Teses / dissertações sobre o tema "Curcumine – Analogues"
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Jourdan, Jean-Pierre. "Conception, synthèse et évaluation biologique de nouveaux analogues de la curcumine : potentiels agents pléiotropes d'intérêt thérapeutique dans la maladie d'Alzheimer". Caen, 2015. http://www.theses.fr/2015CAEN4012.
Texto completo da fonteAlzheimer's disease, the most common form of elderly dementia in the world, is a progressive, chronic, degenerative and irreversible disease. They are many pathophysiological causes of dementia, among them there may be mentioned β-aggregation of amyloid peptides, tau protein hyperphosphorylation, neuronal inflammation and oxidative stress. A recently developed therapeutic approach to modify the evolution of this multifactorial disease is the design of multi-target directed ligands. In the nature, there are molecules with such functions like curcumin. It’s a natural polyphenol extracted from the plant Curcuma longa L. And it can be considered as an active product useful in the treatment of Alzheimer's disease because of its inhibitory properties of β-amyloid aggregation, antioxidant and inflammatory inhibition activities. However, it suffers from poor bioavailability and can’t be used in therapy. That's why we designed novel curcumin analogs in pyrrolizinone and aminoindanone series as potential multi-target ligands potentially useful in the treatment of Alzheimer's disease. In this manuscript, is described the drug design approach combining medicinal chemistry, molecular modeling and biological assessments leading to these analogues. Finally, a preliminary drugability study of the newly synthesized compounds is presented
Pecourneau, Jérémy. "Réponses photoinduites d'analogue biomimétique de la cyclocurcumine : vers des thérapies assistées par la lumière". Electronic Thesis or Diss., Université de Lorraine, 2022. http://www.theses.fr/2022LORR0205.
Texto completo da fonteBeyond photodynamic therapy (PDT), there are several light-assisted therapeutic alternatives, including photothermal therapy (PTT) and photoisomerization, whose mechanical action would induce cellular damage within the membranes. Also, molecules able to simultaneously absorb two photons would overcome the need for high energy excitation per photon while maintaining sufficient tissue penetration. In this context, we were interested in designing and studying biomimetic analogues of cyclocurcumin (CC), a natural E/Z photoswitch. Guided by molecular modeling, those novel donor-acceptor compounds were structurally designed to increase the effective two-photon absorption cross section (σ2).First, we synthesized two classes of CC analogues bearing acceptor (oxo and malonitrile) and donor (hydroxy, alkoxy and amine) groups as well as a PEG arm to increase their hydrophilicity. Free in solution, the oxo derivatives show a reversible photoinduced isomerization, without any thermal isomerization in the dark, whereas the malonitrile derivatives do not photoswitch but undergo a vibrational relaxation. This is leading to a temperature increase, of interest in photothermal therapy. Finally, confined in a lipidic environment (liposomes bilayers and Langmuir monolayers), the direct E→Z isomerization kinetics of oxo compounds is strongly slowed down and no Z→E back isomerization is observed. Those compounds also showed a certain efficiency to disrupt membrane fluidity, more or less pronounced depending on the form, Z or E, the length of the alkoxy chain or the presence of the PEG unit. The malonitrile derivatives exhibit a diminished photothermal effect in lipid bilayers after several irradiation cycles.Taken together, this study is a proof of concept for the potential of photoinduced responses of cyclocurcumin analogs for disruption of membrane fluidity towards potential use in vivo
Schmitt, Bonell. "Curcumin analogues as ligands for Re (I) and (V)". Thesis, Nelson Mandela Metropolitan University, 2012. http://hdl.handle.net/10948/d1020975.
Texto completo da fonteSouza, Nayane de. "Efeitos citotóxicos do DM-1 em células de melanoma resistentes a um inibidor de BRAF e na expressão de metaloproteinases". Universidade de São Paulo, 2017. http://www.teses.usp.br/teses/disponiveis/9/9143/tde-06122017-105135/.
