Academic literature on the topic 'Antiproliferative activities'

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Journal articles on the topic "Antiproliferative activities"

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Zhou, Lin, Xiaohui Lin, Arshad Mehmood Abbasi, and Bisheng Zheng. "Phytochemical Contents and Antioxidant and Antiproliferative Activities of Selected Black and White Sesame Seeds." BioMed Research International 2016 (2016): 1–9. http://dx.doi.org/10.1155/2016/8495630.

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Sesame (Sesamum indicumL.) seeds are popular nutritional food but with limited knowledge about their antioxidant and antiproliferative activities of various varieties. Phytochemical profiles and antioxidant and antiproliferative activities of six varieties of sesame (Sesamum indicumL.) seeds were studied.Fenheizhi3(black) cultivar exhibited the maximum contents of total phenolics and lignans and values of total oxygen radical absorbance capacity (ORAC) and antiproliferative activity (EC50) against HepG2 cells. Bound ORAC values showed strong associations with bound phenolics contents (r=0.976,p<0.01); in bound phenolic extracts, EC50values showed strong negative associations with phenolic contents (r=-0.869,p<0.05) and ORAC values (r=-0.918,p<0.01). Moreover, the contents of free phenolics were higher than that of the bound phenolics, and the three black sesame seeds generally depicted higher total phenolics compared to the three white varieties. The antioxidant (ORAC values) and antiproliferation activities of six sesame seeds were both associated with contents of bound phenolics (r>0.8,p<0.05). Interestingly, nonlignan components in bound phenolics contributed to the antioxidant and antiproliferative activities. This study suggested thatFenheizhi3variety is superior to the other five varieties as antioxidant supplements.
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Liu, Ming, Xin Qi Li, Courtney Weber, Chang Yong Lee, Janice Brown, and Rui Hai Liu. "Antioxidant and Antiproliferative Activities of Raspberries." Journal of Agricultural and Food Chemistry 50, no. 10 (May 2002): 2926–30. http://dx.doi.org/10.1021/jf0111209.

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Xu, XiXi, Tristan Rawling, Ariane Roseblade, Roger Bishop, and Alison T. Ung. "Antiproliferative activities of alkaloid-like compounds." MedChemComm 8, no. 11 (2017): 2105–14. http://dx.doi.org/10.1039/c7md00435d.

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Meyers, Katherine J., Christopher B. Watkins, Marvin P. Pritts, and Rui Hai Liu. "Antioxidant and Antiproliferative Activities of Strawberries." Journal of Agricultural and Food Chemistry 51, no. 23 (November 2003): 6887–92. http://dx.doi.org/10.1021/jf034506n.

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Huang, Hung-Tse, Chia-Ching Liaw, Yu-Chi Lin, Geng-You Liao, Chih-Hua Chao, Chun-Tang Chiou, Yao-Haur Kuo, and Kung-Ta Lee. "New Diterpenoids from Mesona procumbens with Antiproliferative Activities Modulate Cell Cycle Arrest and Apoptosis in Human Leukemia Cancer Cells." Pharmaceuticals 14, no. 11 (October 29, 2021): 1108. http://dx.doi.org/10.3390/ph14111108.

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Mesona procumbens is a popular material used in foods and herbal medicines in Asia for clearing heat and resolving toxins. However, phytochemical research on this plant is very rare. In this study, eleven new diterpenoids, mesonols A-K (1–11), comprising seven ent-kauranes, three ent-atisanes, and one sarcopetalane, were isolated from its methanolic extract. Structural elucidation of compounds 1–11 was performed by spectroscopic methods, especially 2D NMR, HRESIMS, and X-ray crystallographic analysis. All isolates were assessed for their antiproliferative activity, and compounds 1–4 showed potential antiproliferative activities against A549, Hep-3B, PC-3, HT29, and U937 cancer cells, with IC50 values ranging from 1.97 to 19.86 µM. The most active compounds, 1 and 2, were selected for further investigation of their effects on cell cycle progression, apoptosis, and ROS generation in U937 human leukemia cancer cells. Interestingly, it was found that compounds 1 and 2 induced antiproliferative effects in U937 cells through different mechanisms. Compound 1 caused cell cycle arrest at the G2/M phase and subsequent cell death in a dose- and time-dependent manner. However, 2-mediated antiproliferation of U937 cells triggered ROS-mediated mitochondrial-dependent apoptosis. These results provide insight into the molecular mechanism involved in the antiproliferative activities of compounds 1 and 2 in U937 cells. Altogether, the study showed that new diterpenoid compounds 1 and 2 from M. procumbens are potent and promising anticancer agents.
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Zhou, Mingming, Pei Chen, Yuan Lin, Shengzuo Fang, and Xulan Shang. "A Comprehensive Assessment of Bioactive Metabolites, Antioxidant and Antiproliferative Activities of Cyclocarya paliurus (Batal.) Iljinskaja Leaves." Forests 10, no. 8 (July 26, 2019): 625. http://dx.doi.org/10.3390/f10080625.

