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Статті в журналах з теми "Acetylcholinesterase – analyse"
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Kamal, Mohammad A., M. Reale, and Abdulaziz A. Al-Jafari. "Multiple Approaches to Analyse the Data for Rat Brain Acetylcholinesterase Inhibition by Cyclophosphamide." Neurochemical Research 35, no. 10 (July 21, 2010): 1501–9. http://dx.doi.org/10.1007/s11064-010-0199-y.
Повний текст джерела
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Singh, Manju. "Studies on Effects of Chronic Exposure of Some Organophosphates to Catla catla (HaM.)." UTTAR PRADESH JOURNAL OF ZOOLOGY 44, no. 13 (July 13, 2023): 131–41. http://dx.doi.org/10.56557/upjoz/2023/v44i133552.
Повний текст джерелаАнотація:
The present study deals with the long-term toxic effects of the lowest sub-lethal concentration of dimethoate and malathion on a freshwater fish Catla catla. Toxicity is measured in terms of inhibition in acetylcholinesterase activity and fish behaviour. Technical grades of dimethoate (30 EC) and malathion (50 EC) were used for the present study. LC50 values for 96 hours were calculated for both pesticides. The lowest sublethal concentration (1/5 of LC50) of both pesticides was taken for chronic exposure. As organophosphates are potent inhibitors of acetylcholinesterase (AChE) activity, the AChE activity was estimated by the method of Metcalf (1957) in the brain and liver tissue of the test fishes to evaluate chronic toxicity. The fish were observed regularly to analyse the changes in behaviour. A significant increase in inhibition of acetylcholinesterase activity was observed. Experimental fishes exhibited a decreased rate of opercular movement, loss of balance, excessive mucous secretion, erratic swimming, and increased surfacing with increasing exposure time. Probable reasons for these alterations have been discussed in detail.
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Podolska, Magdalena, and Dorota Napierska. "Acetylcholinesterase activity in hosts (herring Clupea harengus) and parasites (Anisakis simplex larvae) from the southern Baltic." ICES Journal of Marine Science 63, no. 1 (January 1, 2006): 161–68. http://dx.doi.org/10.1016/j.icesjms.2005.08.001.
Повний текст джерелаАнотація:
Abstract This study compares the acetylcholinesterase (AChE) activity of herring Clupea harengus infected with Anisakis simplex larvae and non-infected individuals caught in coastal waters of the southern Baltic. Acetylcholinesterase activity was measured spectrophotometrically. Generalized linear models were applied to analyse the dependence of AChE activity on the area of sampling and the biological parameters of fish and their parasites. The AChE activity of herring was higher in samples from the western and central coasts (regarded as “clean” waters) than in fish caught in the semi-enclosed areas of the Gulf of Gdańsk and Vistula Lagoon (regarded as “polluted” sites). The opposite relationship was noted in the activity of AChE extracted from A. simplex larvae. In male hosts, the parasitic AChE activity was markedly higher than in the females in all examined areas.
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ROSENBAUM, ENRIQUE ARTURO, ANA MARÍA PECHEN DE D'ANGELO, ROSA MARÍA BERGOC, and ANDRÉS VENTURINO. "MODELLING ACETYLCHOLINESTERASE KINETICS: THE IDENTIFIABILITY PROBLEM IN PARAMETER ESTIMATION." Journal of Biological Systems 07, no. 01 (March 1999): 95–111. http://dx.doi.org/10.1142/s0218339099000097.
Повний текст джерелаАнотація:
Acetylcholinesterase (E.C. 3.1.1.7) is a typical hydrolase showing substrate inhibition. Classical works stated a two-step kinetics for the catalytic mechanism. We analyse here a full interacting model for the substrate bound to an inhibitory site different to the catalytic one, in agreement with current tridimensional data. A mixed model derived from equilibrium-steady state analysis fits fairly well to experimental data. We conclude that both catalytic steps are susceptible of partial inhibition, with 15% of remaining activity for substrate saturated enzyme. Indeed, substrate inhibition would be preferentially exerted on one of the catalytic steps, leading to particular cases which fit to data as well. The parametric identity among the mathematical expressions from restricted models disables identifiability of kinetic constants solely by fitting to data. Thus, additional information is required from other experimental approaches. Based on the cited closeness between both rate constants for the substrate acetylthiocholine, dissociation constants at the catalytic and inhibitory sites are estimated in ~ 63 μM and ~ 0.35 mM respectively, while interaction between binding sites might enhance the latter up to 16 mM. We also emphasise the relevance of considering substrate inhibition in kcat extrapolations even at low substrate concentrations. Finally, we are able to predict total acetylated enzyme values in the order of those done from direct experimental measurements.
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KOVARIK, Zrinka, Zoran RADIĆ, Harvey A. BERMAN, Vera SIMEON-RUDOLF, Elsa REINER, and Palmer TAYLOR. "Acetylcholinesterase active centre and gorge conformations analysed by combinatorial mutations and enantiomeric phosphonates." Biochemical Journal 373, no. 1 (July 1, 2003): 33–40. http://dx.doi.org/10.1042/bj20021862.
Повний текст джерелаАнотація:
A series of eight double and triple mutants of mouse acetylcholinesterase (AChE; EC 3.1.1.7), with substitutions corresponding to residues found largely within the butyrylcholinesterase (BChE; EC 3.1.1.8) active-centre gorge, was analysed to compare steady-state kinetic constants for substrate turnover and inhibition parameters for enantiomeric methylphosphonate esters. The mutations combined substitutions in the acyl pocket (Phe295→Leu and Phe297→Ile) with the choline-binding site (Tyr337→Ala and Phe338→Ala) and with a side chain (Glu202→ Gln) N-terminal to the active-site serine, Ser203. The mutations affected catalysis by increasing Km and decreasing kcat, but these constants were typically affected by an order of magnitude or less, a relatively small change compared with the catalytic potential of AChE. To analyse the constraints on stereoselective phosphonylation, the mutant enzymes were reacted with a congeneric series of SP- and RP-methylphosphonates of known absolute stereochemistry. Where possible, the overall reaction rates were deconstructed into the primary constants for formation of the reversible complex and intrinsic phosphonylation. The multiple mutations greatly reduced the reaction rates of the more reactive SP-methylphosphonates, whereas the rates of reaction with the RP-methylphosphonates were markedly enhanced. With the phosphonates of larger steric bulk, the enhancement of rates for the RP enantiomers, coupled with the reduction of the SP enantiomers, was sufficient to invert markedly the enantiomeric preference. The sequence of mutations to enlarge the size of the AChE active-centre gorge, resembling in part the more spacious gorge of BChE, did not show an ordered conversion into BChE reactivity as anticipated for a rigid template. Rather, the individual aromatic residues may mutually interact to confer a distinctive stereospecificity pattern towards organophosphates.
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Moreta, Marta Pérez-Gómez, Natalia Burgos-Alonso, María Torrecilla, José Marco-Contelles, and Cristina Bruzos-Cidón. "Efficacy of Acetylcholinesterase Inhibitors on Cognitive Function in Alzheimer’s Disease. Review of Reviews." Biomedicines 9, no. 11 (November 15, 2021): 1689. http://dx.doi.org/10.3390/biomedicines9111689.
Повний текст джерелаАнотація:
Alzheimer’s disease (AD) is the most common form of dementia over the age of 65. It is estimated that 115.4 million people will be affected by AD by 2050. Acetylcholinesterase inhibitors (AChEI) are the only available and approved treatment for AD. The aim of the present study was to analyse the evidence on the efficacy of the AChEI in the treatment of cognitive symptoms of Alzheimer’s disease. For that purpose, a review of review of the systematic reviews (SRs) on this topic was carried out by Web of Science, PubMed, and The Cochrane Library, among others, were searched until 24 September 2021. Thirteen of the 1773 articles evaluated the efficacy of AChEI on cognitive function and/or general condition and/or behavioural disturbances of patients with mild to moderate AD. Methodological quality and risk of bias were rated using the ROBIS scale. The quality of the identified studies was high for nine of them, unclear for two, and finally only in two of the 13 studies did we detect low quality. Overall, AChEI showed very low efficacy in improving cognition in patients with mild to moderate AD. Better results were obtained in improving global state, with donepezil being the most effective treatment. No improvements in behavioural disturbances were found. Few high-quality reviews provide clear evidence of the effects of AChEI on cognition, global change, behaviour, and mortality. The data suggest that AChEI stabilize or slow cognitive deterioration, improving global status. In addition, data indicate that the use of AChEI decreases mortality in patients with mild to moderate AD. However, there is no evidence that they improve patient behaviour. Donepezil is the best therapeutic alternative at a dose of 10 mg/day.