Texto completo da fonteMalignant melanoma is the most aggressive cancer and the BRAF V600E mutation is the most frequent among patients. Vemurafenib was the first specific inhibitor for this mutation approved by Food and Drug Administration. Therefore around six months later there is relapse and overcoming it is still a challenge. Curcumin is a turmeric and it has been deeply researched because of its anti-inflammatory and antitumoral effects. However the low stability limits its use, therefore, encouraged the investigation of analogues capable to be efficient and commercialized. DM-1 is a monoketone curcumin analog and it showed antitumoral effects in vitro and in vivo in previous studies The aim of this project was to evaluate the cytotoxical effects of DM-1 for vemurafenib responsive (naïve) and resistant melanoma cells, as well as metalloproteinases modulation. Melanoma cells were treated with different DM-1 concentrations, and this compound was cytotoxic for responsive and resistant cell lines, besides inducing G1/G0 cell cycle arrest and reducing the number of colonies, nonetheless it was not selective in assays performed with melanocytes and fibroblasts. Subtoxic treatment of those cells modulated important MMPs in the cell invasion process. DM-1 reduced metalloproteinases -1, -2 and -9 (MMP-1,-2 and -9) in a quantification assay, and MMP-2 and -9 activities by zymography in a cell-dependent way. Negative modulations of MMP inhibitor TIMP-2 and MMP-14 for SKMEL-28 naïve were associated with MMP-2 and -9 reduced activities, whereas positive modulations for SKMEL-19 naïve were correlated to MMP-2 increase. Furthermore, this compound reduced migration of those cells and endothelial cell tube formation.
Al-shdifat, Laith Mohammad Hilal. "Approaches to Enhancing the Properties of a Promising Curcumin Analogue". Thesis, The University of Sydney, 2021. https://hdl.handle.net/2123/25786.
Texto completo da fonteAbdelhamid, Dalia. "Natural Products as Lead Compounds for Drug Development. Part I: Synthesis and Biological Activity of a Structurally Diverse Library of Curcumin Analogues. Part II: Synthesis of Novel Sterol Natural Products and Related Analogues as Antileishmanial Ag". The Ohio State University, 2011. http://rave.ohiolink.edu/etdc/view?acc_num=osu1299685922.
Texto completo da fonteTedesco, Serena. "Activation phenotypes of human monocyte-derived macrophages: methodological approaches and pharmacological modulation by curcumin analogues". Doctoral thesis, Università degli studi di Padova, 2016. http://hdl.handle.net/11577/3427229.
Texto completo da fonteIn condizioni normali i macrofagi sono i responsabili della risposta immunitaria e della difesa dell’ospite per mantenere l’omeostasi tissutale. In seguito a stimoli presenti nel microambiente, i macrofagi possono attivarsi, andando incontro a uno switch morfologico e funzionale. L’attivazione di queste cellule non è un processo “tutto o nulla” ma piuttosto un continuum caratterizzato da un ampio spettro di fenotipi molecolari e funzionali, i cui estremi sono rappresentati dal fenotipo definito “classico” o M1, con un profilo pro-infiammatorio, e da quello “alternativo” o M2, anti-infiammatorio e protettivo. La possibilità di promuovere un fenotipo macrofagico protettivo sta diventando un obiettivo terapeutico nel trattamento delle condizioni infiammatorie e l’identificazione di fattori che regolano l’attivazione cellulare è attualmente un’area di ricerca molto attiva. La maggior parte degli studi in questo ambito sono stati condotti utilizzando culture primarie di macrofagi di topo o linee cellulari; inoltre, i vari laboratori usano protocolli diversi di isolamento/differenziamento dei monociti e marcatori diversi di attivazione. Inoltre, il controllo farmacologico dell’attivazione macrofagica non è ancora stato indagato sufficientemente. Una serie di composti naturali e sintetici, ad esempio il calcone e la curcumina, il principale componente attivo della Curcuma longa (pianta nota per effetti anti-ossidanti, anti-microbici, anti-tumorali e anti-infiammatori) hanno dimostrato un effetto sulla funzione dei macrofagi, agendo attraverso diversi meccanismi farmacologici, ad esempio interferendo con il signaling del