings report highly variable pain experiences following exposure to the same noxious stimulus, including noxious heat. A series of missense single nucleotide polymorphisms (SNPs) have been found in the human noxious heat transducer, transient receptor potential vanilloid type 1 ion channel (hTRPV1), which responds to, exogenous, and endogenous, vanilloids, protons, and depolarisation. The aim of this project was to examine the effect of SNPs on the sensitivity of hTRPV1 to certain activators. The three most frequently occurring SNPs (I315M, T469I, V585I) were used to generate 4 haplotypes: hTRPV1112 (V585I); hTRPV1121 (T469I); hTRPV1211 (I315M); and hTRPV1222 (I315M, T469I, V585I). The responses of these haplotypes to these activators were compared to the responses of the “wild type” hTRPV1 (hTRPV1111, I315, T469, V585) using whole-cell patch-clamp recordings from HEK293 cells which transiently-expressed the relevant ion channels. Site-directed mutagenesis was used to confirm the role of the SNPs in altering the sensitivity of hTRPV1 to the activators applied. In addition, in control experiments, several important collateral issues were investigated, namely: (a) the effect of the solvent, dimethyl sulphoxide (DMSO), on untransfected, and transfected, cells, respectively; and (b) the extent to which acid-sensing ion channels, constitutively-expressed by HEK293 cells, compromised the assessment of the proton-evoked responses of hTRPV1. The techniques employed included: the co-transfection of the cells with vector carrying the coding region of the green fluorescent protein (GFP) gene; the reverse transcriptase polymerase chain reaction; immunocytochemistry; the cobalt uptake assay; and whole-cell patch-clamp recordings. The pharmacological and biophysical properties of the DMSO-evoked, and capsaicin-evoked, responses were similar. Furthermore, DMSO desensitised TRPV1. Acid-sensing ion channels were sensitive to the diuretic, amiloride (30μM). However, amiloride increased hTRPV1-mediated responses evoked by noxious heat but not capsaicin. hTRPV1222 showed a higher sensitivity than hTRPV1111 to capsaicin, and heat. Thus, when capsaicin was applied, the EC50 of hTRPV1111 and hTRPV1222 was 817 nM and 89 nM, respectively. The activation thresholds when heat was applied to hTRPV1111 and hTRPV1222 were 44.5±0.31 oC, and 42.3±045 oC, respectively). However, hTRPV1111 was more sensitive to depolarisation than hTRPV1222, with the V1/2 at 37oC for hTRPV1111 and hTRPV1222 being 42.3 mV and 83.3 mV, respectively. Furthermore, no differences were found between the proton-and anandamide- sensitivity of hTRPV1111 and hTRPV1222. The sensitivities of hTRPV1121 to heat and depolarization were similar to those of hTRPV1222, but different from those of hTRPV1111. Furthermore, the sensitivity of hTRPV1112 and hTRPV1211 were similar to that of hTRPV1111, but different from that of hTRPV1222 and hTRPV1121. Charge-neutralising and conserving mutations at position 469 produced clones with similar sensitivities to hTRPV1121 and hTRPV1111, respectively. The studies undertaken established, first, that DMSO is able to activate TRPV1. Second, the non-synonymous SNP at position 469 in hTRPV1 alters the sensitivity of the ion channel to vanilloids, heat, and depolarisation. These findings suggest that missense SNPs in hTRPV1 may contribute to the development of different pain experience in humans in response to the same noxious stimulus. Accordingly, regard must be had to SNPs found in hTRPV1 when attempting to develop analgesics for pain which depends on TRPV1 activation and in treating that pain. Finally, the finding that the T469I mutation increased the sensitivity of the molecule to heat, but reduced its sensitivity to depolarisation, suggests that the various sensors in TRPV1 may be coupled allosterically rather than directly.
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Helps, Stephen. "Cerebral blood flow in rats after treatment with the primary sensory neurotoxin capsaicin." Title page, contents and summary only, 1987. http://web4.library.adelaide.edu.au/theses/09SM/09smh484.pdf.
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Reinöhl, Jochen. "Adenosintriphosphat und Capsaicin als Auslöser von Muskelschmerz eine Untersuchung an mechanosensitiven Gruppe-IV-Muskelafferenzen der Ratte." Saarbrücken VDM Verlag Dr. Müller, 2006. http://d-nb.info/99125841X/04.
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Mapplebeck, Sarah. "Molecular mechanisms of sensitization of VRI, the heat and capsaicin receptor." Thesis, King's College London (University of London), 2002. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.398258.
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Holland, Susan Stephanie. "Studies on enzymes of the capsaicin biosynthetic pathway in Capsicum frutescens." Thesis, University of Edinburgh, 1989. http://hdl.handle.net/1842/10962.
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Rempe, Torge [Verfasser]. "Spinale und Supraspinale Verarbeitung Capsaicin-induzierter Allodynie und Hyperalgesie / Torge Rempe." Kiel : Universitätsbibliothek Kiel, 2015. http://d-nb.info/1069814571/34.
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Hoffmeister, Carin Gorete Hendges. "PAPEL DO RECEPTOR TRPV1 NA NOCICEPÇÃO E NO EDMA INDUZIDO POR CRISTAIS DE URATO MONOSSÓDICO EM RATOS." Universidade Federal de Santa Maria, 2009. http://repositorio.ufsm.br/handle/1/8949.
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Conselho Nacional de Desenvolvimento Científico e TecnológicoGout is characterized by the deposition of monosodium urate (MSU) crystals. Despite being one of the most painful forms of arthritis, gout and the mechanisms responsible for its acute attacks are poorly understood. In the present study, we found that MSU caused dose-related nociception (DE50=0.04 (0.01-0.11) mg/paw) and edema (DE50=0.08 (0.04-0.16) mg/paw) when injected into the hind paw of rats. Treatment with the selective TRPV1 receptor antagonist SB366791 largely inhibited nociceptive and edematogenic responses to MSU. Moreover, the desensitization of capsaicin-sensitive afferent fibers as well as the pretreatment with the tachykinin NK1 receptor antagonist RP 67580 also significantly reduced MSU-induced nociception and edema. Once MSU was found to induce mast cell stimulation, we investigated the participation of these cells on MSU effects. Prior degranulation of mast cells by repeat treatment with compound 48/80 decreased MSU-induced nociception and edema or histamine and serotonin levels in the injected tissue. Moreover, pretreatment with the mast cell membrane stabilizer cromolyn effectively inhibited nociceptive and edematogenic responses to MSU. MSU induced a release of histamine, serotonin and tryptase in the injected tissue, confirming mast cell degranulation Furthermore, the antagonism of histaminergic H1 and serotoninergic receptors decreased the edema, but not the nociception, of MSU. Finally, the inhibition of tryptase activity was capable of largely reducing either MSU-induced nociception or edema. Collectively, the present findings demonstrate that MSU produces a nociceptive and edematogenic response mediated by TRPV1 receptor activation and mast cell degranulation.
A gota é caracterizada pela deposição de cristais de urato monossódico (MSU) nas articulações. Apesar de ser um dos mais dolorosos tipos de artrite, os mecanismos responsáveis pela indução da dor durante os ataques agudos de gota são pouco entendidos. No presente estudo, objetivamos investigar o papel do receptor TRPV1 na nocicepção e edema induzidos por cristais de MSU em ratos. Assim, demonstramos que o MSU causa nocicepção (DE50=0.04 (0.01-0.11) mg/pata) e edema dependentes da dose (DE50=0.08 (0.04-0.16) mg/pata) quando injetado na pata dos ratos. O tratamento com o antagonista seletivo do receptor vanilóide TRPV1 SB 366791 inibiu significativamente as respostas nociceptiva e edematogênica causadas pelo MSU. De maneira semelhante, a dessensibilização de fibras aferentes sensíveis a capsaicina bem como o tratamento com o antagonista do receptor para taquicinina NK1 RP67580 também reduziram significativamente a nocicepção e o edema induzidos pelo MSU. Sabendo que estudos prévios demonstraram que MSU induz a estimulação de mastócitos, nós investigamos a participação destas células nos efeitos do MSU. A desgranulação prévia de mastócitos por tratamento repetido com o composto 48/80 reduziu a nocicepção e o edema induzidos pelo MSU assim como os níveis de histamina e serotonina no tecido injetado. Adicionalmente, o tratamento com o estabilizador de membrana de mastócitos cromolina, reduziu efetivamente as respostas nociceptivas e edematogênicas ao MSU. A administração de MSU induziu a liberação de histamina, serotonina e triptase no tecido injetado, confirmando a desgranulação mastocitária. Além disso, o antagonismo de receptores histaminérgicos H1 e serotoninérgicos, reduziram o edema, mas não a nocicepção causados pelo MSU. Finalmente, a inibição da atividade da triptase foi capaz de reduzir amplamente a nocicepção e o edema induzidos pelo MSU. Coletivamente, nossos resultados demonstram que o MSU produz uma resposta nociceptiva e edematogênica mediada pela ativação do receptor TRPV1 e pela desgranulação de mastócitos.
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Nogueira, Luciane de Souza Romero. "Efeito do análogo capsiate (Capsicum annuum) sobre a termogênese e perfil lipídico de ratas Wistar obesas e não obesas." Universidade do Oeste Paulista, 2013. http://bdtd.unoeste.br:8080/tede/handle/tede/275.
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Previous issue date: 2013-08-26The aim of the study was to evaluate the effect of analogous capsiate (Capsicum annuum) on thermogenesis and lipid profile of Wistar obese and non-obese. We used 64 Wistar rats, 60 days old and weighing 200g. The animals were divided into four groups (n = 16), where they received treatment for six weeks: control group (C) fed a commercial (Labina ®) and filtered water (placebo), Group Control + Capsiate (CC) : fed a commercial (Labina ®) and capsiate; Obese Group (The): fed with high fat diet and filtered water (placebo); capsiate group O + (OC): fed with high fat diet and capsiate. For evaluation of thermogenesis were measured every seven days during the experiment, rectal body temperature and weight of the rats. At 7 weeks the animals were anesthetized and euthanasia performed by exsanguination by cardiac puncture for lipid profile determination through the measurement of triglycerides, total cholesterol and HDL-Col (high density lipoprotein). The results showed an increase in temperature of the OC group, as well as increased levels of HDL-Chol in the supplemented groups (OC and CC). It is concluded that supplementation with capsiate briefly increased thermogenesis by speeding up metabolism and positively influencing the levels of HDL-Chol and can be used as another form of treatment of obesity. Further studies are needed to evaluate the potentiation of the effect of capsiate associated with regular physical activity and a balanced diet.
O objetivo do estudo foi avaliar o efeito do análogo capsiate (Capsicum annuum) sobre a termogênese e perfil lipídico de ratas Wistar obesas e não obesas. Foram utilizadas 64 ratas Wistar, com 60 dias de idade e peso médio de 200g. Os animais foram divididos em quatro grupos (n=16), onde receberam os tratamentos por seis semanas: Grupo Controle (C): alimentados com dieta padrão comercial (Labina®) e água filtrada (placebo); Grupo Controle+Capsiate (CC): alimentados com dieta padrão comercial (Labina®) e capsiate; Grupo Obeso (O): alimentados com dieta hiperlipídica e água filtrada (placebo); Grupo Obeso+Capsiate (OC): alimentados com dieta hiperlipídica e capsiate. Para avaliação da termogênese, foram aferidos a cada sete dias, durante o experimento, a temperatura corporal retal e o peso das ratas. Na 7ª semana os animais foram anestesiados e a eutanásia realizada através de exanguinação por punção cardíaca para determinação do perfil lipídico por meio da dosagem dos triglicérides, colesterol total e fração HDL-Col (lipoproteína de alta densidade). Os resultados evidenciaram um aumento de temperatura do grupo OC, bem como elevação dos níveis de HDL-Col nos grupos suplementados (CC e OC). Conclui-se que a suplementação com capsiate por curto tempo, aumentou a termogênese, acelerando o metabolismo e influenciando positivamente os níveis de HDL-Col, podendo ser utilizada como mais uma forma de tratamento da obesidade. Novos estudos são necessários para avaliar a potencialização do efeito do capsiate associado à atividade física regular e alimentação balanceada.