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Anju, T. R., and C. S. Paulose. "Striatal cholinergic functional alterations in hypoxic neonatal rats: Role of glucose, oxygen, and epinephrine resuscitation." Biochemistry and Cell Biology 91, no. 5 (October 2013): 350–56. http://dx.doi.org/10.1139/bcb-2012-0102.
Повний текст джерелаАнотація:
Molecular processes regulating cholinergic functions play an important role in the control of respiration under hypoxia. Cholinergic alterations and its further complications in respiration due to hypoxic insult in neonatal rats and the effect of glucose, oxygen, and epinephrine resuscitation was evaluated in the present study. Receptor binding and gene expression studies were done in the corpus striatum to analyse the changes in total muscarinic receptors, muscarinic M1, M2, M3 receptors, and the enzymes involved in acetylcholine metabolism, choline acetyltransferase and acetylcholinesterase. Neonatal hypoxia decreased total muscarinic receptors with reduced expression of muscarinic M1, M2, and M3 receptor genes. The reduction in acetylcholine metabolism is indicated by the downregulated choline acetyltransferase and upregulated acetyl cholinesterase expression. These cholinergic disturbances were reversed to near control in glucose-resuscitated hypoxic neonates. The adverse effects of immediate oxygenation and epinephrine administration are also reported. The present findings points to the cholinergic alterations due to neonatal hypoxic shock and suggests a proper resuscitation method to ameliorate these striatal changes.
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Suciati, Suciati, Erlinda Rhohmatul Laili, Hamizah Haula, Lidya Tumewu, Nitra Nuengchamnong, Nungruthai Suphrom, and Aty Widyawaruyanti. "Phytoconstituents, antioxidant, and cholinesterase inhibitory activities of the leaves and stem extracts of Artocarpus sericicarpus." Pharmacia 71 (February 19, 2024): 1–8. http://dx.doi.org/10.3897/pharmacia.71.e112499.
Повний текст джерелаАнотація:
The study aimed to investigate the antioxidant and cholinesterase inhibitory activities of the leaves and stems of Artocarpus sericicarpus and to analyse the phenolic compounds in the extracts. The modified Ellman’s method was used to determine the cholinesterase inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) enzymes. The antioxidant properties were evaluated using DPPH and ABTS methods. The total phenolic content (TPC) was measured by spectrometric assay, and compound identification was carried out by LC-MS/MS analysis. The results showed that the leaf and stem extracts of A. sericicarpus exerted significant inhibitory effects against AChE and BChE, as well as antioxidant activities. The stem ethanolic extract exhibited the highest potency against AChE and BChE with IC50 values of 5.81 and 11.46 µg/mL, respectively. The leaf and stem ethanolic extracts gave higher antioxidant activities and TPC compared to the water-based extracts. The LC-MS/MS analysis indicated the presence of phenolic compounds, such as flavones, flavonols, flavanones, prenylated chalcones, and xanthones in the extracts.
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Abd Rashed, Aswir, Ahmad Zuhairi Abd Rahman, and Devi Nair Gunasegavan Rathi. "Essential Oils as a Potential Neuroprotective Remedy for Age-Related Neurodegenerative Diseases: A Review." Molecules 26, no. 4 (February 19, 2021): 1107. http://dx.doi.org/10.3390/molecules26041107.
Повний текст джерелаАнотація:
Despite the improvements in life expectancy, neurodegenerative conditions have arguably become the most dreaded maladies of older people. The neuroprotective and anti-ageing potentials of essential oils (EOs) are widely evaluated around the globe. The objective of this review is to analyse the effectiveness of EOs as neuroprotective remedies among the four common age-related neurodegenerative diseases. The literature was extracted from three databases (PubMed, Web of Science and Google Scholar) between the years of 2010 to 2020 using the medical subject heading (MeSH) terms “essential oil”, crossed with “Alzheimer’s disease (AD)”, “Huntington’s disease (HD)”, “Parkinson’s disease (PD)” or “amyotrophic lateral sclerosis (ALS)”. Eighty three percent (83%) of the studies were focused on AD, while another 12% focused on PD. No classifiable study was recorded on HD or ALS. EO from Salvia officinalis has been recorded as one of the most effective acetylcholinesterase and butyrylcholinesterase inhibitors. However, only Cinnamomum sp. has been assessed for its effectiveness in both AD and PD. Our review provided useful evidence on EOs as potential neuroprotective remedies for age-related neurodegenerative diseases.
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Pham, Van Dung, Tuan Anh To, Cynthia Gagné-Thivierge, Manon Couture, Patrick Lagüe, Deqiang Yao, Marie-Ève Picard, et al. "Structural insights into the putative bacterial acetylcholinesterase ChoE and its substrate inhibition mechanism." Journal of Biological Chemistry 295, no. 26 (May 5, 2020): 8708–24. http://dx.doi.org/10.1074/jbc.ra119.011809.
Повний текст джерелаАнотація:
Mammalian acetylcholinesterase (AChE) is well-studied, being important in both cholinergic brain synapses and the peripheral nervous systems and also a key drug target for many diseases. In contrast, little is known about the structures and molecular mechanism of prokaryotic acetylcholinesterases. We report here the structural and biochemical characterization of ChoE, a putative bacterial acetylcholinesterase from Pseudomonas aeruginosa. Analysis of WT and mutant strains indicated that ChoE is indispensable for P. aeruginosa growth with acetylcholine as the sole carbon and nitrogen source. The crystal structure of ChoE at 1.35 Å resolution revealed that this enzyme adopts a typical fold of the SGNH hydrolase family. Although ChoE and eukaryotic AChEs catalyze the same reaction, their overall structures bear no similarities constituting an interesting example of convergent evolution. Among Ser-38, Asp-285, and His-288 of the catalytic triad residues, only Asp-285 was not essential for ChoE activity. Combined with kinetic analyses of WT and mutant proteins, multiple crystal structures of ChoE complexed with substrates, products, or reaction intermediate revealed the structural determinants for substrate recognition, snapshots of the various catalytic steps, and the molecular basis of substrate inhibition at high substrate concentrations. Our results indicate that substrate inhibition in ChoE is due to acetate release being blocked by the binding of a substrate molecule in a nonproductive mode. Because of the distinct overall folds and significant differences of the active site between ChoE and eukaryotic AChEs, these structures will serve as a prototype for other prokaryotic acetylcholinesterases.
Дисертації з теми "Acetylcholinesterase – analyse"
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El, Tahchy Anna. "Etude de la voie de biosynthèse de la galanthamine chez Leucojum aestivum L. : criblage phytochimique de quelques amaryllidaceae." Thesis, Nancy 1, 2010. http://www.theses.fr/2010NAN10072/document.