TLR4. Sulla base di queste premesse, gli scopi specifici di questo lavoro di tesi erano: a) testare un modello cellulare e un protocollo di differenziamento diverso da quello spontaneo, in particolare la linea cellulare monocitaria THP-1 e il differenziamento in presenza di CSF-1; b) determinare il profilo delle citochine presenti nel terreno di coltura e c) determinare la modulazione dei marcatori dei fenotipi di attivazione da parte di agenti farmacologici, in particolare da derivati di sintesi della curcumina, noti per la loro capacità di modulare l’attivazione di cellule murine di microglia attraverso la riduzione della produzione e rilascio di mediatori pro-infiammatori. I macrofagi sono stati differenziati a partire dai linfo-monociti umani isolati tramite gradiente di densità e coltivati in terreno RPMI + 10% FBS con aggiunta di CSF-1 per 6 giorni, ottenendo così macrofagi in condizioni basali (M0). Il fenotipo classico (M1) e il fenotipo alternativo (M2) sono stati ottenuti incubando i macrofagi M0 rispettivamente con 0.1-1 μg/ml LPS e IL-4 20 ng/ml + IL-13 5 ng/ml, in presenza o assenza di analoghi della curcumina, desametazone o CLI095, un inibitore del dominio intracellulare del TLR4 (questi ultimi utilizzati come composti di riferimento). I fenotipi macrofagici sono stati determinati tramite citofluorimetria utilizzando specifici anticorpi legati a fluorofori. L’espressione genica è stata valutata tramite qRT-PCR. La composizione dei terreni condizionati (macrophage conditioned media, MCM) è stata valutata con la tecnologia Luminex. Gli analoghi della curcumina sono stati gentilmente forniti dalla Prof.ssa Federica Belluti (Università di Bologna). In seguito a polarizzazione per 24 h con IL-4/IL-13 abbiamo osservato un aumento dell’espressione dei marcatori M2 rispetto a M0. Per quanto riguarda l’espressione genica di macrofagi differenziati con CSF-1, come atteso, i macrofagi M1 dopo 6 o 48h presentavano livelli superiori di mRNA per TNF-α e IL-1β rispetto a M0. L’aumento dell’mRNA era più marcato dopo 48 h per tutti i geni tranne TNF-α, che raggiungeva il picco a 6h. L’mRNA della citochina anti-infiammatoria IL-10 inaspettatamente era più espresso nei macrofagi M1 rispetto a M2 e raggiungeva il picco dopo 6 h. Rispetto a M0, l’MCM M2 era caratterizzato da alti livelli di citochine anti-infiammatorie tra le quali CCL22 e IL-4. Al contrario, l’MCM M1 presentava livelli elevati di IL-1α, IL-1β, IL-6, IL-8, MCP-1, VEGF e TNF-α. Il pre-trattamento con l’analogo della curcumina GG9 e il controllo positivo CLI095 ha prevenuto l’aumento indotto da LPS del marcatore M1 CD80. Un effetto simile è mantenuto anche sulla frazione di cellule a doppia marcatura CD80+/CCR2+. Al contrario del desametazone, che aumenta la percentuale di cellule CD163+ (M2), il GG9 non ha modulato i marcatori M2. Il trattamento con GG9 ha bloccato in maniera significativa la produzione di IL-1β valutata come citochina cell-bound, nel lisato cellulare o rilasciata nel terreno di coltura. Al contrario, l’analogo GG6 non ha modificato i livelli di IL-1β intra- ed extra-cellulare. Per indagare più nel dettaglio le vie di segnale coinvolte nell’attivazione di queste cellule, abbiamo effettuato analisi Western Blot di fattori coinvolti nella via di segnale di NF-κB. L’attivazione con LPS ha ridotto significativamente l’espressione relativa di IκB-α. Curcumina, GG6 e CLI095 hanno riportato IκB-α ai livelli di controllo, a differenza del GG9 che non modificava significativamente l’espressione di questa proteina. Pertanto, i macrofagi M1 ed M2 presentano specifici profili di attivazione genica e di marcatori di superficie che possono essere modulati in seguito a trattamento farmacologico con desametazone o analoghi della curcumina. Nel complesso, questi dati suggeriscono che protocolli di attivazione macrofagica possono avere un impatto sullo stato funzionale di queste cellule e sono fondamentali per definire nuove strategie di targeting farmacologico nei macrofagi umani.
SINGH, REETIKA. "COMPARATIVE ANALYSIS OF DIFFERENT CURCUMIN ANALOGUES TO INHIBIT TLR4 EXPRESSION IN BREAST CANCER- AN IN-SILICO STUDY". Thesis, DELHI TECHNOLOGICAL UNIVERSITY, 2021. http://dspace.dtu.ac.in:8080/jspui/handle/repository/18459.