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Carlos, Teresa Cristina de Freitas. "Avaliação de extratos vegetais na produção de frangos de corte." Universidade de São Paulo, 2012. http://www.teses.usp.br/teses/disponiveis/10/10135/tde-27092013-122318/.
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Foram desenvolvidos três experimentos para avaliação de uma mistura de extratos vegetais de orégano, pimenta e canela na produção de frangos de corte: Experimento I - Utilizou-se 320 pintos machos de um dia de idade da linhagem Cobb 500, distribuídos em delineamento experimental inteiramente casualisado com quatro tratamentos (0, 75, 150 e 225 ppm de extratos vegetais) com dez repetições de oito aves cada, criadas até 21 dias para determinação da digestibilidade dos nutrientes das dietas, pela metodologia de coleta do conteúdo ileal. Experimento II - Utilizou-se 600 pintos machos de um dia de idade da linhagem Cobb 500, distribuídos em delineamento experimental inteiramente casualisado com cinco tratamentos (Controle Positivo (CP) com 54 ppm de Bacitracina de Zinco; Controle Negativo (CN) sem aditivos melhoradores de desempenho; CN com a adição de 75 ppm; 150 ppm e 225 ppm de extratos vegetais) com dez repetições de doze aves cada para avaliação de desempenho e características de carcaça. Experimento III - Utilizou-se 600 pintos machos de um dia de idade da linhagem Cobb 500, distribuídos em delineamento experimental inteiramente casualisado com cinco tratamentos (Controle Positivo (CP) com 54 ppm de Bacitracina de Zinco; Controle Negativo (CN) sem aditivos melhoradores de desempenho; CP até 33 dias e posteriormente substituído pelo CN, no período de 34 a 42 dias de idade, com a adição de 75 ppm; 150 ppm e 225 ppm de extratos vegetais) com dez repetições de doze aves cada para avaliação de desempenho e características. Todos os dados foram analisados pelo Statistical Analysis System (SAS Institute Inc., 2008), submetidos à análise de regressão polinomial pelo procedimento GLM ao nível de 5% de significância. No experimento I, não foi observado efeito significativo entre os tratamentos para digestibilidade ileal da energia bruta, e a digestibilidade ileal da proteína bruta e dos aminoácidos apresentou efeito quadrático (P<0,05). No experimento II o consumo de ração não apresentou efeito significativo entre os tratamentos, já para ganho de peso e conversão alimentar foi observado efeito significativo (P<0,05) na comparação entre o antibiótico e os níveis de extratos vegetais adicionados a dieta. No experimento III, não foi observado efeito significativo entre os tratamentos para consumo de ração e ganho de peso, mas a conversão alimentar apresentou efeito significativo (P<0,05) na comparação entre o antibiótico e os níveis de extratos vegetais adicionados a dieta. Nos experimentos II e III, para as características de carcaça não foram observados efeitos significativos (P<0,05) entre os tratamentos. Concluiu-se que a inclusão de uma mistura de extratos vegetais de orégano, pimenta e canela na dieta de frangos de corte em substituição aos aditivos melhoradores de desempenho proporcionou maior digestibilidade ileal da proteína bruta e dos aminoácidos, e de acordo com os níveis praticados, os extratos vegetais não proporcionaram efeitos positivos no desempenho quando comparados com o tratamento com antibiótico, no período total de criação. Entretanto, o fornecimento na fase final apresentou um comportamento diferente, melhorando o rendimento de peito.We developed three experiments to evaluate a mixture of herbal extracts of oregano, pepper and cinnamon in the production of broilers: Experiment I - was used 320 male chicks from one day old Cobb 500, distributed in completely randomized design with four treatments (0, 75, 150 and 225 ppm of plant extracts) with ten replicates of eight birds each, created up to 21 days to determine the nutrient digestibility of diets, the collection methodology of the ileal content. Experiment II - was used 600 male chicks from one day old Cobb 500, distributed in completely randomized design with five treatments (Positive Control (PC) with 54 ppm Bacitracin Zinc; Negative Control (NC) without enhancing additives performance; CN with the addition of 75 ppm, 150 ppm and 225 ppm of plant extracts) with ten replicates of twelve chicks each to assess performance and carcass characteristics. Experiment III - was used 600 male chicks from one day old Cobb 500, distributed in completely randomized design with five treatments (Positive Control (PC) with 54 ppm Bacitracin Zinc; Negative Control (NC) without enhancing additives performance; CP up to 33 days and subsequently replaced by CN, from 34 to 42 days of age, with the addition of 75 ppm, 150 ppm and 225 ppm plant extracts), with ten replicates of twelve chickens each for performance evaluation and characteristics. All data were analyzed using Statistical Analysis System (SAS Institute Inc., 2008), submitted to polynomial regression analysis by GLM procedure at the 5% level of significance. In the first experiment, no significant effect was observed between treatments for ileal digestibility of raw energy and ileal digestibility of crude protein and amino acids showed a quadratic effect (P <0.05). In experiment II feed intake had no significant effect between treatments, as for weight gain and feed conversion was no significant effect (P <0.05) in the comparison between the antibiotic and the levels of plant extracts added to the diet. In experiment III, no significant effect was observed between treatments for feed intake and weight gain, feed conversion but significant effect (P <0.05) in the comparison between the antibiotic and the levels of plant extracts added to the diet. In experiments II and III, for carcass traits were not significant effects (P <0.05) among treatments. It was concluded that the inclusion of a mixture of herbal extracts of oregano, pepper and cinnamon in the diet of broilers in place of performance enhancing additives provided higher ileal digestibility of crude protein and amino acids, and according to the levels prevailing, vegetable extracts yielded no positive effect on performance when compared with the antibiotic treatment, the total periods. However, the provision in the final phase showed a different behavior by improving the yield of breast.
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Orndorff, Brandy Michelle-Woolsey. "Comparison of Prophylactic or Therapeutic Dietary Administration of Capsaicin Oleoresin for Resistance to Salmonella in Broiler Chickens." Thesis, Virginia Tech, 2004. http://hdl.handle.net/10919/33812.
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Expt. 1 evaluated effects of 0 or 10 ppm CAP in the starter phase (d 1-16) on chicks challenged with SE on d of age. Therapeutic inclusion of 10ppm CAP increased (P < 0.05) L/S and ceca positives. In Expt. 2, capsaicin oleoresin (CO) was included in finisher diets (d 30-37) at 0, 5, or 20 ppm with SE challenge on day 31. Inclusion of 5 ppm CO increased (P < 0.05) ceca SE positives and demonstrated 1.05 and 1.39-log fewer SE cfu at CO concentration of 5 or 20 ppm, respectively. A linear decrease (P < 0.05) in lamina propria thickness of SE challenged birds was observed with increased CO. Expt. 3 evaluated prophylactic CO treatment at 0, 5, or 20 ppm in starter, grower, and finisher diets for resistance to SE or ST challenge on d 14 or 29. With challenge on d 14, 5 ppm CO reduced ceca (P<0.005) SE positives and 1.1-log fewer SE cfu. Likewise, 20 ppm CO reduced (P < 0.05) SE ceca positives. Salmonella typhimurium isolation rate was reduced (P<0.05) with 5 ppm CO, and ST cfu were reduced 1.4-log with 5 ppm CO compared to 20 ppm. Lamina propria thickness increased (P < 0.05) linearly as CO concentration increased. With d 29 challenge birds fed 5 ppm CO exhibited 1.08-log fewer SE cfu, and 20 ppm CO reduced L/S positives (P < 0.025) for SE and resulted in 1.39-log fewer SE cfu. Lamina propria thickness decreased with 5 ppm CO and SE or ST challenge compared to non-challenged birds fed 5 ppm (P < 0.0005). An increase was observed in ST or SE, birds fed 20 ppm CO compared to non-challenged, birds fed 20 ppm CO (P < 0.01). No differences were observed in mast cell number in either Expt. 2 or 3.
These data provide evidence that prophylactic or therapeutic dietary CAP differentially affect broiler susceptibility to Salmonella and prophylactic administration may provide non-antibiotic means to reduce Salmonella in broilers.
Master of Science
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Albanese, Marie-Claire. "Dissociation of the mechanisms of capsaicin actions on thermal and inflammatory pain." Thesis, McGill University, 2001. http://digitool.Library.McGill.CA:80/R/?func=dbin-jump-full&object_id=30805.
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Capsaicin was applied to the sciatic and saphenous nerves of rats under anaesthesia. The time-course of the response to intraplantar formalin and formalin-induced c-FOS expression and alterations in substance P (SP) immunoreactivity (IR) were assessed in capsaicin-treated rats. The foot withdrawal latency to 48°C water was also recorded from 1--75 days after surgery. Formalin-induced pain was reduced by both capsaicin and its vehicle at the earliest test, 3 days after surgery. Formalin pain in the vehicle-treated group recovered by 14 days, and scores in the capsaicin-treated group remained depressed until 28 days. By 75 days, capsaicin-treated rats were hyperalgesic in the first phase. Thermal hyposensitivity was apparent from the first day after surgery until day 75. Capsaicin reduced c-FOS IR and both treatments reduced SP IR at day 14. Thermal hypoalgesia occurs prior to changes at the terminals of unmyelinated afferents and may involve depletion of peptides in the periphery due to disrupted axonal transport. The effects on formalin-induced pain may be due to axonal transport disruption, and by desensitization of the afferents.
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Berry, Danica. "Effect of oral cavity loci and cultural background on responses to capsaicin." The Ohio State University, 2020. http://rave.ohiolink.edu/etdc/view?acc_num=osu1586358754553389.
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Gewehr, Camila de Campos Velho. "CONTRIBUIÇÃO DO RECEPTOR VANILOIDE NA NOCICEPÇÃO INDUZIDA PELA INJEÇÃO PERIFÉRICA DE POLIAMINAS EM CAMUNDONGOS." Universidade Federal de Santa Maria, 2010. http://repositorio.ufsm.br/handle/1/8976.