Повний текст джерелаАнотація:
La galanthamine est un alcaloïde isoquinoléique, utilisé dans le monde entier pour le traitement palliatif de la maladie d’Alzheimer en raison de son pouvoir inhibiteur de l’acétylcholinestérase. Cet alcaloïde est extrait à partir de bulbes d’Amaryllidaceae, Leucojum aestivum, Galanthus nivalis, et Narcissus sp. ou obtenu par synthèse chimique. La difficulté principale de cette dernière réside dans le respect de la configuration des centres d'asymétrie. La culture de tissus in vitro pourrait constituer une alternative intéressante pour obtenir ce composé à haute valeur ajoutée. Le premier objectif de ce projet, vise à améliorer l’accumulation de cet alcaloïde par les biais des biotechnologies. Le second objectif est de rechercher par criblage phytochimique (HPLC, LCMS, GCMS, et HPTLC-MS) de bulbes in vitro et in vivo d’Amaryllidaceae, de nouveaux alcaloïdes biologiquement actifs. Le troisième objectif porte sur l’étude de la voie de biosynthèse en vue de réaliser une synthèse biomimétique de la galanthamine. Nous avons établi des cultures in vitro de 3 espèces d’Amaryllidaceae. La variation des paramètres exogènes a conduit à une accumulation accrue d’alcaloïdes (0,02 à 0,2 % MS). Le criblage phytochimique a conduit à l’identification d’alcaloïdes nouveaux issus des cultures in vitro, n’existant pas in vivo, et présentant un puissant pouvoir inhibiteur de l’acétylcholinestérase (40 à 80 % Inh). L’ajout, de la 4’-Ométhyl-d3-norbelladine aux cultures in vitro a conduit à sa métabolisation en trois types d’alcaloïdes deutérés. Une stimulation de la synthèse et du relargage de la galanthamine native (0,15 % MS et 0,16 % Milieu) a été observée en présence du précurseur deutéréGalanthamine is an Amaryllidaceae alkaloid used worldwide for the symptomatic treatment of Alzheimer’s disease because of his capacity to inhibit the acetylcholinesterase enzyme. There are two galanthamine sources for medical applications. One is the total synthesis, a complicated process because galanthamine has three asymmetric carbons, requiring stereochemically controlled synthesis. Galanthamine is also extracted from bulbs of some Amaryllidaceae such as Leucojum aestivum, Galanthus nivalis, and Narcissus sp.. The first aim of this work is to improve the accumulation of this alkaloid using biotechnologies. The second aim consists on the phytochemical screening (HPLC, LCMS, GCMS, et HPTLCMS) of in vivo and in vitro Amaryllidaceae bulbs, in order to identify new alkaloids with important pharmacological activities. Finally, the third aim concerns the study of the biosynthesis pathway in order to establish a biomimetic synthesis of galanthamine. Therefore, we established in vitro cultures of three Amaryllidaceae species. The variation of exogenousparameters led to the obtainment of high galanthamine accumulation (0.02 to 0.2 % DW). The phytochemical screening showed new alkaloids in extracts of in vitro cultures, which did not exist in in vivo extracts, and possessing high acetylcholinesterase activity (40 to 80 % Inh). The 4’-O-methyl-d3-norbelladine is incorporated into three different groups ofAmaryllidaceae alkaloids. The addition of the labelled precursor to shoot cultures stimulated the synthesis of native galanthamine (0.15 % DW and 0.16 % Culture medium)
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Stepurska, Kateryna. "Développement d'une procédure originale pour la multi-détection de composés toxiques utilisant des biocapteurs à base d'acétylcholinestérase." Thesis, Lyon, 2016. http://www.theses.fr/2016LYSE1067/document.
Повний текст джерелаАнотація:
Les travaux présentés dans ce manuscrit concernent le développement d‘une approche originale permettant la détermination de plusieurs composés (principalement aflatoxines et pesticides organophosphorés), à l‘aide de biocapteurs électrochimiques basés sur l‘inhibition de l‘acétylcholinestérase. Dans un premier temps, un nouveau biocapteur potentiométrique utilisant des transistors à effet de champ sensibles au pH (pH-FETs) comme transducteurs a été développé pour la détermination de l‘aflatoxine B1 (AFB1) et différent paramètres d‘élaboration et de fonctionnement du biocapteur ont été optimisés. Le biocapteur proposé est caractérisé par une stabilité opérationnelle élevée and bonne reproductibilité du signal en cours d‘utilisation et de stockage. Le biocapteur a ensuite été évalué pour l‘analyse d‘échantillons réels (blé, sésame, noix et pois) et une simulation mathématique de la réponse du biocapteur potentiométrique à l‘AFB1 a été proposée pour la première fois et validée. Dans un deuxième temps, un biocapteur conductimétrique utilisant des microélectrodes interdigitées en or a été développé. La sensibilité de ce biocapteur aux aflatoxines ainsi qu‘à d‘autres classes de substances toxiques, tels que les pesticides organophosphorés, les métaux lourds, les glycoalkaloïdes, et les surfactants, a été déterminée. Une nouvelle procédure originale, permettant la détermination sélective de toxines multiclasses par application successive de solutions de réactivation visant spécifiquement des inhibiteurs irréversibles ou réversibles, a été finalement proposée. En utilisant cette méthode, il a été montré que les biocapteurs enzymatiques pouvaient être appliqués à l‘analyse des aflatoxines et des pesticides organophosphorés, ainsi qu‘à la détermination de la toxicité globale des échantillonsInvestigations reported in this manuscript are focused on the development of an original approach for the detection of several toxic compounds, mainly aflatoxins and organophosphorus pesticides, using acetylcholinesterase (AChE)-based inhibitory electrochemical biosensors. In a first step, a new potentiometric biosensor using pH Sensitive Field-Effect Transistors (pH-FETs) as transducers was investigated for aflatoxin B1 (AFB1) determination and different elaboration and working parameters were optimized. The proposed biosensor was characterized by high operational stability and reproducibility of the signal during the work as well as during the storage. The biosensor was further evaluated for real samples analysis (wheat, sesame, walnuts and peas) and a mathematical simulation of the potentiometric biosensor response to aflatoxin B1 was proposed for the first time and validated. In a second step, a conductometric biosensor using interdigitated gold microelectrodes was developed. The sensitivity of the biosensor to aflatoxins and other classes of toxic substances, such as organophosphorus pesticides, heavy metals ions, glycoalkaloids, and surfactants, was determined. A new and original procedure, enabling the selective determination of multiclass toxins by applying successive reactivation solutions targeting either irreversible or reversible inhibitors, was finally proposed. Using this method, the electrochemical enzyme inhibitory biosensors could be applied to the analysis of aflatoxins and organophosphorus pesticides, as well as for the determination of total toxicity of the samples
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Szmicseková, Kristína. "Non-neuronal cholinergic system." Electronic Thesis or Diss., Université Paris Cité, 2021. http://www.theses.fr/2021UNIP5223.
Повний текст джерелаАнотація:
Introduction: Malgré l'absence d'innervation cholinergique, les vaisseaux sont très réactifs à la présence d'acétylcholine (ACh). De plus, ce neurotransmetteur est couramment utilisé pour évaluer la fonction endothéliale des vaisseaux. Cependant, les informations sur les cholinestérases vasculaires (ChE), les enzymes qui mettent fin à l'action de l'ACh, sont rares. Le principal objectif de cette thèse de doctorat était de caractériser les ChE vasculaires et l'ensemble du système cholinergique de l'aorte dans des conditions normales et pathologiques. Méthodes: Des rats Wistar mâles adultes et des rats spontanément hypertendus (SHR) nourris avec une alimentation régulière ou riche en graisses ont été utilisés dans le cadre du projet. L'expression relative des enzymes et des transporteurs étudiés a été déterminée par la méthode RT-qPCR. Les activités de ChE dans les extraits de tissus ont été mesurées par la méthode d'Ellman, la coloration de l'activité a été réalisée par la méthode de Tsuji et la localisation des protéines a été faite par double immunohistochimie. Les formes moléculaires de ChE ont été séparées par des gradients de saccharose. Résultats et conclusion: Toutes les enzymes et tous les transporteurs impliqués dans la synthèse, le stockage, la libération et la dégradation de l’ACh ont été détectés dans l'aorte du rat au niveau de l'ARNm et au niveau des protéines. Cela confirme que l'aorte est un tissu cholinergique non neuronal, capable de soutenir pleinement le cycle de vie des ACh. Les ChE sont présents principalement sous forme de formes ancrées dans la PRiMA dans chaque partie de l'aorte, tandis que la butyrylcholinestérase (BChE) est l’enzyme dominante, localisée principalement sur le muscle lisse. Dans les rat SHR, des niveaux plus faibles de BChE ont été détectés, accompagnés d'une diminution des expressions relatives de la carnitine acétyltransférase et des transporteurs de cations organiques. Cela suggère une signalisation cholinergique plus faible dans l'aorte de la SHR par rapport aux rats normotendus. Dans l'expérience pharmacologique, l'inhibition du BChE et l'alimentation riche en graisses ont toutes deux entraîné une prise de poids significative et une augmentation des taux sériques de TAG. De plus, un régime riche en graisses a induit une augmentation des niveaux d'ARNm du