Texto completo da fonte"INVESTIGATING THE MASS SPECTROMETRIC BEHAVIOR OF NOVEL ANTINEOPLASTIC CURCUMIN ANALOGUES". Thesis, 2015. http://hdl.handle.net/10388/ETD-2015-01-1911.
Texto completo da fonteZe, Chen Chu, e 陳楚澤. "Xanthine Oxidase and α-Glucosidase Inhibition of Curcumin and Curcumin Analogs". Thesis, 2015. http://ndltd.ncl.edu.tw/handle/y83s8x.
Texto completo da fonte輔仁大學
食品科學系碩士班
103
Curcumin is a constituent from root and stem of family Zingiberaceae and Araceae. It has been used as a natural colorant in food industry. Curcumin has a great value in food and medicine, and it has been reported that curcumin could inhibit the activities of xanthine oxidase (XO) and α-glucosidase that make curcumin can be used for treatment of gout and diabetes. Chemical synthesis, which can change the structure of component, can enhance the activities, even create a new one. Therefore, the objective of this research is to evaluate the characterization of curcumin and its analogs as XO and α-glucosidase inhibitors. In this study, after screening XO and α-glucosidase inhibition, the components which have high inhibitory activities were calculated their half-maximal inhibitory concentration (IC50) and enzyme inhibitory kinetics. In order to calculating the inhibitory reaction constant, a docking algorithm simulates binding position between enzyme and inhibitors. The results showed that among all the curcumin and its analogs, CM-F had the strongest anti-oxidant activity with a half-maximal effective concentration (EC50) of 9.39 ± 0.16 μM, which was better than vitamin E (EC50=17.03 ± 0.09 μM). It also had a good XO inhibitory activity, and its IC50 value against XO was 6.14 ± 0.38 μM. The enzyme kinetic result showed it was competitive inhibition. As for α-glucosidase, CM-1 and CM-2 have good α-glucosidase inhibitory activities with the IC50 value of 21.06 ± 0.92 μM and 5.95 ± 0.09 μM, of which kinetic study indicates that both CM-1 and CM-2 are mix-competitive inhibitors on α-glucosidase. Furthermore, docking simulation showed there are 5 hydrogen bonds between XO and CM-F. However, only 1 and 2 hydrogen bonds involved in CM-1 and CM-2 binding to α-glucosidase, respectively. Accordingly, analogs of curcumin have the potentials using in the gout or diabetes patients.
Ou, Jun-Lin, e 歐俊麟. "Comparative analysis of curcumin analogues on anti-influenza virus activity". Thesis, 2013. http://ndltd.ncl.edu.tw/handle/32377636392422952105.
Texto completo da fonte國立中興大學
微生物暨公共衛生學研究所
101
Curcumin is a commonly used colouring agent and spice in food. Accumulated evidence indicates that curcumin is associated with a great variety of pharmacological activities, including an antimicrobial effect. Previously, we reported curcumin inhibits the infection of type A influenza virus (IAV) and proved one of the mechanisms is through interfering the viral HA activity. To investigate the structure contributing to its anti-IAV activity, structural and functional analogues of Curcumin (Cur), such as Tetrahydrocurcumin (THC), Monoacetylcurcumin (MAC) and Petasiphenol (Pet) were comparatively analyzed in the current study. The result of time-of-drug addition tests revealed that all the analogues analyzed were able to inhibit IAV production in cell cultures; MAC has a similar strength to curcumin, whereas Pet and THC inhibit IAV to a much less extent than curcumin. Comparative analysis of curcumin analogues described herein demonstrated that Thc and Pet have much less effect on suppression of plaque formation ability; the EC50 of pet are 14.65 μM, whereas curcumin and MAC is 0.17 and 0.2 μM, respectively. Surprisingly, none of the analogues harbors HA inhibition effect. Considering that as with curcumin, the structure of MAC contains two double bonds in the central seven-carbon chain, whereas Pet and THC has one or none, respectively, it indicates the presence of double bond is crucial for the anti-IAV activity. The unsaturated carbonyl group acts as the acceptor of Michael addition reaction that involves in the intermolecular conjugation by formation of covalent Michael adducts with certain proteins. It is very possible that via Michael addition reaction, curcumin conjugated with viral protein that in turns alters or interferes with the function of viral surface proteins and inactivate virus infectivity. In conclusion, THC, one of the stable curcumin metabolites exhibits anti-IAV activity and MAC appears to be an effective agent for inhibition of IAV infection. Moreover, comparative analysis of curcuminoids indicated that the two double bonds in the central seven-carbon chain contribute to the curcumin -mediated anti-IAV activity.