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Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorPolyamines (putrescine, spermidine and spermine) are important endogenous regulators of ion channels, such as vanilloid (TRPV1), glutamatergic (NMDA or AMPA/kainate) and acid-sensitive (ASIC) receptors. In the present study, it was investigated the possible nociceptive effect induced by polyamines and the mechanisms involved in this nociception in vivo and in vitro. The subcutaneous (s.c.) injection of capsaicin, spermine, spermidine or putrescine produced nociception with ED50 of 0.16 (0.07-0.39) nmol/paw, 0.4 (0.2-0.7) μmol/paw, 0.3 (0.1-0.9) μmol/paw and 3.2 (0.9-11.5) μmol/paw, respectively. The antagonists of NMDA (MK801, 1 nmol/paw), AMPA/kainate (DNQX, 1 nmol/paw) or ASIC receptors (amiloride, 100 nmol/paw) failed to reduce the spermine-trigged nociception. However, the TRPV1 antagonists capsazepine or SB366791 (1 nmol/paw) reduced spermine-induced nociception, with inhibition of 81±10 and 68±9%, respectively. The previous desensitization with resiniferatoxin (RTX) largely reduced the spermine-induced nociception and TRPV1 expression in the sciatic nerve, with reductions of 82±9% and 67±11%, respectively. Furthermore, the combination of spermine (100 nmol/paw) and RTX (0.005 fmol/paw), in doses which alone were not capable of inducing nociception, produced nociceptive behaviors. Moreover, different concentrations of spermine (3-300 μM) enhanced the specific binding of [3H]-RTX to TRPV1 receptor. Altogether, polyamines produce spontaneous nociceptive effect through the stimulation of TRPV1, but not of ionotropic glutamate or ASIC receptors.
As poliaminas (putrescina, espermidina e espermina) são importantes reguladores endógenos de canais iônicos como o receptor vaniloide (TRPV1), os receptores glutamatérgicos (NMDA ou AMPA/cainato) e o canal iônico sensível ao ácido (ASIC). No presente estudo, investigou-se o possível efeito nociceptivo induzido por poliaminas e o mecanismo envolvido nesta nocicepção in vivo e in vitro. A injeção subcutânea (s.c.) de capsaicina, espermina, espermidina e putrescina produziram nocicepção com DE50 de 0,16 (0,07-0,39) nmol/pata, 0,4 (0,2-0,7) μmol/pata, 0,3 (0,1-0,9) μmol/pata e 3,2 (0,9-11,5) μmol/pata, respectivamente. Os antagonistas dos receptores NMDA (MK801, 1 nmol/pata), AMPA/cainato (DNQX, 1 nmol/pata) ou ASIC (amiloride, 100 nmol/pata) não reduziram a nocicepção induzida por espermina. Porém, os antagonistas do receptor TRPV1 capsazepina (1 nmol/pata) e SB366791 (10 nmol/pata) reduziram a nocicepção induzida por espermina, com inibições de 81±10 e 68±9%, respectivamente. A dessensibilização prévia com resiniferatoxina (RTX) reduziu a nocicepção induzida por espermina e a expressão de TRPV1 no nervo ciático, com reduções de 82±9% e 67±11%, respectivamente. Além disso, a combinação de espermina (1 nmol/pata) e RTX (0,005 fmol/pata), em doses que separadamente não são eficientes em induzir nocicepção, produziu comportamento nociceptivo. Finalmente, diferentes concentrações de espermina (3-300 μM) aumentaram a ligação específica de [3H]-RTX ao receptor TRPV1. Assim, os resultados demonstram que poliaminas produzem efeito nociceptivo espontâneo através da estimulação de receptor TRPV1, mas não de receptores glutamatérgicos ionotrópicos ou canal iônico sensível a ácido.
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Santos, Gabriela Trevisan dos. "CARACTERIZAÇÃO DO ESTERÓIDE α-ESPINASTEROL COMO UM NOVO ANTAGONISTA DO RECEPTOR TRPV1 COM EFEITO ANTINOCICEPTIVO." Universidade Federal de Santa Maria, 2011. http://repositorio.ufsm.br/handle/1/11182.
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Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorThe transient receptor potential vanilloid 1 (TRPV1) is relevant to the perception of noxious information and has been studied as a therapeutic target for the development of new analgesics. The goal of this study was to perform in vivo and in vitro screens to identify novel, efficacious, and safe TRPV1 antagonists isolated from leaves of the medicinal plant Vernonia tweedieana Baker. All of the fractions and the hydroalcoholic extract produced antinociception in mice during the capsaicin test, but the dichloromethane fraction (Dcm) also had antioedematogenic effect. Among the compounds isolated from the Dcm fraction, only α-spinasterol reduced the nociception and oedema induced by capsaicin injection. Moreover, α-spinasterol demonstrated good oral absorption and high penetration into the brain and spinal cord of mice. Besides, α-spinasterol was able to displace [3H]-resiniferatoxin (RTX) binding and diminish calcium (Ca2+) influx mediated by capsaicin. Orally administration of the Dcm fraction and α-spinasterol also produced antinociceptive effect in the noxious heat-induced nociception test; however, they did not change the mechanical threshold of naive mice. The treatment with α-spinasterol did not produce antinociceptive effect in mice systemically pre-treated with RTX. In addition, α- spinasterol and the Dcm fraction also reduced the oedema, mechanical and heat hyperalgesia elicited by complete Freund s adjuvant (CFA) paw injection. The Dcm fraction and α-spinasterol did not affect body temperature or locomotor activity. In conclusion, α-spinasterol is an efficacious and safe antagonist of the TRPV1 receptor with antinociceptive effect.
O receptor de potencial transitório vanilóide 1 (TRPV1) é relevante para a percepção de estímulos nocivos e tem sido estudado como um alvo terapêutico para o desenvolvimento de novos analgésicos. O objetivo deste estudo foi desenvolver uma triagem in vivo e in vitro para caracterizar novos antagonistas do receptor TRPV1 isolados das folhas de Vernonia Tweedieana Baker, uma planta medicinal, com atividade antinociceptiva em camundongos. Todas as frações e o extrato hidroalcólico apresentaram efeito antinociceptivo no teste da capsaicina, sendo que a fração diclorometano (Dcm) também mostrou efeito antiedematogênico. Entre os compostos isolados da fração Dcm, apenas o α-espinasterol reduziu a nocicepção e o edema induzidos pela injeção intraplantar de capsaicina. Além disso, o α- espinasterol foi capaz de deslocar o radioligante [3H]-resiniferatoxina, e também de diminuir o influxo de cálcio estimulado pela capsaicina. A fração Dcm e o composto α-espinasterol apresentaram efeito anti-hiperalgésico na nocicepção induzida por estímulo térmico, mas não induzida por estímulo mecânico em animais sem injúria. Porém, o composto α-espinasterol não apresentou atividade antinociceptiva em animais pré-tratados sistemicamente com resiniferatoxina. Este composto e a fração Dcm foram capazes de reduzir a hiperalgesia mecânica e térmica, e também o edema induzidos por adjuvante completo de Freund. A fração Dcm e o α- espinasterol não foram capazes de induzir alteração na temperatura corporal ou atividade locomotora. Também, o α-espinasterol mostrou boa absorção por via oral, e alta penetração no cérebro e na medula espinhal de camundongos. Assim, o α- espinasterol, isolado da fração Dcm, age como um antagonista do receptor TRPV1 com eficaz efeito antinociceptivo, sem indução de efeitos adversos.
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Fischer, Jenny. "Morphologische und klinische Untersuchungen zur experimentellen Denervation des Ellbogengelenks beim Hund." Doctoral thesis, Universitätsbibliothek Leipzig, 2012. http://nbn-resolving.de/urn:nbn:de:bsz:15-qucosa-87695.
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Die Osteoarthrose (OA) des Ellbogengelenks ist eine der wichtigsten Gelenkerkrankungen des Hundes, die sich aufgrund erblich bedingter Fehlstellung der Gelenke sekundär häufig schon bei sehr jungen Hunden entwickelt und zu einer verminderten Lebensqualität der Tiere führt. Im Laufe der Erkrankung kommt es zu einer Schädigung des Gelenkknorpels, der an Elastizität und Spannkraft verliert und seine Funktion, nicht mehr ausüben kann. Eine Ablösung von Knorpelfragmenten und Entzündungen im Gelenk können die Zerstörung des Gelenkknorpels beschleunigen. Die OA ist nicht heilbar. Das Therapieziel ist eine möglichst vollständige Schmerzreduktion und die Verbesserung der Lebensqualität. Eine chirurgische Denervation ist im Ellbogengelenk des Hundes ohne Traumatisierung anatomischer Strukturen nicht möglich.
Ziel der vorliegenden Arbeit war es, erstmalig einen experimentellen Ansatz zur chemischen Denervation sensibler Gelenkafferenzen im Ellbogengelenk beim Beagle mit dem Neurotoxin OX7-Saporin durchzuführen. Zusätzlich wurden Substanzen aus der Humanmedizin zur Schmerzreduktion und symptomatischen Therapie der OA am Hund erprobt und der Therapieerfolg evaluiert.
Im Rahmen eines Therapieversuches in der Klinik für Kleintiere der Universität Leipzig wurde bei zwei, an OA erkrankten Hunden Capsaicin einmalig intraartikulär injiziert. Der erste Hund erhielt intraartikulär 250 mg Capsaicin. Dieser Patient zeigte Nebenwirkungen in Form einer Herz- und Atemfrequenzerhöhung, starker Schmerzhaftigkeit und neurologischen Symptomen. Der zweite Hund wurde mit 83 mg Capsaicin behandelt und zeigte keine Nebenwirkungen. Sowohl die Bewertung der Besitzer als auch die orthopädische Untersuchung ergaben keine Verbesserung der Lahmheit.
Vier kranken Hunden wurde ebenfalls im Rahmen eines Therapieversuches Botox (Botulinumtoxin A) intraartikulär einmalig injiziert. Drei Hunde wurden mit 50 Einheiten, ein Hund mit 100 Einheiten Botox behandelt. Die Applikation von Capsaicin und Botox führten zu keiner Verbesserung der Symptomatik.
In der Humanmedizin ist die Schmerzbehandlung mit Capsaicin und Botox erfolgreich. Deshalb sollten diese Therapieansätze auch für die Anwendung beim Hund weiter optimiert werden.
Das Neurotoxin OX7-Saporin wurde in einer Dosierung von 100 µg erstmalig in das Ellbogengelenk von drei Beagle-Hündinnen appliziert, um eine sensible Denervation des Gelenkes zu erreichen. Der retrograde Transport des Ribosomen-inaktivierenden Proteins in die Perikarya der Spinalganglienzellen, die das Ellbogengelenk sensibel innervieren, sollte eine selektive Zerstörung der Neurone durch das Neurotoxin bewirken. Der retrograde Tracer Fluoro-Gold wurde, zur Kontrolle der Wirkung des Neurotoxins, nach einer Wartezeit von 15 Tagen intraartikulär in das linke und das rechte Ellbogengelenk appliziert. Fluoro-Gold kann ausschließlich von intakten Nervenfasern transportiert werden. Die Ganglien C4 - Th3 wurden bilateral zur histologischen Auswertung entnommen und in Paraffin eingebettet. Zur Bestimmung der Gesamtneuronenanzahl wurden alle Neurone in jedem dritten Schnitt eines Ganglions gezählt. Die Summe dieser Nervenzellen ergab die Gesamtneuronenanzahl eines Ganglions.
Die Einlagerung von Lipofuszin führte zu einer starken Autofluoreszenz im Zytoplasma der Neuronen. Alle Schnitte wurden mit Sudan-Schwarz gefärbt, um die Autofluoreszenz von der retrograden FG-Markierung zu unterscheiden. Die FG-Markierung konnte nur in den Ganglien C6 und Th1 im Zytoplasma sehr weniger Neuronen dokumentiert werden. Der histologische Nachweis einer Neurodegeneration nach Applikation des Neurotoxins OX7-Saporin in das linke Ellbogengelenk war negativ. In den untersuchten Spinalganglien wurden intakte Nervenzellen nachgewiesen.