BChE, indiquant son implication dans le métabolisme des lipidesIntroduction: Despite the lack of cholinergic innervation, vessels are highly reactive to the presence of acetylcholine (ACh). Moreover, this neurotransmitter is commonly used to assess the endothelial function of vessels. However, information about vascular cholinesterases (ChE), the enzymes that terminate ACh action, is spares. The main aim of this dissertation thesis was to characterize vascular ChE and overall non-neuronal cholinergic system in the aorta under physiological and pathological conditions. Methods: Adult male Wistar rats and spontaneously hypertensive rats (SHR) were used in the project, fed either with regular or high-fat diet. Relative expression of studied enzymes and transporters were determined by RT-qPCR method. ChE activities in tissue extracts were measured by Ellman's assay, activity staining was performed by Tsuji’s method and proteins localizations were done by dual immunohistochemistry. Molecular forms of ChE were studied by sucrose gradients. Results and conclusion: The enzymes and transporters necessary for ACh synthesis, storage, release, and degradation were detected in the rat aorta at mRNA and at protein levels. This confirms that aorta is a non-neuronal cholinergic tissue, capable to fully support the ACh life cycle. ChE are present mainly as PRiMA-anchored forms in each part of the aorta, while butyrylcholinesterase (BChE) is the dominant ChE, localized primarily in the smooth muscle. In SHR, lower levels of BChE were detected, accompanied by decreased relative expressions of carnitine acetyltransferase and organic cation transporters. This suggests lower cholinergic signaling in SHR aorta as compared to normotensive rats. In the pharmacological experiment, both inhibition of BChE and high-fat diet resulted in significant weight gain and increased serum TAG levels. Moreover, a high-fat diet induced mRNA expression of BChE. Our data suggest BChE involvement in lipid metabolism
Úvod: Napriek absencii cholínergickej inervácie, cievy sú vysoko reaktívne na prítomnosť acetylcholínu (ACh). Okrem toho, práve tento neurotransmiter sa využíva vo fyziologických experimentoch na sledovanie funkčnosti endotelu. Napriek tomu však chýbajú informácie o prítomnosti cholínesteráz (ChE), enzýmov, ktoré ukončujú jeho účinok v cievach. Cieľom tejto dizertačnej práce bola detailne charakterizovať tieto enzýmy a kompletne preštudovať prítomnosť komponentov neneuronálneho cholínergického systému v aorte normotenzných a spontánne hypertenzných potkanov (SHR). Metódy: V experimentoch boli použité 12-týždňové potkany rodu Wistar a SHR, ktoré boli kŕmené buď štandardnou alebo vysoko-tukovou stravou. Relatívna expresia študovaných enzýmov a transportérov bola stanovená metódou RT-qPCR. Aktivity ChE boli stanovené v tkanivových extraktoch pomocou Ellmanovej metódy, aktivitné farbenie bolo prevedené podľa Tsujiho metódy. Na vizualizáciu a lokalizáciu bola využitá metóda dvojfarebnej immunohistochémie. Molekulové formy ChE boli charakterizované pomocou metódy sacharózového gradientu. Výsledky a diskusia: Všetky enzýmy a transportéry, ktoré sú potrebné na syntézu, uchovávanie, vylučovanie a degradáciu ACh boli potvrdené nielen na úrovni mRNA, ale aj na úrovni proteínov. Tieto zistenia potvrdzujú, že aorta patrí medzi neneuronálne cholínergické tkanivá. ChE sú prítomné primárne v PRiMA-kotvenej forme v každej časti aorty, pričom butyrylcholínesteráza (BChE) je dominantná a je prítomná hlavne v hladkom svalstve. V spontánne hypertenznom modeli bola detegovaná nižšia BChE aktivita a tiež nižšia relatívna expresia karnitínacetyltransferázy a organických katiónových transportérov. Vo farmakologickom experimente, aj inhibícia BChE, aj vysoko-tuková strava spôsobila signifikantný prírastok hmotnosti a zvýšenie sérových hladín triacylglycerolov. Okrem toho, vysoko-tuková strava indukovala zvýšenie hladín mRNA pre BChE, čo naznačuje dôležitú úlohu tohto enzýmu nielen vo fyziológii ciev, ale aj v metabolizme lipidov
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AMBU, GABRIELE. "Ethnobotanical and ethnopharmacological studies of medicinal plants used in rural areas of Kavrepalanchok District (Central Nepal)." Doctoral thesis, Università degli studi di Genova, 2021. http://hdl.handle.net/11567/1047246.
Повний текст джерелаАнотація:
The current economic and social conditions in many rural areas of the world are threatening the
precious heritage of ethnobotanical knowledge and traditional farming practices.This can cause loss
of precious cultural heritage and reduction in plant biodiversity, as ancient crops tend to disappear.
The main aim of this thesis is to document traditional uses of plants by different ethnic groups
(Tibeto-Burman and Indo-Aryan) living in certain rural areas of the Kavrepalanchok District in
Central Nepal. In the study area, due to distance from urban centres and difficulty in accessing the
government healthcare system, people still rely heavily on the use of local plants for various
purposes, above all for primary healthcare.
Through interviews with 32 informants, most of whom were key informants, we explored uses of
116 plant species, of which 101 were plants with medicinal value employed in the treatment of
human and veterinary diseases. Some unusual uses of medicinal plants and original recipes were
also reported.
The data document the richness of the local flora and traditional knowledge of medicinal plant
species used by ethnic communities in these rural areas.
Therefore, future projects will have to involve local people in the improvement and conservation of
the biological and cultural heritage.There is also a need for an ecological strategy for integrated
management of land, water and living resources.
Another aim of the research presented in this thesis is to better characterise some plants found to be
of particular interest among those surveyed in the study area. With this in mind, we have focused
our attention on those plants used by informants in the treatment of nervous system disorders, such
as two species belonging to Caprifoliaceae (formerly Valerianaceae): Valeriana jatamansi Jones ex
Rob. and Nardostachys jatamansi (D. Don) DC. These plants are widely used in traditional
medicine for their sedative and anxiolytic properties in Nepal and in many other Asian countries.
The pharmacognostic and phytochemical profile and the biological effects of essential oils (EOs) of
these species were compared with those of Valeriana officinalis L., a species whose
phytotherapeutic use is widespread in Western medicine.
The multidisciplinary approach used represents a way to avoid adulteration of herbal drugs and
allows evaluation of the effectiveness of EOs that could be used for a wide range of therapeutic
applications. Overall, the results of this research could be useful for enhancing knowledge of the potential of still
little-known medicinal plants for the possible formulation of new pharmaceutical products,
eventually contributing to the economic development of local communities.
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Fernandes, Tanize Stuker. "Analise fitoquímica de duas espécies de rutaceae: Helietta apiculata benth e zanthoxylum fagara (l.) Sarg." Universidade Federal de Santa Maria, 2016. http://repositorio.ufsm.br/handle/1/4280.
Повний текст джерелаАнотація:
Conselho Nacional de Desenvolvimento Científico e TecnológicoThe phytochemical investigation of methanol crude extract of the stem bark of the species Helietta apiculata Benth and Zanthoxylum fagara (L.) Sarg., Rutaceae, provided the isolation of thirty-one compounds. The species H. apiculata were isolated eight furoquinolínicos alkaloids (8, 9, 10, 11, 12, 13, 15 and 24) and one quinolinone (22), six coumarins (51, 52, 53, 58, 115 and 116), 116 first identified in the literature, three cinnamates (121, 122 and 123), two lignans (98 and 123), a limonoid (92), a long-chain acid (126), a steroid (80) and a mixture terpenes (T39). Two benzophenantridine alkaloids (33 and 34), five amides (69, 70, 117, 118 and 119), and a lignan (124) have been identified in species Z. fagara, along with the steroid 80. The cinnamate 120, 123 and the lignan 119 were first identified as a natural product. The cinnamate 122 and coumarin 115 are first described in H. apiculata species, while the amide 115 is first described in the genus Zanthoxylum, and 119 for the first time in the species Z. fagara. Lignans 98, 123 and 124 are identified in the Rutaceae family first time. The limonoid 92 was subjected to structural modifications through aminolysis reactions with various amines, providing fifteen derivatives, which when subjected to evaluation of the antimicrobial potential demonstrated greater power to inhibition of microorganisms that limonoid. Other derivatives obtained during this study was the acetylation and oxidation products of tembamida (69) amide and methylating the flindersiamina (15) alkaloid. Extracts, fractions and products were subjected to analysis of antimicrobial potential and inhibition of AChE enzyme. The alkaloids showed inhibition potential only for gram-positive bacteria, whereas coumarins were compounds which had the largest range of antimicrobial activities front fungi, Gram-negative and Gram-positive. Inhibition of acetylcholinesterase enzyme was significant only for fractions: ether basic H. apiculata, basic butanol, final aqueous and aqueous extract from the leaves Z. fagara with inhibition values ranging from 58,24% to 74,34% while for isolates the results were not significant.