Chen, Yong-Song, e 陳永崧. "Synthesis and anticancer activity of curcumin analogs". Thesis, 2014. http://ndltd.ncl.edu.tw/handle/4qcnpg.
Texto completo da fonte中國醫藥大學
藥物化學研究所碩士班
102
Curcumin is an orange-yellow crystalline powder obtained from rhizome of Curcuma longa Linn (Zingiberaceae). Curcumin has a variety of biological activities. Within the past 30 years, cancer is a leading cause of death in Taiwan. Therefore, developing new anticancer drugs is in an urgent need. In the recent years, there are many studies reported that curcumin displayed anticancer activity. In this study, several curcumin analogs were synthesized and evaluated for anticancer activities. We expected to find a better anticancer agent than curcumin. This study is focus on synthesis of two types of curcumin analogs, which are represented as WC and S series. WC series was used the catecol as a starting material, which was first cyclized with various ketones under P2O5 catalyst to obtain benzodioxole derivatives. The benzodioxoles were reacted with NBS, and then went forward the Grignard reaction to yield the corresponding aldehydes. Finally, the aldehydes were condensed with acetylacetone to give the corresponding curcumin analogs WC4a~4h. As synthetic curcumin analogs S series, bezaldehyde or piperonal was first reacted with acetone under strong base, and then reacted again with the substituted aldehydes to obtain the corresponding curcumin analogs S2a~2h . The anticancer activities of these curcumin analogs WC4a~4h and S2a~2h were evaluated on Hep3B, H460, A498 and COLO-205 human cancer cell lines. The results showed that the S2a exhibited the most potent cytotoxicity against A498 cells with IC50 value 16.8 μM. Moreover, the preliminary mechanism studies indicated that S2a could induce apoptosis in A498 cells by both the mitochondrial pathway and death receptor pathway.
"In vitro studies using curcumin and curcumin analogues as candidate mitochondria-targeting anticancer agents affecting colon cancer cells". Thesis, 2014. http://hdl.handle.net/10388/ETD-2014-09-1714.
Texto completo da fonteKUO, YU-LING, e 郭育伶. "Preparation and characterization of zein-curcumin analogue nanoparticles with α-glucosidase and xanthine oxidase inhibitory activities". Thesis, 2019. http://ndltd.ncl.edu.tw/handle/7kg9yk.
Texto completo da fonte輔仁大學
食品科學系碩士班
107
Curcumin (CM) is a natural lipophilic polyphenol with a variety of pharmacological properties, that provide antioxidizing, antiinflammatory, antimicrobial, antiviral, antirheumatic, anticancer, and neuroprotective effects. However, curcumin is limited in terms of water-solubility, and curcumin analogues as well. Researchers have recently begun using biopolymers to encapsulate hydrophobic compounds in order to improve their bioavailability. The objective of this study was to evaluate the feasibility of using zein nanoparticles as an oral delivery vehicle for curcumin and its analogues. The investigation centered on the radical scavenging activities of ABTS and DPPH as well as the inhibition of α-glucosidase and xanthine oxidase by curcumin and its analogues, including CM-1, CM-2, CM-A, CM-F, and tetrahydrocurcumin. Fourier transform infrared spectroscopy was used to identify and characterize zein-curcumin analogues nanoparticles. All of the analogues except CM-1 presented ABTS radical scavenging activity on par with or superior to that of vitamin E. The α-glucosidase inhibitory activity of the compounds in this study was as follows: CM-F > CM > CM-A > CM-1. The α-glucosidase inhibitory effects of curcumin and its analogues were superior to those of quercetin. Furthermore, only CM-F had a good xanthine oxidase inhibitory activity (IC50 = 2.05 ± 0.15 μM), suggesting a better inhibition than that of allopurinol (IC50 = 12.04 ± 1.54 μM). Amide I, amide II and amide III of zein were observed in the nanoparticles with the peak positions either existed or slightly shifted. The main peaks of all compounds themselves were also occurred or shifted in nanoparticles, indicating that partial hydrogen bonds occurred between the hydrophobic region of zein and compounds. The resulting nanoparticles without surfactant were spherical, small (mean particle size ≈ 125-150 nm), and had a narrow size distribution (polydispersity index < 0.4). Additionally, the encapsulated compounds were in an amorphous as detected by differential scanning calorimetry. These results demonstrate that zein can indeed be used as a carrier of curcumin and its analogues. Especially, zein-CM-F nanoparticle is the most potential inhibitors using in the treatment of gout and diabetes.