Auch die bilaterale intraartikuläre Injektion des retrograden Tracers FG war nicht erfolgreich.
Aus den Ergebnissen dieser experimentellen Ansätze wird zusammenfassend geschlussfolgert:
Ø Vor der Durchführung zukünftiger experimenteller Untersuchungen beim Hund muss die optimale Konzentration und die Wartezeit für das Neurotoxins OX7-Saporin ermittelt werden.
Ø Die Rezeptoren für OX7-Saporin müssen an den Nervenzellen des Hundes zweifelsfrei nachgewiesen werden, bevor das Neurotoxin im caninen Tiermodell eingesetzt werden kann.
Ø Die optimale Konzentration des Fluoreszenzfarbstoffes FG für intraartikuläre Injektionen und dessen retrograde Transportgeschwindigkeit beim Hund müssen ermittelt werden, bevor dieser Tracer wieder im Tierexperiment eingesetzt werden kann.
Ø FG wurde als 1,8%ige Lösung in das Ellbogengelenk beim Beagle appliziert. Diese Konzentration war wahrscheinlich zu gering, um eine retrograde Markierung der sensiblen Neurone in den entsprechenden Spinalganglienzellen nachzuweisen.
Ø Die intraartikuläre Applikation des Neurotoxins OX7-Saporin führte nicht zur selektiven Neurodegeneration. Eine Aussage zur Schmerzausschaltung und symptomatischen Therapie der OA des Hundes mit OX7-Saporin ist deshalb nicht möglich.
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Jones, Christopher M. "Expression and folding studies of the ankyrin repeat domain of the capsaicin receptor." Click here for download, 2006. http://wwwlib.umi.com/cr/villanova/fullcit?p1432833.
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Grimes, Jeffrey Scott. "The impact of a noise stressor on capsaicin-induced primary and secondary hyperalgesia." Thesis, Texas A&M University, 2003. http://hdl.handle.net/1969.1/249.
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In searching for new human pain models that more closely resemble clinical pain states, the capsaicin pain model has emerged as a viable model for both inflammatory and neuropathic pain states. A principal benefit of the capsaicin model is that it allows study of two different pain processes, primary and secondary hyperalgesia. Primary hyperalgesia is characterized by spontaneous pain and both heat and mechanical hyperalgesia. In addition, it is likely the result of activation and sensitization of both peripheral and central nociceptors. In contrast, secondary hyperalgesia is characterized by only mechanical hyperalgesia and is caused by the sensitization of central nociceptive neurons. Previous research utilizing the capsaicin pain model has primarily focused on the neural properties with little focus on the impact of affective states on capsaicin-related pain processes. The present study examined the impact of a noise stressor on both primary and secondary hyperalgesia. Results indicated that the effects of the noise stressor impacted secondary hyperalgesia, but not primary hyperalgesia.
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Calva-Calva, Graciano. "Glycosylation and synthesis of capsaicin in cell cultures and fruits of Capsicum SPP." Thesis, University of East Anglia, 1997. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.389324.
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Opheim, Maximilian Nicholas. "Effect of Capsaicin Supplementation on Performance of and Physiological Response to Repeated Sprinting." Thesis, Virginia Tech, 2010. http://hdl.handle.net/10919/41217.
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Aim: Fatigue during team sports requiring multiple sprints can result from the combined effects of metabolic, mechanical, neurological, and immune factors. The purpose of this study was to investigate the influence of capsaicin on performance of and the physiological response to an exercise test simulating the fitness demands of team sport game conditions. Methods: This study was a placebo-controlled, crossover design. Nineteen healthy male experienced athletes age 18-30 yr consumed either 3 g/d cayenne (25.8 mg/d capsaicin) or placebo for 1 wk. Directly following the supplementation period, they completed a repeated sprint test consisting of 15 30 m maximal effort sprints on 35 s intervals. Sprint times were recorded via electronic dual-beam timing system. Fasted blood draws for interleukin-6 (IL-6) were taken at baseline prior to supplementation, 45-min pretest, and immediately post test. Heart rate (HR), blood pressure (BP), rate of perceived exertion (RPE), muscle soreness (MS), and gastrointestinal distress (GD) were measured 1-min pretest, during, posttest, and 1-min posttest. MS was also measured for 3 d posttest. Results: Relative to the placebo, capsaicin significantly reduced maximum HR by 9.3%, total average HR by 8.5%, and sprinting average HR by 6.0% (P<0.05). Capsaicin caused GD of at least 2/5 in 24.5% of subjects. There was no difference between treatments in fastest or mean sprint time, fatigue, percent change or difference in IL-6, BP, RPE, sprint or posttest MS. Conclusion: Capsaicin did not influence repeated sprint performance or the inflammatory response, but reduced HR during intense activity and causes substantial GD.Master of Science
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Silva, Cássia Regina da. "ENVOLVIMENTO DO RECEPTOR TRPA1 NA RESPOSTA INFLAMATÓRIA INDUZIDA PELA ADMINISTRAÇÃO TÓPICA DE CINAMALDEÍDO EM CAMUNDONGOS." Universidade Federal de Santa Maria, 2011. http://repositorio.ufsm.br/handle/1/11180.
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Coordenação de Aperfeiçoamento de Pessoal de Nível SuperiorCinnamaldehyde, a natural compound frequently present in cosmetic formulations, induces skin irritation when topically applied, but the mechanism by which cinnamaldehyde produces such skin reactions is unclear. Here, we showed that cinnamaldehyde induced ear edema in mice (1-6 μg/ear) with a maximum effect with 4 μg/ear (Emax of 0.18 ± 0.02 mm and an ED50 value of 2.0 (1.1- 3.4 μg/ear). Cinnamaldehyde can induce leukocyte infiltration detected by an increase in MPO activity and confirmed by histological analyses. The edema and cellular infiltration evoked by 4 μg/ear of cinnamaldehyde was prevented through topical application of ruthenium red, a non selective TRP antagonist or by camphor and HC030031, two TRPA1 receptor antagonists. In contrast, the edema and the leukocyte infiltration was unaffected by the TRPV1 receptor antagonist SB366791. Cinnamaldehydeinduced edema but not cellular infiltration was also prevented though topical application of the tachykinin NK1 antagonist aprepitant, indicating a neuropeptides release phenomenon in this process. Also, we observed that repeated topical applications of cinnamaldehyde (4 μg/ear) did not induced sensitization/desensitization alterations. Interestingly, the TRPV1 antagonist, capsaicin, repeated treatment abrogated its edematogenic response, confirming the desensitization process and decrease partially the cinnamaldehyde induced edema, suggesting the involvement of capsaicin-sensitive fibers and additional targets in cinnamaldehyde response. The present results demonstrated that cinnamaldehyde induces mouse skin inflammation through a mechanism involved the TRPA1 receptor activation and subsequent leukocyte infiltration. In addition, evidence supports the assumption that the tachykinin NK1 receptor is involved in these inflammatory responses.
O cinamaldeído é um composto natural frequentemente encontrado em formulações cosméticas, capaz de induzir irritação na pele quando aplicado topicamente, porém o mecanismo pelo qual o cinamaldeído produz estas reações ainda é desconhecido. Neste trabalho demonstramos que o cinamaldeído foi capaz de induzir edema de orelha em camundongos (1-6 μg/orelha) com um efeito máximo obtido com a dose de 4 μg/orelha (Emax de 0,18 ± 0,02 mm e um DE50 de 2,0 (1,1- 3,4) μg/orelha). O cinamaldeído foi capaz ainda de induzir infiltração leucocitária detectada por um aumento na atividade da MPO e confirmada por análise histológica. O edema e a infiltração leucocitária iniciados após aplicação tópica de 4 μg/orelha de cinamaldeído foi prevenido pela aplicação tópica de vermelho de rutênio, um antagonista TRP não seletivo, e por cânfora e HC030031, dois antagonistas seletivos TRPA1. Por outro lado, a aplicação de SB366791, um antagonista seletivo TRPV1, não alterou o edema nem a infiltração leucocitária. Ainda, o edema induzido pelo cinamaldeído foi prevenido pela aplicação tópica de aprepitant, um antagonista seletivo do receptor NK1 para taquicininas, sugerindo que a liberação de neuropeptídeos esteja envolvida neste processo. Também foi observado que a aplicação tópica repetida de cinamaldeído 4 μg/orelha não foi capaz de induzir processos de ensibilização/dessensibilização. No entanto, o tratamento repetidocom o antagonista TRPV1, capsaicina, aboliu o edema induzido pela própria capsaicina, confirmando a ocorrência de dessensibilização, e diminuiu parcialmente o edema induzido pelo cinamaldeído sugerindo o envolvimento de fibras sensíveis a capsaicina, além de outras vias, neste processo. Os resultados demonstram que o cinamaldeído induz um processo inflamatório na pele através de um mecanismo que envolve a ativação do receptor TRPA1 e consequente infiltração leucocitária.
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Moraes, Márcia Adriana Miranda. "Análise morfológica e morfometrica de útero, ovário, glândulas Adrenais e perfil lipídico de ratas suplementadas com capsiate." Universidade do Oeste Paulista, 2015. http://bdtd.unoeste.br:8080/tede/handle/tede/318.
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Previous issue date: 2015-06-22Obesity is characterized by excessive accumulation of adipose tissue, of multifactorial origin. In pursuit of weight reduction, individuals use functional foods, for example the Capsiate, CH-19 extract sweet (Capsicum annuum L.), which contains capsinoids, it is a capsaicin analog, not pungent, with thermogenic properties. The capsiate exhibits potent activity against angiogenesis and vascular permeability induced by vascular endothelial growth factor. The study was conducted face lack studies on capsianóides in reproductive organs in the literature. The aim: was to evaluate the effect of capsiate on the histology of the uterus, ovary, adrenal gland and lipid profile of obese and non-obese rats. Material and methods: Sixty-four male Wistar rats were divided into four groups (n = 16): Control; Obese; Capsiate and Capsiate Obeso. Groups Control and Capsiate received commercial feed. Group Obese and Capsiate Obese received palatable high fat die. For groups Capsiate and Capsiate Obese it was administered by gavage 10 mg capsiate diluted in 0.5 ml of filtered water, 1 once day, for groups Control and Obese it was administered by gavage 0,5 ml of filtered water (placebo). After 12 weeks, the animals anesthetized, blood collected and euthanized. Reproductive organs and the adrenal glands they were stained with HE technique and submitted to morphological analysis and morphometric. Statistical analysis, it was verified by the Levene test, was employed (one-way ANOVA), contrasts with the Tukey method. Performed using SPSS 16.0 software and 5% significance level. Results: significant elevation in HDL Col in the groups Capsiate and Capsiate Obese. The thickness of the endometrium was lower (p <0.05) in Capsiate and was observed increase (p <0.05) in the number of secondary follicles and corpus luteum in group Capsiate Obese. The glomerular regions, crosslinked and medullary they had a lower thickness (p <0.05) in Capsiate group compared to the control. Conclusion: The capsiate reduces endometrial proliferation no obese rats, increases the number of corpus luteum in obese rats and induces an increase in HDL-cholesterol, but not prevented increase in body weight of rats. However, further studies are needed to evaluate the effect of capsiate in reproductive organs because of the shortage in the scientific literature.