A investigação fitoquímica do extrato bruto metanólico das cascas do caule das espécies Helietta apiculata Benth e Zanthoxylum fagara (L.) Sarg., Rutaceae, levaram ao isolamento de trinta e um compostos. Da espécie H. apiculata foram identificados oito alcaloides furoquinolínicos (8, 9, 10, 11, 12, 13, 15 e 24), um quinolinona (22), seis cumarinas (51, 52, 53, 58, 115 e 116) sendo a 116 identificada pela primeira vez na literatura, três cinamatos (121, 122 e 123), duas lignanas (98 e 123), um limonoide (92), um ácido de cadeia longa (126), um esteroide (80) e uma mistura de terpenos (T39). Dois alcaloides benzofenantridínicos (33 e 34), cinco amidas (69, 70, 117, 118 e 119) e uma lignana (124) foram identificados na espécie Z. fagara, juntamente com o esteroide 80. O cinamato 120, a lignana 123 e a amida 119 foram identificados pela primeira vez como produto natural. O cinamato 122 e a cumarina 115 são descritos pela primeira vez na espécie H. apiculata, enquanto a amida 115 é descrita pela primeira vez no gênero Zanthoxylum, e 119 pela primeira vez na espécie Z. fagara. As lignanas 98, 123 e 124 são identificadas na família Rutaceae pela primeira vez. O limonoide 92 foi submetido a modificações estruturais através de reações de aminólise com diferentes aminas, proporcionando quinze derivados, que quando submetidos à avaliação do potencial antimicrobiano demonstraram maior poder de inibição dos microrganismos que o limonoide. Outros derivados obtidos durante este trabalho foram os produtos da acetilação e a oxidação da amida tembamida (69), e a metilação do alcaloide flindersiamina (15). Os extratos, frações e produtos obtidos foram submetidos a analise do potencial antimicrobiano e de inibição da enzima AChE. Os alcaloides apresentaram potencial de inibição apenas para bactérias gram-positivas, enquanto as cumarinas foram os compostos que apresentaram o maior leque de atividades antimicrobianas frente a fungos, bactérias gram-negativas e gram-positivas. A inibição da enzima Acetilcolinesterase foi relevante apenas para as frações: etérea básica de H. apiculata, butanólica básica, aquoso final e extrato aquoso a partir das folhas de Z. fagara com valores de inibição entre 58,24% a 74,34% enquanto para os produtos isolados os resultados não foram significativos.
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Mazzanti, Cinthia Melazzo de Andrade. "Efeito do interferon beta, da ciclosporina A, do ebselen e da vitamina E no sistema colinérgico e purinérgico de ratos normais e submetidos à desmielinização pelo brometo de etídio." reponame:Biblioteca Digital de Teses e Dissertações da UFRGS, 2007. http://hdl.handle.net/10183/11127.
Повний текст джерелаАнотація:
A esclerose múltipla é a principal doença desmielinizante do sistema nervoso central (SNC). É considerada a principal causa de incapacidade neurológica em adultos jovens. O comprometimento cognitivo é muito comum nessa doença, envolvendo o aprendizado, a memória e a organização cortical do movimento, funções vitais que são reguladas pelo sistema colinérgico. O modelo de desmielinização tóxica induzida pelo brometo de etídio (BE) foi utilizado neste estudo, para avaliar a atividade da enzima acetilcolinesterase (AChE) no estriado (ST), hipocampo (HP), córtex cerebral (CC), hipotálamo (HY) e ponte (PN) associado ao tratamento com interferon beta (IFN-b), ciclosporina A (CsA), vitamina E (vit E) e ebselen (Ebs). Além disso, também foi investigado o efeito in vitro do BE na atividade da AChE, juntamente com os parâmetros cinéticos dessa enzima no ST, HP, CC e CB de ratos adultos. Os resultados demonstraram que o BE inibiu significativamente a atividade da AChE no ST, HP, CC e CB nas concentrações de 0,00625, 0,0125, 0,025, 0,05 e 0,1mM e a análise dos dados cinéticos mostraram uma inibição do tipo incompetitiva no ST, HP e CC, enquanto no CB a inibição foi do tipo mista. No estudo in vivo, foi observado uma inibição na atividade da AChE no CC, ST, HP, HY, PN e CB nos diferentes períodos avaliados pós-injeção do BE (3, 7, 15, 21 e 30 dias). Quando ratos desmielinizados com BE foram tratados com IFN-b e CsA, não houve alteração na atividade dessa enzima. Por outro lado, o tratamento com Vit E e Ebs foram capazes de aumentar a atividade da AChE no ST, CC e HP. Estudos imuno-histoquímicos demonstraram que nos ratos tratados com Vit E e Ebs as lesões induzidas pelo BE foram menores, sugerindo que estes compostos interferem no desenvolvimento de lesões desmielinizantes. Foi também avaliado o efeito per se do IFN-b, da CsA, da Vit E e do Ebs na atividade da AChE, os quais demonstraram um efeito inibitório sobre a atividade dessa enzima. Em plaquetas de ratos desmielinizados, foi observado uma diminuição na atividade da NTPDase e o tratamento com a Vit E e o Ebs modularam a hidrólise dos nucleotídeos de adenina. O presente trabalho demonstrou que o BE é um potente inibidor da atividade da AChE in vitro e os resultados in vivo demonstraram que a atividade dessa enzima está alterada após um evento de desmielinização tóxica no SNC. Os resultados deste estudo ajudaram a confirmar que drogas utilizadas no tratamento de pacientes com esclerose múltipla tais como o IFN-b e a CsA causam efeitos na atividade da AChE. A Vit E e o Ebs, além de demonstrarem uma interação com a neurotransmissão colinérgica, também modularam a hidrólise dos nucleotídeos de adenina em plaquetas de ratos, contribuindo no controle da coagulação plaquetária em processos desmielinizantes. Neste contexto, sugere-se que o IFN-b, a CsA, a vitamina E e o ebselen podem ser investigados em estudos futuros com a intenção de encontrar uma melhor terapia para beneficiar pacientes com patologias desmielinizantes.Multiple sclerosis is the main demyelinating disease of the central nervous system (CNS). It is the most common cause of neurological disability among young adults. The cognitive impairment is very commum in this illness, involving learning, memory and cortical organization of the movement, vital functions regulated by the cholinergic system. The model of toxic demyelination induced by ethidium bromide (EB) was used to evaluate brain acetylcholinesterase (AChE) activity in the striatum (ST), hippocampus (HP), cerebral cortex (CC), cerebellum (CB), hypothalamus (HY) and pons (PN), associated with treatment with interferon beta (IFN-b), ciclosporine A (CsA), vitamin E (Vit E) and ebselen (Ebs). In addition, the per se effect of EB on AChE activity was studied in vitro together with the kinetic parameters of this enzyme in the ST, HP, CC and CB of adult rats. The results showed that EB in vitro significantly inhibited AChE activity in the ST, HP, CC and CB at concentrations of 0.00625, 0.0125, 0.025, 0.05 and 0.1mM. The kinetic analysis demonstrated an uncompetitive inhibition in the ST, HP and CC, whereas in the CB the inhibition type was mixed. In relation to the in vivo results, AChE activity was inhibited after demyelination by EB in the CC, ST, HP, HY, PN and CB at the post-injection points of time evaluated (3-7-15-21 and 30 days). When demyelinated rats were submitted to the treatment with IFN-b and CsA, the results demonstrated that these compounds did not alter AChE activity. However, Vit E and Ebs were able to increase AChE activity in the ST, CC and HP. In addition, immunohistochemistry studies demonstrated that in Vit E and Ebs treated rats, the lesions induced by EB were smaller suggesting that these compounds somehow interfered in the development of the lesions. The per se effect of IFN-b, CsA, Vit E and Ebs were also evaluated, demonstrating that these compounds have an inhibitory effect on AChE activity. Platelets of the demyelinated rats demonstrated a reduction in NTPDase activity and the treatments with Ebs and Vit E modulated adenine nucleotide hydrolysis. The present investigation demonstrated that EB is a strong inhibitor of AChE activity in vitro and the results in vivo showed that the activity of this enzyme is altered after an event of toxic demyelination in the CNS. The results this study help the confirm that drugs used in the treatment of the patients with multiple sclerosis such as IFN-b and CsA cause effects in the AChE activity. The Vit E and Ebs besides of interaction with the cholinergic neurotransmission also modulated adenine nucleotide hydrolysis in platelets of the rats, contributing to the control of the platelet coagulant status in the demyelinating process. In this context, we can suggest that IFN-b, CsA, Vit E and Ebs may be investigated in future studies with the intention of finding a better therapy for to improve patients with demyelinating pathologies.