Li, Cho-Han, e 李卓涵. "Studies on Curcumin and its analogs on anti-metastatic activities of human fibrosarcoma cells (HT-1080)". Thesis, 2009. http://ndltd.ncl.edu.tw/handle/00651349802485252607.
Texto completo da fonte臺北醫學大學
生藥學研究所
97
Curcumin, a yellowish pigment existed in turmeric plant has been shown to exhibit numerous biological properties, such as anti-inflammation, antioxidation, anti-invasion, and antimetastatic activity. Chemical modifications of curcumin have been studied intensively in an attempt to find an analog with similar but enhanced biological activities of curcumin. In literatures, matrix metalloproteinases (MMPs) and urokinase plasminogen activator (uPA) played important roles in cancer cell invasion by hydrolysing extracellular matrix (ECM). In this study, curcumin and 23 novel analogs were used to screen for inhibition of matrix metalloproteinase-9 (MMP-9) activities, protein and gene expression of highly metastatic HT-1080 human fibrosarcoma cells to explore the mechanisms of action. All tested compounds, except analog 24 and analog 31 at concentration of 2.5 μM showed no cytotoxic activities at 5 μM. The analog 2 (six methoxy substitutes in phenyl groups) and analog 7 (three hydroxyl and one methoxyl substitutes in phenyl groups) showed higher MMP-9 inhibitory activities than curcumin did at 5 μM in gelatin zymography analysis. We comparatively examined the influence of analog 2, 7, 24 (three hydroxyl substitutes in phenyl groups), and 31(two hydroxyl and two methoxyl substitutes in phenyl groups) on the expression of MMP-9 of HT-1080 cells at concentration of 2.5 μM. Analog 2, 7, 24 and 31 suppressed the gene expression of MMP-9 as the results of RT-PCR assay and Western blot assay, and decreased their corresponding activities in HT-1080 cells revealed by gelatin zymography assay, MMP-9 activity ELISA and fibrin zymography assay which resulted in inhibition of HT-1080 cell invasion and migration differentially. All in all, analog 2 and 7 showed higher anti-metastatic activities than analog 24 and analog 31 did. Heme oxygenase 1(HO-1), a stress-responsive enzyme, which was found to correlate with production of reactive oxygen species (ROS), suggesting a causative relationship on MMP inhibition. Therefore, the effect of curcumin and analog 2, 7, 24 and 31 on HO-1 protein expression were also studied. Interestingly, exposure to curcumin, analog 2 and 31 treatment maximally induce HO-1 protein expression in HT-1080 cells, however, analog 7 and 24 were less apparently. These data suggested that the inhibitory effects of curcumin and analog 2, 7, 24 and 31 on MMP-9 gene expression and uPA activity was closely related to tumor invasion and migration in vitro. Furthermore, analog 2 showed highly MMP-9 inhibitory activity which possibly involved mechanisms related to its ability to induce HO-1 to suppress PMA-induced ROS, which can activate MMP-9 gene expression. In summary, these data demonstrated that analog 2, 7, 24 and 31 show higher anti-metastasis potency than curcumin by the differentially down-regulation of MMP-9 and uPA.
Chiang, Ting-Hsuan, e 江庭萱. "Studies on curcumin and its analogs on apoptotic activities in human breast adenocarcinoma cells (MCF-7 and MDA-MB-231)". Thesis, 2010. http://ndltd.ncl.edu.tw/handle/57106318055398201666.