Obesidade é caracterizada pelo acúmulo excessivo de tecido adiposo, de origem multifatorial. Em busca da redução de peso, indivíduos utilizam alimentos funcionais, como exemplo o Capsiate, CH-19 extrato doce (Capsicum annuum L.), que contém capsinóides, é um análogo de Capsaicina, não pungente, com propriedades termogênicas. O capsiate exibe potente atividade contra a angiogênese e permeabilidade vascular induzida pelo fator de crescimento endotelial vascular. O estudo foi desenvolvido face ausência de estudos sobre capsianóides em órgãos reprodutivos na literatura. O objetivo foi avaliar o efeito do capsiate na histologia do útero, ovário, glândula adrenal e perfil lipídico de ratas obesas e não obesas. Material e Métodos: Sessenta e quatro ratas Wistar divididas em quatro grupos (n=16): Controle; Obeso; Capsiate e Capsiate Obeso. Os Grupos Controle e Capsiate receberam ração comercial. Já Grupo Obeso e Capsiate Obeso receberam dieta palatável hiperlipídica. Para os grupos Capsiate e Capsiate Obeso foi administrado por gavagem 10 mg de capsiate diluído em 0,5 ml de água filtrada, 1 vez dia, para os grupos Controle e Obeso foi administrado por gavagem 0,5 ml de água filtrada (placebo). Após 12 semanas, os animais anestesiados, sangue coletado e eutanasiados. Órgãos reprodutivos e as glândulas adrenais foram corados pela técnica de HE e submetidos à análise morfológica e morfométrica. Análise estatística foi verificada pelo teste de Levene, empregou-se (ANOVA one-way), com contrastes pelo método de Tukey. Realizadas com auxílio do Software SPSS 16.0 e com nível de significância de 5%. Resultados: significativa elevação nos níveis de HDL Col nos grupos Capsiate e Capsiate Obeso. A espessura do endométrio foi menor (p<0,05) no grupo Capsiate e foi observado aumento (p<0,05) no número de folículo secundário e corpos lúteos no grupo Capsiate Obeso. As regiões glomerular, reticulada e medular apresentaram espessura menor (p<0,05) no grupo Capsiate comparado ao Controle. Conclusão: O capsiate reduz proliferação endometrial em ratas não obesas, aumenta o número de corpos lúteos em ratas obesas e induz o aumento do HDL-colesterol, porém não evitou aumento no peso corporal das ratas. Porém, novos estudos são necessários para avaliar o efeito do capsiate em órgãos reprodutivos, devido à escassez na literatura científica.
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Fréo, Bianca. "Estudo clínico da atividade da capsaicina em portadores da Síndrome de Ardência Bucal." Universidade de São Paulo, 2008. http://www.teses.usp.br/teses/disponiveis/23/23139/tde-09042009-120646/.
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A Síndrome de Ardência Bucal (SAB) caracteriza - se por sensação de ardor, com ausência de sinais clínicos ou laboratoriais associados. A etiopatogenia é desconhecida, inexistindo protocolo terapêutico satisfatório. O objetivo deste trabalho foi avaliar a eficácia da aplicação tópica de capsaicina, como alternativa terapêutica, em um grupo de pacientes portadores da SAB, além de investigar, nessa população, indicativos de ansiedade e depressão, correlacionando estes últimos aspectos com a resposta à terapêutica aplicada. Constituiu-se um grupo de vinte indivíduos portadores da síndrome, todos de acordo com os termos do consentimento esclarecido. Quinze sujeitos constituíram o grupo teste (GT) e foram tratados com capsaicina, em aplicações diárias, durante três semanas, repetindo-se o ciclo por quatro semanas após uma semana de intervalo. O grupo controle (GC) foi tratado com o creme base utilizado como veículo da capsaicina, durante o mesmo período. Ambos foram controlados após 30 dias do término da medicação. A evolução dos sintomas foi controlada por escala visual de sintomatologia (EVS) e questionário acerca do efeito global percebido (EGP). A intensidade média do sintoma de ardência antes do início dos ciclos de tratamento, mensurado pela EVS, foi de 5,1 (GT) e 4,4 (GC). Ao final da quarta semana o GT mostrou redução dos sintomas (EVS=3,6), enquanto o GC declarou aumento da sintomatologia (EVS=4,8). No GT, entre a quarta e a oitava semana houve redução dos sintomas da ordem de 8,3%, e entre a oitava e a décima segunda semana observou-se aumento de 13,5% da sintomatologia. No GC houve 22.8% de piora (EVS=5,75) entre o início e a décima segunda semana. Ao EGP houve pelo menos algum alívio do sintoma em seis pacientes (40%) do GT e em um paciente do GC (20%). Quatro pacientes (26,6%) reportaram remissão total do sintoma após tratamento com capsaicina e um paciente (20%) do controle. Para três pacientes do GT e dois do GC não houve modificações do sintoma. Houve relato de piora em dois pacientes (13,3%) do GT e um (20%) do GC. Oito pacientes do GT apresentaram alto nível de ansiedade e sete níveis médios. No GC um paciente apresentou nível baixo, três mostraram valores médios e um classificou-se como alto. Ao CES-D valores indicativos de depressão foram registrados por dez pacientes (66,6%) do GT e 40% (02) do GC. Concluímos que a capsaicina apresentou efetividade no controle da sintomatologia da SAB, parecendo haver correlação com a intensidade inicial de sintomas e manutenção do uso do medicamento. Além disso, houve correlação entre alto nível de ansiedade e indicativos de depressão, embora não se tenha percebido influência destes aspectos sobre a resposta terapêutica.Burning mouth syndrome (BMS) is characterized by an oral burning sensation, with no corresponding clinical signs or laboratory abnormalities. The etiology is unknown, and there was no satisfactory treatment available. The objective of this study was to evaluate the effectiveness of topical use of capsaicin, as an alternative therapy in a group of BMS patients, as well as to correlate anxiety and depression levels to response to the therapy applied. Twenty BMS individuals in accordance to the terms to informed consent comprised the study group. Fifteen subjects were allocated to the test group (TG) and were treated with capsaicin, in daily applications for three weeks, one-week interval and an additional treatment cycle of four weeks. The control group (CG) was treated with the cream base used as a vehicle of capsaicin preparation, during the same period. All patients were examined 30 days after discontinuation of the medication. Results were assessed through a visual analogue scale (VAS) and a questionnaire on the global perceived effect (GPE). The average symptoms intensity before treatment, on EVS, was 5.1 (TG) and 4.4 (CG). At the fourth week control, TG presented reduction on the level of symptoms (EVS = 3.6), while CG presented an increase of symptoms intensity (VAS = 4.8). In the TG, between fourth and eighth week of follow-up, symptoms decreased around 8.3%, and between the eighth and twelfth week there was an increase of 13.5% on symptoms intensity. In the CG it was registered 22.8% of worsening (EVS = 5.75) between the beginning of the study and the twelfth week of control. On GPE assessment, six patients (40%) of TG and one patient of CG (20%), presented some relief of symptoms; four patients TG (26.6%) reported total remission of symptoms after treatment with capsaicin and one patient (20%) of control; three patients of TG and two of the CG remained unaltered. There were reports of worsening in two patients (13.3%) of TG and one (20%) of the CG. Eight patients of TG showed a high level of anxiety and seven moderate levels. In CG one patient presented low level, three showed a moderate level and one was ranked as having a high level of anxiety. CES-D suggested traits of depression in ten patients (66.6%) of TG and 40% (2) of the CG. We concluded that capsaicin is effective in controlling the burning symptom of BMS, suggesting some correlation with initial symptoms intensity and the maintenance of drug use. Moreover, there was some correspondence between high levels of anxiety and traits of depression, but it was not perceived influence of these aspects to the therapeutic response.
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Moraux, Thomas. "Synthesis and evaluation of α-fluoro analogues of capsaicin and 2-(aminomethyl)piperidine derivatives." Thesis, University of St Andrews, 2011. http://hdl.handle.net/10023/2094.
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Chapter 1 gives an overview of the fluorine chemistry field, from its early developments to recent applications in medicinal chemistry. The development of asymmetric electrophilic or nucleophilic installation of fluorine in organic molecules is highlighten. Chapter 2 of this thesis discusses the enantioselective synthesis of α-fluoroamides. The study is applied to the synthesis of fluoroenantiomers of the bioactive molecule capsaicin and short-chain analogues. The biological activity of these compounds is assayed with the TRPV1 receptor. Results show that enantioselective α-fluoroamides (R)-97, (R)-99 and (S)-99 can generate differentiated biological responses, from TRPV1 agonists to TRPV1 antagonists. Chapter 3 focuses on the optimisation and development of 2-(aminomethyl)piperidine (R)-251 dihydrochloride. The development of 2-(aminomethyl)piperidine (R)-251 as its ditetrafluoroborate salt proved to offer excellent reactivity and solubility for the preparation of derivatives. This tetrafluoroborate salt was used to improve the syntheses of organocatalysts 2,2,2-trifluoro-N-(piperidin-2-ylmethyl)acetamide 363 and 4-methyl-N-(piperidin-2-ylmethyl)benzenesulfonamide 364.The catalytic properties of these latter two molecules for asymmetric Mannich reaction is demonstrated. Both (R)-363 and (R)-364 show up to 86% ee, in a typical 20 mol% loading, but loading of (R)-363 as low as 5 mol% still induces the catalysis.
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Heilek, Anna-Maria [Verfasser], and Alwin E. [Akademischer Betreuer] Goetz. "Sensitivierung des Capsaicin- Rezeptors nach Remifentanil- Infusion / Anna-Maria Heilek ; Betreuer: Alwin E. Goetz." Hamburg : Staats- und Universitätsbibliothek Hamburg, 2018. http://d-nb.info/1155304683/34.
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Almeida, Martinha Antunes. "DESENVOLVIMENTO E AVALIAÇÃO DE MICROPARTÍCULAS POLIMÉRICAS CONTENDO CAPSAICINOIDES." UNIVERSIDADE ESTADUAL DE PONTA GROSSA, 2013. http://tede2.uepg.br/jspui/handle/prefix/109.
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Previous issue date: 2013-02-27Capsaicinoids show several therapeutic uses. However they cause pungency in contact with skin and mucosae. In that sense, the aim of this study was to obtain microparticles of poly (-caprolactone) (PCL) containing capsaicinoids for prolonged release through the gastrointestinal tract in order to improve the treatment of obesity. Formulations containing 3, 5 and 10% capsaicinoids were successfully prepared by simple emulsion/solvent evaporation. Values of encapsulation efficiency above 90% were observed for these vanillylamide-loaded microparticles. Microparticles showed spherical shape and smooth surface. The size was suitable for oral use in order to provide a release through the gastrointestinal tract. No chemical bonds were observed between drug and polymer. Microencapsulation led to drug amorphization. Formulations prolonged the release of capsaicinoids without changing the release kinetics (biexponential model). Microencapsulation increased the gastric tolerability of capsaicin and dihydrocapsaicin because it prevented inflammatory processes in the stomach of rats. Microparticles containing 5% capsaicinoids had an effect similar to ranitidine and omeprazole in preventing ulcerative lesions induced by ethanol. This same formulation demonstrated a statistically significant reduction of Lee index, mesenteric fat and retroperitoneal fat in rats with obesity induced by hypothalamic lesion using monosodium L-glutamate. These rats also showed a remarkable improvement in lipid profile and glucose level compared to the control groups. Based on the experimental results, it is possible to suggest that capsaicinoids-loaded PCL microparticles are feasible approaches for the treatment of obesity.