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Omena, Cristhiane Maria Bazílio de. "Atividade antioxidante e anticolinesterase dos extratos etanólicos dos frutos: Siriguela Spondia purpurea Linnaeus; Umbu Spondia tuberosa Arruda; Genipapo Genipa americana Linnaeus e Mangaba Hancornia speciosa Gomes." Universidade Federal de Alagoas, 2012. http://www.repositorio.ufal.br/handle/riufal/2031.
Повний текст джерелаАнотація:
Ethanol extracts of “jenipapo” (Genipa americana Linnaeus), “umbu" (Spondia tuberosa Arruda), “siriguela” (Spondia purpurea Linnaeus) and “mangaba” (Hancornia speciosa Gomes) were prepared from separate pulp, seeds and peel; except mangaba which are used pulp and peel. The investigation of antioxidant capacity of the ethanol extracts were carried out by the methods of determining the
content of ascorbic acid and total phenolics; scavenging 2, 2 -diphenyl-1-picrilhydrazyl and 2, 2’- azinobis (3-ethylbenzothiazoline-6-sulfonic acid) radical, antioxidant capacity of reduction of iron and copper and lipid peroxidation using a biomimetic membrane system, and measurement enzymatic of catalase and superoxide dismutase. It was also analyzed the acetylcholinesterase inhibitory activity, cytotoxic effect on corneal epithelial cells of sheep, as well as phytochemicals assays and identification of phenolic compounds and organic acids present in the extracts by UPLC - MS. The highest values of total phenolic content were obtained with peel and seed extracts and to ascorbic acid in the seed of
siriguela, showing better antioxidant activities of seeds and peel extracts of siriguela and umbu. Lipid peroxidation assays indicated that genipap pulp is a promising antioxidant. Genipap pulp and siriguela seed ethanol extracts presented an acetylcholinesterase inhibition zone similar to that of the positive control, carbachol. The investigation of phenols and organic acid contents revealed the presence of
quercetin (48,38 to 3,88 μg.g-1), quinic acid (43,28 to 41,88 μg.g-1) and citric acid (3,78 to 0,43 μg.g-1) in several extracts and chlorogenic acid with the highest amount found in siriguela seeds (356,93 μg.g-1). These data suggest new uses for these foods as potential antioxidant supplements for the food, pharmaceutical and cosmetic industries.Coordenação de Aperfeiçoamento de Pessoal de Nível Superior
A partir das cascas, polpas e sementes do jenipapo (Genipa americana Linnaeus), umbu (Spondia tuberosa Arruda), siriguela (Spondia purpurea Linnaeus) e mangaba (Hancornia speciosa Gomes) foram preparados extratos etanólicos, com exceção da mangaba onde o extrato foi preparado utilizando casca e polpa. Os extratos foram submetidos à investigação da capacidade antioxidante através dos métodos de determinação do conteúdo de ácido ascórbico e fenóis totais, sequestro do radical 2,2-difenil-1-picril-hidrazil e 2,2´- azinobis (3-etilbenzotiazolina-6-ácido sulfônico), capacidade antioxidante de redução do ferro e cobre, lipoperoxidação utilizando um sistema de membranas biomimético e mensuração enzimática da catalase e superóxido dismutase. Também foi avaliada a atividade inibitória da enzima acetilcolinesterase, o efeito citotóxico em células epiteliais da córnea de ovelhas, além da realização de ensaios fitoquímicos e a identificação de compostos fenólicos e ácidos orgânicos presentes nos extratos. Os maiores teores de fenóis totais foram obtidos nos extratos das cascas e sementes e no referente ao ácido ascórbico na semente da siriguela, apresentando melhor atividade antioxidante os extratos das sementes e cascas da siriguela e do umbu. Porém, no ensaio de peroxidação lipídica, o extrato etanólico da polpa de jenipapo demonstrou ser um antioxidante promissor. Os extratos etanólicos da polpa do jenipapo e da semente da siriguela apresentaram uma zona de inibição da enzima acetilcolinesterase semelhantes ao controle positivo, carbacol. Na investigação dos compostos fenólicos e ácidos orgânicos por UPLC-MS verificou-se a presença nos extratos de quercetina (48,38 a 3,88 μg.g-1), ácido quínico (43,28 a 41,88 μg.g-1), ácido cítrico (3,78 a 0,43 μg.g-1) em vários extratos. E ácido clorogênico, na semente da siriguela (356,93 μg.g-1). Os resultados obtidos desses extratos sugerem novas formas de utilização desses alimentos como potenciais suplementos antioxidantes na indústria alimentícia, farmacêutica e cosmética.
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Janura, Michal. "Biologická aktivita obsahových látek rostlin XXVIII. Alkaloidy vybraných odrůd taxonu Narcissus cyclamineus REDOUTÉ a jejich účinek na acetylcholinesterasu a butyrylcholinesterasu." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-332599.
Повний текст джерелаАнотація:
Biological activity of plant metabolites XXVIII. Alkaloids from selected cultivars of Narcissus cyclamineus REDOUTÉ and their influence on acetylcholinesterase and butyrylcholinesterase. JANURA M.: Diploma work, Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of Pharmaceutical Botany and Ecology, Hradec Králové 2015, Czech Republic. Abstract: The summary extracts of alkaloids from bulbs of N. cyclamineus esp. N. cyclamineus cv. Jenny, N. cyclamineus cv. Little Witch, N. cyclamineus cv. Rapture, N. cyclamineus cv. Surfside, N. cyclamineus cv. Peeping Tom, N. cyclamineus cv. Warbeld and N. cyclamineus cv. Skater's Waltz were obtained by the procedures common for this type of compounds. The alkaloid extracts were analyzed by GC/MS and the probable occurrence of individual alkaloid substances was observed. These extracts were also assayed for HuAChE and HuBuChE inhibitory activity. N. cyclamineus cv. Surfside with IC50 = 61,26 ± 6,42 µg/ml and N. cyclamineus cv. Warbeld with IC50 = 85,43 ± 11,13 µg/ml have the best results in inhibition of HuBuChE. The best inhibitory activity on HuAChE has N. cyclamineus cv. Warbeld with IC50 (HuAChE) = 36,82 ± 4,50 µg/ml. Key words: Narcissus, Acetylcholinesterase, Butyrylcholinesterase, GC/MS, Alzheimer's disease.
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Farkašovský, Marek. "Biologická aktivita obsahových látek rostlin XXIX. Alkaloidy vybraných odrůd taxonu Narcissus triandrus L. a jejich účinek na acetylcholinesterasu a butyrylcholinesterasu." Master's thesis, 2015. http://www.nusl.cz/ntk/nusl-335201.
Повний текст джерелаАнотація:
Farkašovský M.: Biological activity of plant metabolites XXIX. Alkaloids of selected cultivars of Narcissus triandrus L. and their influence on acetylcholinesterase and butyrylcholinesterase. Diploma thesis. Charles University in Prague, Faculty of Pharmacy in Hradec Králové, Department of pharmaceutical botany and ecology, Hradec Králové 2015, 70 pages Screening of seven bulb samples of Narcissus genus was performed. It included cultivars Narcissus triandrus cv. Hawera, Narcissus triandrus cv. Ice Wings, Narcissus triandrus cv. Stint, Narcissus triandrus cv. Tresamble, Narcissus cyclamineus cv. February Gold, Narcissus cyclamineus cv. Greenlet and Narcissus cyclamineus cv. Itzim. Primary extract was prepared by boiling crushed bulbs in ethanol 95% and then it was condensated. After extraction in diethyl ether and ethyl acetate was pure alkaloid extract dried with air flow in water bath. Isolated alkaloid extracts were tested for their inhibition activity on acetylcholinesterase and butyrylcholinesterase. Also GC-MS analysis was provided to identify alkaloids. These alkaloids were identified with GC-MS analysis - epinorgalanthamine, galanthamine, galanthine, haemanthamine, hippeastrine, homolycorine, cherylline, incartine, lycoramine, lycoramine-acetate, lycorine, narwedine, neruscine, sanguinine...