Texto completo da fonte臺北醫學大學
生藥學研究所
98
Curcumin is the primary bioactive constituent of turmeric, which is an herbal medicine used in Asia for a long time. It has been shown to possess anti-inflammatory, antioxidant, anti-metastatic, and apoptosis- induced properties. In this study, curcumin and 23 different kinds of curcumin analogs were evaluated for cytotoxicity effects on two breast cancer cell lines—MCF-7 and MDA-MB-231. According to the results of cell viability assay, analog 2, 6 and 85 showed stronger growth inhibition activities in both MCF-7 and MDA-MB-231 cell lines than curcumin under concentration of 5 μM and were selected as test candidates. The analog 2, 6, and 85 together with negative control of analog 9 with four to six methoxyl substituents in the phenyl groups were chosen to compare structure-activity relationships. Apoptosis activity was examined by Annexin-V-FITC fluorescence stain by a confocal microscopy under 5 μM treatments. Among them, analog 6 was demonstrated to effectively induce apoptosis activity. By flow cytometry analysis for Annexin-V-FITC/PI fluorescence under concentration of 15 μM treatment for 24 hours, analog 6 showed almost 100% apoptosis in both MCF-7 and MDA-MB-231 cell lines; analog 2 induced 80% apoptosis in MDA-MB-231 cell line; analog 85 exhibited 80% apoptosis in MCF-7 cell line. Cell cycle distribution was arrested by curcumin, analog 2, 6, and 85 in G2/M phase in MCF-7 cells. In MDA-MB-231 cells, curcumin, analog 2, and 85 caused cell cycle arrest in G2/M phase; analog 6 caused cell cycle arrest in G0/G1 phase. Analog 9 showed no influence on cell cycle distribution in both cell lines. To study the mechanism of apoptosis induction by analog 6 and curcumin, cellular reactive oxygen species (ROS) produced levels were detected. It was found that curcumin and analog 6 elevated ROS levels in MDA-MB-231 cells after being treated with 30 minutes. Furthermore, curcumin and analog 6 for 24-h treatments induced heme oxygenase-1 (HO-1) protein expressions in both cell lines. Analog 6 increased MDA-MB-231 cells caspase-9 and caspase-3 actived form expression. We concluded that analog 6 induce MDA-MB-231 cells undergo apoptosis through intrinsic pathway. In addition, according to gelatin zymograhy and wound healing assay, analog 6 inhibits MDA-MB-231 cells migration through suppressing MMP-9 activity.
Huang, Yu-Wei, e 黃昱瑋. "Study on the effects of curcumin and its analogs on the protection of hydrogen peroxide-treated human immortalized keratinocyte cell line (HaCaT)". Thesis, 2014. http://ndltd.ncl.edu.tw/handle/gbbegy.
Texto completo da fonte臺北醫學大學
生藥學研究所
102
Hydrogen peroxide can produce large amounts of intracellular reactive oxygen species (reactive oxygen species, ROS) which can cause oxidative stress in cells. Many diseases and skin aging are associated with oxidative stress in cells. To find out which drug can reduce intracellular oxidative stress, hydrogen peroxide is used to treat cells for drug screenings. Curcumin, a polyphenol in turmeric, it has been reported to have various biological activities. In this study, we used curcumin and its analogs as materials to find out the protective activities against hydrogen peroxide-induced oxidative stress in HaCaT cells and the possible mechanisms. In the cell viability tests, it was found that the pretreatment of samples 7 and 24 at 5 μM for 2.5-h have significant protection against 150 μM hydrogen peroxide-induced apoptosis in human keratinocyte cell line (HaCaT cells). Using the flow cytometric analysis, it was found that the pretrement of samples 7 and 24 at 5 μM for 2.5-h could reduce the levels of early stage apoptosis in HaCaT cells. The pretreatment of samples 7 and 24 also reduce the expressions of p53 tumor suppressor protein, and reverse the loss of mitochondrial membrane potentials in HaCaT cells. The c-jun, c-fos, and iNOS mRNA expressions in HaCaT cells were also significantly decreased after being pretreated with samples 7 or 24. It was also found that the pretreatments of samples 7 and 24 at 5 μM for 2.5-h could significantly reduce intracellular ROS levels elevated by 150 μM hydrogen peroxide treatments. Using western blotting and enhanced chemiluminescence (ECL) system, it was found that the pretreatments of samples 7 and 24 could significantly induce heme oxygenase-1 (HO-1) expressions and glutathione peroxidase (GPx) activity in HaCaT cells. These results indicate that curcumin analogs, samples 7 and 24, show significantly protective effects against hydrogen peroxide-induced oxidative stress in HaCaT cells which may have protentials in cosmetics to develop anti-aging for skin cares.