Os capsaicinoides apresentam diversas aplicações terapêuticas, entretanto causam elevada pungência quando em contato com a pele e com as mucosas. Nesse sentido, o objetivo do presente trabalho foi desenvolver micropartículas de poli(-caprolactona) (PCL) contendo capsaicinoides para a liberação prolongada ao longo do trato gastrointestinal, com o propósito de otimizar o tratamento da obesidade. As formulações foram obtidas com sucesso pelo método de emulsão simples e evaporação do solvente, nas concentrações teóricas de 3, 5 e 10% de capsaicinoides. Valores de eficiência de encapsulação acima de 90% foram observados para todas as micropartículas contendo essas vanililamidas. As micropartículas apresentaram formato esférico e superfície lisa. O tamanho foi adequado para uso oral, a fim de permitir uma liberação ao longo do trato gastrointestinal. Não foi verificada a formação de ligações químicas entre o fármaco e o polímero. A microencapsulação promoveu a amorfização do fármaco. As formulações prolongaram a liberação dos capsaicinoides, sem alterar a cinética de liberação (modelo biexponencial). A microencapsulação foi capaz de aumentar a tolerância gástrica da capsaicina e da di-hidrocapsaicina, prevenindo a formação de processos inflamatórios no estômago dos ratos. As micropartículas contendo 5% de capsaicinoides tiveram efeito comparável à ranitidina e ao omeprazol na prevenção de lesões ulcerativas induzidas por etanol. Essa mesma formulação promoveu a redução estatisticamente significativa do índice de Lee, da gordura mesentérica e da gordura retroperitonial de ratos com obesidade induzida por lesão hipotalâmica utilizando L-glutamato monossódico. Esses ratos também apresentaram uma melhora expressiva no perfil lipídico e na glicemia, em comparação aos grupos controle. Com base nos resultados experimentais, é possível sugerir que as micropartículas de PCL contendo capsaicinoides são alternativas viáveis para o tratamento da obesidade.
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Silva, Leonardo Vieira da. "Desenvolvimento de sensores eletroquímicos baseados em nanotubos de carbono e polímeros de ácido ferúlico e capsaicina para detecção e quantificação de 3-nitro-L-tirosina, epinefrina e dopamina." Universidade Federal de Alagoas, 2017. http://www.repositorio.ufal.br/handle/riufal/2096.
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This thesis reports the development of different electrochemical sensors based on carbon nanotubes (CNT) for the detection and determination of analytes of biological relevance, with evaluation of the analytical and kinetic parameters. The work is divided into three parts. In the first part, the electrochemical study of 3-nitro-L-tyrosine (3-NT) in protic medium is described, using the techniques of cyclic voltammetry and differential pulse. The development of a sensor based on CNT for the determination and quantification of 3-NT, is also shown, with a linear range of 10 - 100 μmol L-1 and a detection limit of 0.42 μmol L-1 in the cathodic range. In the anodic range, a linear range of 10 - 60 μmol L-1 and a detection limit of 1.83 μmol L-1 were obtained. In the second part, a sensor was developed based on CNT with electrochemically generated ferulic acid (FA) polymer, generated in situ to determine dopamine (DA). The techniques used to perform this work were cyclic voltammetry and chronoamperometry, which were used to evaluate kinetic and analytical parameters. Through chronoamperometry and the use of the Cottrell equation, the diffusion coefficient (DDA) and catalytic constant (kcat) values determined for DA were 2.48 x 10-6 cm2 s -1 and 1.15 X 104 M-1 s-1, respectively. The amperometric sensor has the following values for the determination of DA: linear range of 5-120 μmol L-1 and limit of detection of 2.2 μmol L-1. The third part describes the development of a nanostructured platform based on CNT and electrochemically oxidized capsaicin (CAP) for the determination of dopamine (DA) and epinephrine (EP). Thus, by means of chronoamperometric studies and Cottrell's equations, it was possible to obtain the values in relation to DA: DDA of 6.97 x 10-4 cm2 s -1 and kcat of 3.12 x 105 M -1 s -1, and in relation to EP, the values obtained were 4.00 × 10 -5 cm 2 s -1 and 2.41 × 104 M-1 s-1 for DEP and kcat, respectively. The amperometric sensor presented the following values in relation to the separate determinations of DA and EP: for DA, linear range of 5-115 μmol L-1 and detection limit of 1.8 μmol L-1; for EP, a linear range of 50-1150 μmol L-1 and a detection limit of 7.2 μmol L-1. Considering the results obtained in this work, the developed sensors justify their use for determination and quantification of 3-nitro-L-tyrosine, dopamine and epinephrine.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
Essa tese apresenta o desenvolvimento de diferentes sensores eletroquímicos baseados em nanotubos de carbono (NTC) para detecção e determinação de analitos de relevância biológica, com avaliação dos parâmetros analíticos e cinéticos. O trabalho encontra-se dividido em três partes. Na primeira parte, descreve-se o estudo eletroquímico, em meio prótico, da 3-nitro-L-tirosina (3-NT), com a utilização das técnicas de voltametria cíclica e de pulso diferencial. Mostra-se, também, o desenvolvimento de um sensor baseado em NTC para a determinação e a quantificação da 3-NT, com obtenção de faixa linear de 10 – 100 mol L-1 e limite de detecção de 0,42 mol L-1 na faixa catódica. Na faixa anódica, foi obtida uma faixa linear de 10 – 60 mol L-1 e limite de detecção de 1,83 mol L-1. Na segunda parte foi desenvolvido um sensor baseado em NTC com polímero eletrogerado de ácido ferúlico (AF), gerado in situ para determinar dopamina (DA). As técnicas empregadas para a realização deste trabalho foram voltametria cíclica e cronoamperometria, as quais foram utilizadas para avaliar parâmetros cinéticos e analíticos. Através de cronoamperometria e com o emprego da equação de Cottrell, os valores de coeficiente de difusão (DDA) e de constante catalítica (kcat), determinados para DA, foram de 2,48 x 10-6 cm2 s-1 e 1,15 x 104 M-1 s-1, respectivamente. O sensor amperométrico permitiu obter os seguintes valores relativos à determinação de DA: faixa linear de 5-120 mol L-1 e limite de detecção de 2,2 mol L-1. Na terceira parte, é descrito o desenvolvimento de uma plataforma nanoestruturada baseada em nanotubos de carbono e polímero eletrogerado por oxidação de capsaícina (CAP) para determinação de dopamina (DA) e epinefrina (EP). Assim, por meio de estudos cronoamperométricos e equações de Cottrell, foi possível obter os valores em relação a DA: DDA de 6,97 x 10-4 cm2 s-1 e kcat de 3,12 x 105 M-1 s-1, e em relação a EP, os valores obtidos foram 4,00 x 10-5 cm2 s-1 e 2,41 x 104 M-1 s-1 para o DEP e kcat, respectivamente. O sensor amperométrico apresentou, em relação às determinações em separado de DA e EP, os seguintes valores: para DA, faixa linear de 5-115 mol L-1 e limite de detecção de 1,8 mol L-1; para EP, faixa linear de 50-1150 mol L-1 e limite de detecção de 7,2 mol L-1. Diante dos resultados obtidos nesse trabalho, os sensores desenvolvidos justificam as suas utilizações para determinação e quantificação de 3-nitro-L-tirosina, dopamina e epinefrina.
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Damião, Mariana Celestina Frojuello Costa Bernstorff. "Planejamento e síntese de análogos da capsaicina e avaliação da atividade antitumoral." Universidade de São Paulo, 2014. http://www.teses.usp.br/teses/disponiveis/9/9138/tde-28042014-145554/.
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O número de casos de câncer tem aumentado significativamente em todo o mundo, principalmente a partir do século passado. Dessa forma, a busca por novas moléculas capazes de combater esta doença é cada vez maior, visto que muitos fármacos utilizados na terapêutica mostram-se tóxicos e pouco seletivos para células tumorais, causando efeitos adversos que muitas vezes alteram a qualidade de vida do paciente drasticamente. Muitos fármacos antineoplásicos tiveram sua origem relacionada aos produtos naturais. A capsaicina é o principal componente pungente das pimentas vermelhas do gênero Capsicum, e seu efeito antitumoral é extensivamente discutido devido a sua capacidade de induzir apoptose seletivamente em diferentes linhagens de células cancerígenas. Este trabalho teve como objetivo utilizar a estratégia de modificação molecular para o planejamento racional de análogos funcionais da capsaicina, visando à obtenção de moléculas com atividade citotóxica superior. Os análogos foram sintetizados utilizando reações de uma única etapa baseadas em metodologias clássicas de acilação e caracterizados através de metodologias analíticas como espectroscopia de RMN de 1H e 13C, análise elementar e ponto de fusão. Posteriormente, foram avaliadas as atividades biológicas contra quatro linhagens tumorais (PC3, MACL-1, H1299, U138MG) e fibroblastos (3T3), utilizando o método de redução do MTT 3-(4,5-dimetil-tiazol-2-il)-2,5-difeniltetrazólio. Três compostos (RPF306, 452 e 404) inibiram seletivamente o crescimento celular na faixa de concentração de micromolar (µM). Estudos teóricos adicionais revelaram que propriedades topológicas e eletrônicas influenciaram na discriminação de amostras e podem ser importantes no processo de reconhecimento molecular e, subsequentemente, na resposta biológica. Tais resultados indicam que amidas e ésteres aromáticos, como o RPF306 e 404 podem ser modelos interessantes para o planejamento de novas séries de moléculas seletivas e pouco tóxicas, que representem uma alternativa interessante no tratamento do câncer.Over the past century, the number of cancer cases has increased significantly worldwide. Therefore, the quest for discovery of new molecules able to treat the disease is increasing, since many drugs used in therapy are poorly selective and toxic to normal cells, causing adverse effects that often change dramatically the patient\'s quality of life. Many chemotherapeutic agents had its origin related to natural products. Capsaicin is the main component of pungent red peppers of the genus Capsicum, and its antitumor effect is extensively discussed, due to its ability to selectively induce apoptosis in several cancer cell lines. In this context, our research aims to use the strategy of molecular modification to the rational design of capsaicin functional analogues, in order to obtain molecules with superior cytotoxic activity. The analogues were synthesized using an one-step reaction, based on classical acylation methods and characterized by analytical methods such as 1H and 13C NMR spectroscopy, elemental analysis and melting point. Subsequently, their cytotoxicity were evaluated against four human cancer cell lines (PC3, MACL-1, H1299 and U138MG) and fibroblast (3T3) using the MTT - 3-(4,5 dimethyl thiazole-2-yl)-2,5 diphenyltetrazolium assay. Three compounds (RPF306, 452 and 404) selectively inhibited the growth of cancer cell lines at micromolar (µM) range. In silico studies revealed that topological and electronic properties mostly influenced the samples discrimination and also might be important for the molecular recognition process and, subsequently, biological response or function. The results indicate that aryl amides and esters, such as RPF306 and 404 might be interesting scaffolds to develop a novel series of compounds with higher selective and low toxicity that could represent an alternative in the treatment of cancer.
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Zhang, Guangfan. "EFFECT OF CHRONIC AIRWAY INFLAMMATION INDUCED BY ALLERGEN SENSITIZATION ON VAGAL BRONCHOPULMONARY SENSORY NERVES IN RATS." UKnowledge, 2008. http://uknowledge.uky.edu/gradschool_diss/688.