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Tanková, Sabina. "Alkaloidy rodu Narcissus a jejich biologická aktivita." Master's thesis, 2019. http://www.nusl.cz/ntk/nusl-396795.
Повний текст джерелаАнотація:
Charles University, Faculty of Pharmacy in Hradec Králové Department of Pharmacognosy Candidate: Sabina Tanková Supervisor: PharmDr. Daniela Hulcová, PhD. Title of diploma thesis: Alkaloids of the genus Narcissus and their biological activity. Key worlds: Narcissus pseudonarcissus L. cv. Dutch Master, Amaryllidaceae, alkaloids, AChE, BuChE, POP, GSK-3β, biological activity. Alkaloid extract obtained from bulbs of Narcissus pseudonarcissus L. cv. Dutch Master was extracted by ethanol and was purified by liquid-liquid extraction and fractionated by column chromatography to individual fractions. At the end, were obtained 11 pooled fractions, which were used to isolate pure alkaloids. The ND 3-5 / 7 fraction was processed by preparative thin layer chromatography followed by crystallization of pure substances. In total, 5 alkaloid substances of ST1D2, ST1D3, ST2A, ST2B1 and ST3C were obtained from this fraction in various amounts. These substances were determined by GC-MS analysis, NMR analysis and optical rotation. Subsequently, the obtained data were compared with the NIST library spectra and the literature. Isolated substances have been identified as caranine, O-ethyllycorenine, narwedine, pluviine and N-demethylhomolycorine. The alkaloids obtained in sufficient amounts were subsequently subjected to...
Книги з теми "Acetylcholinesterase – analyse"
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Bjorkman, Camilla. Methodological and biochemical aspects of acetylcholinesterase and acetate in blood from cattle , and acetyl-CoA synthesizing enzymes in spinal cord from ruminants and monogastric animals. Uppsala: Sveriges Lantbruksuniversitet, 1989.
Знайти повний текст джерелаЧастини книг з теми "Acetylcholinesterase – analyse"
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Bachmann, Till, Jürgen Pleiss, Francois Villatte, and Rolf D. Schmid. "Bioresponse-Linked Analysis Based on Acetylcholinesterase Inhibition." In Bioresponse-Linked Instrumental Analysis, 105–30. Wiesbaden: Vieweg+Teubner Verlag, 2001. http://dx.doi.org/10.1007/978-3-322-86568-7_5.
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Schalk, Isabelle, Laurence Ehret-Sabatier, Françoise Bouet, Maurice Goeldner, and Christian Hirth. "Structural Analysis of Acetylcholinesterase Ammonium Binding Sites." In Multidisciplinary Approaches to Cholinesterase Functions, 117–20. Boston, MA: Springer US, 1992. http://dx.doi.org/10.1007/978-1-4615-3046-6_16.
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Sippl, Wolfgang, Jean-Marie Contreras, Yveline Rival, and Camille G. Wermuth. "Comparative Molecular Field Analysis of Aminopyridazine Acetylcholinesterase Inhibitors." In Molecular Modeling and Prediction of Bioactivity, 53–58. Boston, MA: Springer US, 2000. http://dx.doi.org/10.1007/978-1-4615-4141-7_4.
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Pinto, Julia C., Jean Jacques Bourguignon, and Camille-Georges Wermuth. "Characterization of the pharmacophoric pattern of acetylcholinesterase inhibitors through conformational analysis." In Trends in QSAR and Molecular Modelling 92, 425–26. Dordrecht: Springer Netherlands, 1993. http://dx.doi.org/10.1007/978-94-011-1472-1_104.
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Voogd, J., N. M. Gerrits, and D. T. Hess. "Parasagittal Zonation of the Cerebellum in Macaques: An Analysis based on Acetylcholinesterase Histochemistry." In Cerebellum and Neuronal Plasticity, 15–40. Boston, MA: Springer US, 1987. http://dx.doi.org/10.1007/978-1-4613-0965-9_2.
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Aranda, Mario, Jonathan Carrasco, and Karem Henríquez. "Acetylcholinesterase (ACHE) and α-Glucosidase Inhibitory Assay by Effect-Directed Analysis on High Performance Thin-Layer Chromatography Coupled to Mass Spectrometry." In Mass Spectrometry for Food Analysis, 213–18. New York, NY: Springer US, 2022. http://dx.doi.org/10.1007/978-1-0716-2107-3_16.
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Fournier, Didier, Annick Mutero, Madeleine Pralavorio, and Jean Marc Bride. "Drosophila Acetylcholinesterase: Analysis of Structure and Sensitivity to Insecticides by In Vitro Mutagenesis and Expression." In Multidisciplinary Approaches to Cholinesterase Functions, 75–81. Boston, MA: Springer US, 1992. http://dx.doi.org/10.1007/978-1-4615-3046-6_10.
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Dolezal, Rafael, Jiri Krenek, Veronika Racakova, Natalie Karaskova, Nadezhda V. Maltsevskaya, Michaela Melikova, Karel Kolar, Jan Trejbal, and Kamil Kuca. "ANN and GMDH Algorithms in QSAR Analyses of Reactivation Potency for Acetylcholinesterase Inhibited by VX Warfare Agent." In Computational Collective Intelligence, 171–81. Cham: Springer International Publishing, 2017. http://dx.doi.org/10.1007/978-3-319-67077-5_17.
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Boué, André, and F. Muller. "Ultrasound Indications for Laboratory Testing." In Fetal Medicine, 203–15. Oxford University PressNew York, NY, 1995. http://dx.doi.org/10.1093/oso/9780192619044.003.0009.
Повний текст джерелаАнотація:
Abstract Fortuitous finding of anomaly on ultrasound examination is a frequent indication for laboratory analyses which are increasingly indispensable in the appropriate management of cases. In terms of diagnosis, the indication may be for diagnosis of cause (e.g. chromosomal anomaly), or for more precise diagnosis (e.g. acetylcholinesterase for neural tube defect).
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Fernandes, C. C., M. B. Santiago, C. H. G. Martins, J. B. A. Silva, A. E. M. Crotti, and M. L. D. Miranda. "ESSENTIAL OIL FROM EUGENIA PYRIFORMIS CAMBESS AERIAL PARTS AND ITS MAJOR CONSTITUENT LIMONENE AS AN AGENT WITH ANTI-ACETYLCHOLINESTERASE AND ANTICARIOGENIC ACTIVITIES." In Open Science Research XII, 510–22. Editora Científica Digital, 2023. http://dx.doi.org/10.37885/230613489.
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This study aimed at determining, for the first time, anticariogenic and anti-acetylcholinesterase activities of essential oil from Eugenia pyriformis aerial parts (EP-EO) and its major constituent limonene against cariogenic bacteria and the enzyme acetylcholinesterase (AChE). EP-EO and limonene were subject to the broth microdilution method on 96-well microplates and determination of minimum inhibitory concentration (MIC) and minimum inhibitory concentration of biofilm (MICB50) (µg/mL). AChE inhibition was qualitatively evaluated by Thin Layer Chromatography (TLC). EP-EO and limonene not only showed strong anticariogenic activity, since their MIC and MICB50 values ranged between 20 and 400 µg/mL, but also inhibited cholinesterase when subject to TLC. Both GC-MS and GC-FID analyses identified and quantified the following major constituents: limonene (14.8%), nerolidol (11.0%) and α-cadinol (10.3%). This study showed that EP-EO and limonene were active in in vitro assays and, thus, may be important targets of further in vivo studies.
Тези доповідей конференцій з теми "Acetylcholinesterase – analyse"
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Wilcox, Phillip G., and Jin U. Kang. "Raman spectroscopic analysis of whole blood acetylcholinesterase." In SPIE Sensing Technology + Applications, edited by Šárka O. Southern, Mark A. Mentzer, Isaac Rodriguez-Chavez, and Virginia E. Wotring. SPIE, 2014. http://dx.doi.org/10.1117/12.2052701.
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Krunić, Mihajlo J., Jelena Z. Penjišević, Slađana Kostić-Rajačić, Vladimir B. Šukalović, Deana B. Andrić, and Ivana I. Jevtić. "Pyrazole/tacrine derivatives as potential cholinesterase inhibitors." In 2nd International Conference on Chemo and Bioinformatics. Institute for Information Technologies, University of Kragujevac, 2023. http://dx.doi.org/10.46793/iccbi23.567k.