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Airway hyperresponsivness (AHR) is one of most prominent pathophysiological features of asthma. Increasing evidence suggests that vagal bronchopulmonary afferents may be involved in the development of AHR. However, the underlying mechanisms are not clear. Therefore, the purpose of this dissertation was to investigate the effect of chronic airway inflammation induced by allergen sensitization on vagal bronchopulmonary afferents. The study was carried out in an animal model of allergic asthma. Brown-Norway rats were sensitized by intraperitoneal Ovalbumin (Ova) and exposed to aerosolized Ova 3 times/week for three weeks. Control rats received the vehicle. In vivo single-fiber recording technique was applied in this study. Our results showed that chronic Ova exposure caused an elevated baseline activity of pulmonary Cfibers, and a distinctly higher sensitivity of these afferents to chemical stimulants and lung inflation. After an acute Ova inhalation challenge, the increase in baseline activity and the excitability of pulmonary C-fibers were further augmented in sensitized rats, but not in control rats. In addition, sensitivity of pulmonary myelinated afferents to capsaicin was significantly elevated after chronic airway inflammation was induced by allergen. Furthermore, immunohistochemsitry data showed that, in nodose ganglia the proportion of transient receptor potential vanilloids type 1 channels (TRPV1)-expressing bronchopulmonary neurons was significantly higher in sensitized rats than in controls. This increase of TRPV1 expression was found mainly in neurofilament-positive neurons (myelinated neurons), but this effect was absent in jugular ganglia. In conclusion, allergen-induced airway inflammation caused a pronounced sensitizing effect on vagal pulmonary non-myelinated (C-fiber) afferents and elevated the sensitivity of vagal pulmonary myelinated afferents to capsaicin. The latter was accompanied by the upregulation of TRPV1 expression in these myelinated neurons.
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Huang, J. "Modulation of the heat- and capsaicin-gated channel TRPV1 : role of NGF and PKC beta." Thesis, University of Cambridge, 2006. http://ethos.bl.uk/OrderDetails.do?uin=uk.bl.ethos.604706.
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Nerve growth factor (NGF), one of the major inflammatory mediators released following tissue injury, causes thermal hyperalgesia by sensitisation of the heat- and capsaicin-gated ion channel, TRPV1. The molecular mechanisms by which NGF causes sensitisation of TRPV1 remain controversial. In this thesis, the functional effect of NGF on TRPV1 was investigated in HEK 293 cells and cultured mouse dorsal root ganglion (DRG) neurons using calcium imaging. The results support the hypothesis that sensitisation of TRPV1 by NGF is mediated by two pathways. The major pathway is activated by the Y760 site TrkA, which stimulates P13 kinase with Src kinase being involved at a subsequent stage. Src kinase phosphorylates TRPV1 at a single tyrosine residue, Y200, leading to trafficking and insertion of the channel into the surface membrane and thus enhancing the membrane ionic currents. The second and more minor pathway is the PLCγ / PKCε signalling pathway which causes phosphorylation TRPV1 at the S502 and S801 sites. The actions of different PKC isoforms in modulating TRPV1 are largely unknown. PKCβ was found to be located in the membrane of small DRG neurones from wild-type mice but in the cytoplasm of neurones from TRPV1 knockout mice, suggesting a physical interaction between PKCβ and TRPV1. Immunoprecipitation and in vitro GST pull down experiments confirmed that PKCβ binds predominantly to the N-terminal of TRPV1. The protein-protein interaction between PKCβ and TRPV1 suggests that PKCβ might play a specific role in modulation of TRPV1. These findings provide new insights into the molecular mechanisms underlying TRPV1 modulation by inflammatory mediators and PKC isoforms.
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Onuki, Koichiro. "Effect of capsiate, a non-pungent capsaicin analog, on energy metabolism and body fat accumulation." Kyoto University, 2002. http://hdl.handle.net/2433/149890.
Full textAbstract:
Kyoto University (京都大学)0048
新制・課程博士
博士(農学)
甲第9598号
農博第1226号
新制||農||840(附属図書館)
学位論文||H14||N3630(農学部図書室)
UT51-2002-G356
京都大学大学院農学研究科応用生物科学専攻
(主査)教授 伏木 亨, 教授 小川 正, 教授 大東 肇
学位規則第4条第1項該当
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Stravinskaitė, Kristina. "Kosulio reflekso jautrumo pokyčiai metus rūkyti sveikiems asmenims ir sergantiems lėtine obstrukcine plaučių liga." Doctoral thesis, Lithuanian Academic Libraries Network (LABT), 2008. http://vddb.library.lt/obj/LT-eLABa-0001:E.02~2008~D_20081003_091317-35863.
Full textAbstract:
Darbo tikslas
Ištirti kosulio reflekso jautrumo pokyčius metus rūkyti sveikiems asmenims ir sergantiems lėtine obstrukcine plaučių liga.
Darbo uždaviniai
1. Ištirti ir įvertinti rūkymo metimo poveikį sveikų asmenų kosulio reflekso jautrumui.
2. Ištirti ir įvertinti metusių ir vėl pradėjusių rūkyti sveikų asmenų kosulio reflekso jautrumą.
3. Ištirti ir palyginti sergančių lėtine obstrukcine plaučių liga rūkorių ir sergančių lėtine obstrukcine plaučių liga buvusių rūkorių kosulio reflekso jautrumą.
4. Palyginti sergančių lėtine obstrukcine plaučių liga rūkorių ir sergančių lėtine obstrukcine plaučių liga buvusių rūkorių bei sveikų rūkorių ir sveikų nerūkančiųjų kosulio reflekso jautrumą
5. Ištirti bronchoalveolinio lavažo skysčio ląstelių sudėtį ir uždegimo žymenų (interleukino-8, leukotrieno B4, leukotrieno E4) koncentraciją sergantiems lėtine obstrukcine plaučių liga rūkoriams, sergantiems lėtine obstrukcine plaučių liga buvusiems rūkoriams ir sveikiems rūkoriams.
6. Įvertinti galimas kosulio reflekso jautrumo sąsajas su uždegimo ląstelių kiekiu ir uždegimo žymenų (interleukino-8, leukotrieno B4, leukotrieno E4) koncentracija bronchoalveolinio lavažo skystyje sergantiems lėtine obstrukcine plaučių liga rūkoriams, sergantiems lėtine obstrukcine plaučių liga buvusiems rūkoriams ir sveikiems rūkoriams.
Šiame darbe pirmą kartą ištirtas rūkymo metimo poveikis sveikų asmenų kosulio reflekso jautrumui ir sveikų asmenų kosulio reflekso jautrumas jiems metus ir vėl... [toliau žr. visą tekstą]The aim of the study To evaluate changes of cough reflex sensitivity after smoking cessation in healthy subjects and patients with chronic obstructive pulmonary disease (COPD). Objectives of the study 1. To evaluate the effect of smoking cessation on cough reflex sensitivity changes in healthy subjects. 2. To investigate cough reflex sensitivity changes after cessation and resumption of smoking in healthy subjects. 3. To evaluate and compare cough reflex sensitivity in COPD smokers and COPD ex-smokers. 4. To compare cough reflex sensitivity in COPD smokers and COPD ex-smokers with the cough reflex sensitivity in healthy smokers and healthy never smokers. 5. To evaluate the inflammatory cells count and the concentration of inflammatory mediators (IL-8, LTB4, LTE4) in bronchoalveolar lavage (BAL) fluid from COPD smokers, COPD ex-smokers and healthy smokers. 6. To investigate probable association between cough reflex sensitivity and inflammatory cells count and concentration of inflammatory mediators (IL-8, LTB4, LTE4) in BAL fluid in COPD smokers, COPD ex-smokers and healthy smokers. This is the first study, where the effect of smoking cessation on cough reflex sensitivity in healthy subjects was evaluated and this is the first time, when cough reflex sensitivity in COPD smokers and COPD ex-smokers was evaluated and compared.
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Silva, Ana Rita Freitas da. "Utilização tópica da capsaicina veiculada em lipossomas para o tratamento da artrite reumatóide." Master's thesis, 2017. http://hdl.handle.net/10284/6645.
Full textAbstract:
Esta monografia visa realizar uma revisão bibliográfica sobre a possibilidade de utilização da capsaicina na artrite reumatóide. A AR é uma doença inflamatória crónica, que pode conduzir á destruição do tecido articular e periarticular, provocando dor e uma dificuldade na mobilização normal do utente. Embora sendo uma doença sem cura, nos últimos anos o tratamento tem sofrido uma melhoria substancial, tendo-se desenvolvido novos fármacos e novas formas terapêuticas para o seu tratamento.
Há muito tempo que se conhece o poder analgésico/ anestésico tópico da capsaicina, uma substância extraída das pimentas chilli, que se deve ao seu mecanismo de ação que estimula as fibras aferentes do tipo C e a libertação da substância P, inicialmente levando a sensação de queimadura e prurido, mas que em aplicações repetidas vai levar a uma redução da sensibilidade na zona devido à depleção da substância P e à degeneração das fibras nervosas periféricas.
Esta substância tem sido usada, portanto, em tratamento de dor neuropática, condições de osteoartrite e também artrite reumatóide; no entanto, os seus efeitos de ardor, queimação, e aumento de sensibilidade nas primeiras aplicações, fazem com que haja uma taxa grande de desistência do tratamento. Foi por esta razão que se estudou a possibilidade de incorporar esta substância em lipossomas, que funcionariam como transportador da mesma, aumentando a sua biodisponibilidade e a sua ação terapêutica, promovendo uma libertação controlada e diminuindo assim substancialmente os seus efeitos secundários. Estas vantagens, devem-se ao facto de os lipossomas serem estruturas microscópicas compostas por constituintes anfifilicos, e se assemelharem às membranas das células, interagindo intimamente e com maior eficiência com as células e tecidos do organismo. Desta forma, o uso da capsaicina tópica incorporada em lipossomas torna-se muito vantajoso nos casos de artrite reumatóide, diminuindo substancialmente a dor nas articulações, sem que o utente sofra com os efeitos provocados pela substância não encapsulada.This literature review aims to understand the possibility of the use of capsaicin on the treatment of RA. RA is a chronic inflammatory disease, which can lead to the destruction of articular and periarticular tissue, causing pain and difficulty in the normal mobilization of the patient. It is a disease without cure, but in the last years the treatment has undergone a substantial improvement, having new therapeutic strategies been developed. The analgesic / topical anesthetic power of capsaicin, a substance extracted from chilli peppers, has long been known, and its due to its mechanism of action, that stimulates afferent type C fibers and the release of substance P, initially leading to a burning sensation and itch, but which in repeated applications will lead to a reduction of sensitivity in the zone due to depletion of substance P and degeneration of peripheral nerve fibers. This substance has therefore been used in the treatment of neuropathic pain, conditions of osteoarthritis and also rheumatoid arthritis. However, the effects of burning, burning, and increased sensitivity in the first applications, cause a high dropout in treatment. For this reason, it was studied the possibility of incorporating this substance into liposomes, which would act as a transporter of capsaicin, increasing its bioavailability, its therapeutic action, promoting a controlled release and thus substantially reducing its side effects. These acquired advantages are due to the fact that liposomes are microscopic structures composed of amphiphilic constituents, that resemble the cell membranes, interacting intimately and more efficiently with the body's cells and tissues. Thus, the use of topical capsaicin incorporated into liposomes becomes advantageous in cases of rheumatoid arthritis, substantially decreasing joint pain, without the user suffering from the effects caused by the non encapsulated drugs.
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羅怡卿. "= Pharmacological actions and mechanisms of capsaicin derivatives on the activation of capsaicin-sensitive primary afferent neurons." Thesis, 1997. http://ndltd.ncl.edu.tw/handle/11879188674809412098.
Full text
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Lu, Cho-Ying, and 呂卓穎. "Capsaicin induces apoptosis and autophagy in B16F10 cells." Thesis, 2013. http://ndltd.ncl.edu.tw/handle/w6k82n.
Full textAbstract:
碩士國立中興大學
生命科學院碩士在職專班
101
Melanoma is a malignant tumor of melanocytes. If melanoma is found at early stage, it can be removed completely by surgery and the chance of cure is high. Unfortunately, if it is diagnosed late it may lead to skin cancer-relatred death. The treatments to melanoma these days include chemo- and immunotherapy, and radiation therapy. Capsaicin has an anti-proliferative effect in vitro on prostate, colon, gastric, hepatic and leukemic cancer cell lines. It is demonstrated that capsaicin inhibited melanoma cacncer cell lines, however, most of the mechanisms are still unclear. In this study, we used rat melanoma cell line, B16F10, for the evaluation of the anticancer effect of capsaicin . We found that the percentage of apoptosis and changes of mitochondrial membrane potential are notably increased in high concentration of capsaicin (400 μM). Western blot also shows that high concentration of capsaicin decreases Bcl-2 protein. Low concentrations of capsaicin are found to not to activate PARP (Poly ADP ribose polymerase) resulting in no apoptosis. While oxidative stress is not significantly different among different concentrations of capsaicin. We suggest that high concentration of capsaicin might induce apoptosis in B16F10 through mitochondrial dependent pathway. We also found that low concentrations of capsaicin (10, 100 μM) result in autophagy induction in B16F10 cells. Western blot also shows that high concentration of capsaicin increases the level of mTOR phosphorylation. On the other hand, low concentrations of capsaicin increase beclin-1 and autophagy. We suggest that capsaicin-mediated autophagy may involved in cell survival mechanism in B16F10 cells. Thus, we propose to utilize inhibitors of autophagy to examine the percentage of apoposis in B16F10. Similarly, inhibitors of apoptosis will be used to study the autophagy mechanism in B16F10 cells, with the hope to find out the relationship between autophagy and apoptosis in capsaicin-exposed B16F10 cells.
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Yang, Yu-Chiao, and 楊玉嬌. "Study on Capsaicin-Derived Vasodilatory β-Adrenoceptor Blocker." Thesis, 1999. http://ndltd.ncl.edu.tw/handle/96207610099653252154.
Full textAbstract:
博士高雄醫學院
醫學研究所
87
Capsinodilol (N - { 4 - [ 2-Hydroxy-3-(1-oxyethylamino-2-methoxy- benezene)propoxy]-3-methoxybenzyl}nonamide) is a newly synthesized capsaicin-derived α, β-adrenoceptor blocker designed to increase the vasodilatory activity of capsinolol which was reported to be a β-adrenergic blocker with a calcitonin gene related peptide (CGRP)-associated cardiogenic activity. In this study, theβ-adrenoceptor blocking properties and cardiovascular activities of capsinodilol were investigated under in vivo and in vitro conditions including the receptor binding experiments and the radioimmunoassay (RIA) of CGRP. Furthermore, the sensory cardiovascular activities of capsaicin and its derivatives, including nonivamide (NVA), nitrononivamide (NVANO), glyceryl nonivamide (GLNVA), sodium nonivamide acetate (SNA) and capsinolol, were studied under in vivo and in vitro conditions, including extracellular recording technique on the isolated vagus nerve. In addition, the proton role of capsaicin-associated sensory activities and the possible parasympathetic afferent, efferent and β-adrenoceptor binding activities of capsinolol in the cardiovascular system were also exploed in the present study. The sensory cardiovascular activities of capsaicin and its derivatives, such as NVA, NVANO, GLNVA and capsinolol, were studied under in vivo and in vitro. NVA, NVANO and capsinolol (2.0 mg/kg, i.v.), similar to capsaicin, elicited a triphasic blood pressure (effect A, B and C) and a biphasic bradycardia response (effect F and S) in the Wistar rats, while at lower dose, capsinolol (0.5 mg/kg, i.v.) and GLNVA (1.0 mg/kg, i.v.) didn''t reveal capsaicin-like cardiovascular changes. The nonphenolic derivatives such as GLNVA and capsinolol could produce the sensory activity in the isolated atrium to induce the positive inotropic and chronotropic activities. The potency of capsaicin derivatives on cardiogentic activity was capsaicin > NVA > GLNVA >> capsinolol > NVANO. In addition, the nonphenolic derivative GLNVA could produce more vasodilatory response than capsaicin and its derivatives. The potency of capsaicin derivatives on vasodilatory activity in aorta was GLNVA > capsaicin ≧ NVA > NVANO >> capsinolol. This study make a drawback of proton''s role in capsaicin associated sensory and neuronal activities. Nitrononivamide (([N-4-hydroxy, 5-nitro]-3-methoxybenzyl) nonanamide; NVANO; Fig. 5-1) was an analogue of NVA, chemically added with an electrophilic NO2 on its aromatic ring to modify the proton activity of capsaicin''s phenolic OH. The purpose to synthesize this compound was to investigate the role of proton on the capsaicin-associated sensory and neuronal activities in Wistar rat. In the present study, NVANO (5.0 mM) increased the intensity of intracellural fluorescence (F340/F380) of Fura-2-AM and revealed a calcium influx activity in the isolated dorsal root ganglion cells (DRGs). In the isolated vagus nerve, NVANO (5.0 mM-100.0 mM) induced membrane depolarization and sensory C-spike inhibition by extracellural recording technique. These sensory neuronal activities were all significantly inhibited by capsazepine (1.0 mM, 10.0 mM), a capsaicin receptor antagonist, on DRGs and vagus of rats. NVANO (0.25, 0.5, 1.0 mg/kg, i.v.) dose-dependently revealed triphasic blood pressure and biphasic bradycardia as capsaicin in vivo. The sensory cardiovascular activity of NVANO (1.0 mg/kg, i.v.) was significantly changed by capsazepine (100.0 mg/kg, i.v.), atropine (1.0 mg/kg, i.v.) and bilateral cervical vagotomy. In a retrograde epigastric intraarterial injection, NVANO (5.0 mg/kg) revealed a spinal reflex activity and changed the cardiovascular response into monophasic hypotension and a mild tachycardia. Since these sensory activities of NVANO being less than those of capsaicin, it was suggested that NVANO act as a partial agonist of capsaicin on spinal DRGs and vagus nerve. These results show an argument on the hypothesis that capsaicin act on a protonation site in the ligand recognition domain of vanilloic receptor. Chemical modification on NVA to increase the possible phenolic acidity of proton fails to increase the proton-dependent sensory stimulation in vagus nerve and spinal DRGs. It is concluded that proton is required in capsaicin-induced sensory and neuronal activities. In the present study, capsinodilol was synthesized to be a capsaicin-derived vasodilatoryβ-adrenoceptor competitive blocker. It revealed both α- and β-adrenoceptor competitive blocking activities in in vitro, in vivo and receptor binding assay. At the dose of 1.0 mg/kg (i.v.), capsinodilol antagonized the phenylephrine (10.0 μg/kg, i.v.) induced-hypertension in the reserpinized Wistar rat and the (-)isoproterenol-induced positive chronotropic response in the vagotomized Wistar rat. In addition, capsinodilol ( 0.1-10.0μM ) also attenuated boththe(-)isoproterenol-induced positive chronotropic and inotropic activities in rat atria and (-)isoproterenol-induced tracheal relaxant effects, in a concentration-dependent manner. On the isolated rat aorta, capsinodilol ( 0.1-10.0μM ) dose dependently attenuated the phenylephrine-induced vasoconstriction . The parallel shift to the right of the concentration - response curve of (-)isoproterenol and phenylephrine by capsinodilol on atria, trachea and aorta have suggested that capsinodilol was an α-,β -adrenoceptor competitive antagonist. Moreover, theα-,β-adrenoceptor binding characteristics of capsinodilol were evaluated by [3H]prazosin and [3H]CGP-12177 in the rat brain, ventricular and trachea membranes. Furthermore, capsinodilol revealed positive inotropic activity, tracheal relaxant and vasorelaxation which were associated with the intrinsic sensory-like activity (ISA) in rat atria, tracheal and aorta, respectively. An radioimmunoassay of released CGRP from rat isolated perfused heart indicated that capsinodilol (10.0μM and 100.0μM) increased the release of CGRP and thus produces positive cardiotonic effects. Capsinodilol (1.0 mg/kg, i.v.) induced a substain hypotention and bradycardia over one hour in Wistar rat. In the spontaneous hypertension rat (SHR), capsinodilol (25.0 and 100.0 mg/kg, oral.) elicited a long lasting hypotention and bradycardia over 24 hours. In order to further identify the sensory properties of capsaicin and its deriviative, the action potential of vagal sensory C-fiber was recorded by extracellular recording technique. In the extracellular recording of isolated rat vagus nerve, capsaicin and its derivatives, such as capsinodilol, capsinolol, NVA, NVANO, GLNVA and SNA, inhibited the sensory C-spike action potential and induced the membrane depolarization on the vagal sensory nerve. The polarization of these compounds was similar to the effect of KCl (10.0 - 45.0 mM). It was concluded that capsaicin derivatives revealed a capsaicin-like sensory activities in the rat vagal sensory C-fiber to induce the membrane depolarization and inhibited the C-spike action potential. The potency of these capsaicin derivatives in the vagal sensory activities was capsaicin ≧ NVA > GLNVA > caposinolol ≧capsinodilol > NVANO > SNA. In this study, the sensory activities of capsinolol, a capsaicin-derived β-adrenoceptor blocker, was investigated to explore the possible parasympathetic afferent, efferent and β-adrenoceptor binding activities in the cardiovascular system. Capsinolol (2.0 and 5.0 mg/kg, i.v.), similar to capsaicin, elicited a triphasic blood pressure and a biphasic bradycardia response in the Wistar rats. These cardiovascular activities were significantly changed after the treatment with capsazepine (1.0 mg/kg, i.v.), atropine (1.0 mg/kg, i.v.), capsaicin desensitization (50.0 mg/kg/day, for one week) and bilateral cervical vagotomy. Microinjection of capsinolol (80.0 fmol) into the nucleus tractus solitarii (NTS) produced the hypotensive and bradycardia responses. In the extracellular recording of isolated rat vagus nerve, capsinolol, in contrast to propranolol, significantly depolarized the nerve membrane and affected the amplitude of sensory C-spike. Moreover, capsinolol further displayed the β-adrenoceptor binding characteristics in the rat ventricular and lung membranes. It is concluded that capsinolol is a β- adrenoceptor blocker with vagal sensory C-fiber-evoked parasympathetic afferent and efferent neuron activation properties. This special merit has not been found in other conventional β- blockers. In conclusion, (i) proton is required in capsaicin induced sensory and neuronal activities; however, it is not essential; (ii) capsinolol is a β- blocker with vagal sensory C-fiber-evoked parasympathetic afferent and efferent neuron activation properties; (iii) a new capsaicin-derived vasodilatoryβ-adrenoceptor competitive blocker, capsinodilol , was synthesized successfully.