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Two new tacrine/pyrazole conjugates were designed, synthesized, and pharmacologically evaluated for their inhibitory activity toward acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). A scalable and cost-efficient synthetic route was developed, and key reaction steps for the synthesis of compounds 4a,b were nucleophilic substitution of α-aroylketene dithioacetals with tacrine intermediates, followed by cyclocondensation of respective N,S-acetals with hydrazine hydrate. The preliminary pharmacological evaluation revealed high inhibitory activities of 4a,b toward AChE (180 and 259 nM, respectively) and BuChE (51 and 95 nM, respectively) as compared with known inhibitor, tacrine. Overall, both compounds were more efficient BuChE inhibitors while 4a, with a shorter linker connecting tacrine and phenylpyrazole moieties, showed higher inhibitory activity toward both enzymes. Molecular docking analysis strongly corroborated pharmacological results since both compounds interacted favorably with target enzymes. Calculated pharmacokinetic properties (absorption, distribution, metabolism, and excretion (ADME) showed that 4a,b obey Lipinski’s rule of druglikeness and are promising lead compounds for the development of new drug candidates.
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Vasilyev, V. V., and A. A. Bliznyuk. "Analysis of the role of different environmental effects in enzymatic catalysis. A hybrid quantum chemical and molecular mechanical study of acetylcholinesterase activity." In The first European conference on computational chemistry (E.C.C.C.1). AIP, 1995. http://dx.doi.org/10.1063/1.47660.
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Lima, Márcio Pinheiro, Rafael Tuzino Leite Neves Maffei, Pedro Henrique Almeida Fraiman, João Victor Cabral Correia Férrer, Adriel Rêgo Barbosa, Victor Cardoso de Faria, Gabriel Pinheiro Martins de Almeida e. Souza, Ruan Gambardella Rosalina de Azevedo, Lucas Toshio Uenishi, and Gisele Sampaio Silva. "Super-refractory status epilepticus after intoxication by quetiapine and carbamate." In XIV Congresso Paulista de Neurologia. Zeppelini Editorial e Comunicação, 2023. http://dx.doi.org/10.5327/1516-3180.141s1.584.
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Introduction: Quetiapine, an atypical antipsychotic, works through the agonism of multiple brain receptors, including dopaminergic, serotonergic, and adrenergic receptors. Compared to typical antipsychotics, quetiapine has a more favorable profile of adverse reactions. Myoclonus is infrequent. However, there have been reports of quetiapine overdose associated with generalized myoclonus. Electroencephalogram (EEG) modifications linked to the use of quetiapine are unusual. Aldicarb, commonly known as ‘chumbinho’ in Brazil, is a carbamate used as a rodenticide. Its toxicity is caused by the inhibition of acetylcholinesterase. A few reported cases of myoclonus related to its use may be due to the anticholinesterase effect causing hyperactivity. This is a case report based on retrospective analysis of the patient’s records. Case report: A 23-year-old woman was admitted after a suicide attempt by ingesting carbamate and quetiapine 36 hours after the attempt. Her initial symptoms were vomiting and sialorrhea, followed by generalized tonic-clonic seizures and coma. At admission, she was already sedated with midazolam, with her last tonic-clonic generalized seizure two hours earlier. Her pupils were myotic, with persistent tachycardia and diffuse muscular hyperexcitability – clonic movements were evoked with minimal stimuli. Brain imaging and cerebrospinal fluid analysis showed no alterations. A loading dose of 20 mg/kg of phenytoin was administered. Upon admission, an EEG showed status myoclonus. Midazolam was then titrated to 0.8 mg/kg/h, and clobazam (30 mg/day) and levetiracetam (1.500 mg/day) were added, with resolution of the status epilepticus after three days. Conclusion: Status epilepticus should be considered a possible presentation of quetiapine and carbamate intoxication.
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Radić, Zoran, Stephanie Luedtke, Celine Bojo, Yunshen Li, Emilio Luna та Bianca Pomar. "Shifts in Cα backbone conformation in X-ray structures of human acetylcholinesterase covalently inhibited by organophosphorates and organophosphoramidates revealed by PACCT3 comparative analysis". У The 2nd International Online Conference on Crystals. Basel, Switzerland: MDPI, 2020. http://dx.doi.org/10.3390/iocc_2020-07339.
Повний текст джерелаЗвіти організацій з теми "Acetylcholinesterase – analyse"
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Ginzberg, Idit, Richard E. Veilleux, and James G. Tokuhisa. Identification and Allelic Variation of Genes Involved in the Potato Glycoalkaloid Biosynthetic Pathway. United States Department of Agriculture, August 2012. http://dx.doi.org/10.32747/2012.7593386.bard.
Повний текст джерелаАнотація:
Steroidal glycoalkaloids (SGAs) are secondary metabolites being part of the plant defense response. The two major SGAs in cultivated potato (Solanum tuberosum) are α-chaconine and α-solanine, which exhibit strong cellular lytic properties and inhibit acetylcholinesterase activity, and are poisonous at high concentrations for humans. As SGAs are not destroyed during cooking and frying commercial cultivars have been bred to contain low levels, and their content in tubers should not exceed 20 mg/100 g fresh weight. However, environmental factors can increase tuber SGA content above the safe level. The focus of the proposed research was to apply genomic approaches to identify candidate genes that control potato SGA content in order to develop tools for potato improvement by marker-assisted selection and/or transgenic approaches. To this end, the objectives of the proposal included identification of genes, metabolic intermediates and allelic variations in the potato SGAbiosynthetic pathway. The SGAs are biosynthesized by the sterol branch of the mevalonic acid/isoprenoid pathway. Transgenic potato plants that overexpress 3-hydroxy-3-methylglutaryl-CoA reductase 1 (HMG1) or squalene synthase 1 (SQS1), key enzymes of the mevalonic acid/isoprenoid pathway, exhibited elevated levels of solanine and chaconine as well as induced expression of genes downstream the pathway. These results suggest of coordinated regulation of isoprenoid (primary) metabolism and SGA secondary metabolism. The transgenic plants were further used to identify new SGA-related candidate genes by cDNA-AFLP approach and a novel glycosyltransferase was isolated. In addition, genes involved in phytosterol biosynthesis may have dual role and synthesize defense-related steroidal metabolites, such as SGAs, via lanosterol pathway. Potato lanosterol synthase sequence (LAS) was isolated and used to prepare transgenic plants with overexpressing and silencing constructs. Plants are currently being analyzed for SGA content. The dynamics of SGA accumulation in the various organs of a potato species with high SGA content gave insights into the general regulation of SGA abundance. Leaf SGA levels in S. chacoense were 10 to 20-fold greater than those of S. tuberosum. The leptines, SGAs with strong antifeedant properties against Colorado potato beetles, were present in all aerial tissues except for early and mid-developmental stages of above ground stolons, and accounted for the high SGA content of S. chacoense. These results indicate the presence of regulatory mechanisms in most tissues except in stolons that limit the levels of α-solanine and α-chaconine and confine leptine accumulation to the aerial tissues. The genomes of cultivated and wild potato contain a 4-member gene family coding for SQS. Three orthologs were cloned as cDNAs from S. chacoense and heterologously expressed in E. coli. Squalene accumulated in all E. coli lines transformed with each of the three gene constructs. Differential transcript abundance in various organs and amino acid sequence differences in the conserved domains of three isoenzymes indicate subfunctionalization of SQS activity and triterpene/sterol metabolism. Because S. chacoense and S. phureja differ so greatly for presence and accumulation of SGAs, we selected four candidate genes from different points along the biosynthetic pathway to determine if chcor phuspecific alleles were associated with SGA expression in a segregating interspecific diploid population. For two of the four genes (HMG2 and SGT2) F2 plants with chcalleles expressed significantly greater total SGAs compared with heterozygotes and those with phualleles. Although there are other determinants of SGA biosynthesis and composition in potato, the ability of allelic states at two genes to affect SGA levels confirms some of the above transgenic work where chcalleles at two other loci altered SGA expression in Desiree. Present results reveal new opportunities to manipulate triterpene/sterol biosynthesis in more targeted ways with the objective of altering SGA content for both human health concerns and natural pesticide content without disrupting the essential metabolism and function of the phytosterol component of the membranes and the growth regulating brassinosteroids.