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Cyclocarya paliurus (Batal.) Iljinskaja is an indigenous and multifunction tree species in China, but it is mainly used in pharmaceutical and nutraceutical ingredients. To make a comprehensive evaluation on its bioactive metabolites, antioxidant and antitumor potentials of C. paliurus leaves, the leaf samples were collected from 15 geographic locations (natural populations) throughout its distribution areas. High-performance liquid chromatography (HPLC) and colorimetric methods were used to detect the contents of bioactive metabolites. The antioxidant activity was evaluated by 2,2′-diphenyl-1-picrylhydrazyl (DPPH), 2,2-azino-bis (3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) and reducing power assays. The antiproliferative activity on different cancer cell types was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. Contents of bioactive metabolites, and antioxidant and antiproliferative activities in the extracts were significantly affected by solvent and population. In most cases, the contents of flavonoids and triterpenoids, and the antioxidant and antiproliferative activities in the ethanol extracts were higher than the water extracts. The best scavenging capacity of DPPH (IC50 = 0.34 mg/mL) and ABTS (IC50 = 0.50 mg/mL) radical occurred in the ethanol extracts of S15 and S7 population respectively, while the strongest reducing power (EC50 = 0.71 mg/mL) was achieved in the ethanol extracts of S14 population. The antiproliferation effects of C. paliurus extracts on cancer cells varied with different cell types. The HeLa cell was the most sensitive to C. paliurus extracts, and their IC50 values of the ethanol extracts varied from 0.13 to 0.42 mg/mL among C. paliurus populations. Redundancy analysis showed that total polyphenol had the greatest contribution to the antioxidant activity, but total flavonoid was mostly responsible for the antiproliferation effects. These results would provide important scientific evidences not only for developing C. paliurus as a potent antioxidant and antitumor reagent, but also for obtaining the higher yield of bioactive compounds in the C. paliurus plantation.
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Chang, Tien-Ning, Guan-Jhong Huang, Yu-Lin Ho, Shyh-Shyun Huang, Heng-Yuan Chang, and Yuan-Shiun Chang. "Antioxidant and Antiproliferative Activities of Crossostephium chinensis (L.) Makino." American Journal of Chinese Medicine 37, no. 04 (January 2009): 797–814. http://dx.doi.org/10.1142/s0192415x09007259.

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Crossostephium chinensis (L.) (CC) Makino is a common traditional Chinese medicinal plant used to dehumidify and cure rheumatism and arthralgia. The water and methanol extracts of C. chinensis (CCW and CCM) were evaluated for their antioxidant and antiproliferative activities. The antioxidant activities of CC were evaluated by using ABTS radical scavenging, DPPH radical scavenging, nitric oxide scavenging and superoxide scavenging methods. Iron chelating activity, lipid peroxidation, total polyphenol contents, total flavonoid contents and total flavonol contents were also detected. In all the tested models, both CCW and CCM showed their ability to scavenge the free radicals in a does-dependent manner. CCW had higher antioxidant and antiproliferative activities than CCM. In LC-MS-MS analysis, the chromatograms of CCW with good antioxidant activities were established. Rutin might be an important bioactive compound in CCW. The antiproliferative activities of CCW and CCM were also studied in vitro by using human hepatoma HepG2 cells. CCW exhibited good antiproliferative activity. These results indicated that CCW might be used as a potential source of natural antioxidants and as an anti-tumor agent.
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Vollár, Martin, András Gyovai, Péter Szűcs, István Zupkó, Marianna Marschall, Boglárka Csupor-Löffler, Péter Bérdi, et al. "Antiproliferative and Antimicrobial Activities of Selected Bryophytes." Molecules 23, no. 7 (June 23, 2018): 1520. http://dx.doi.org/10.3390/molecules23071520.

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Negi, Arvind Singh, Suaib Luqman, Suchita Srivastava, Vinay Krishna, Namita Gupta, and Mahendra Pandurang Darokar. "Antiproliferative and antioxidant activities ofJuglans regiafruit extracts." Pharmaceutical Biology 49, no. 6 (May 9, 2011): 669–73. http://dx.doi.org/10.3109/13880209.2010.537666.

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B. Ng, T., and J. H. Wong. "Fungal Proteins with Antiproliferative and Anticancer Activities." Protein & Peptide Letters 20, no. 4 (February 1, 2013): 433–38. http://dx.doi.org/10.2174/092986613805290363.

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Dissertations / Theses on the topic "Antiproliferative activities"

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Oliveira, Marcelio. "Synthesis and Evaluation of N6,5'-Bis-Ureido-5'-Amino-5'-Deoxyadenosine Derivatives: Novel Nucleosides with Antiproliferative and Protein Kinase Binding Activities." Diss., CLICK HERE for online access, 2009. http://contentdm.lib.byu.edu/ETD/image/etd3231.pdf.

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SAAB, Antoine. "Phytochemical analysis, antiproliferative against k562 humam chronic myelogenus leukemia, antiviral and hypoglycaemic activities of cedrus species and medicinal plants native from Libanon." Doctoral thesis, Università degli studi di Ferrara, 2011. http://hdl.handle.net/11392/2388806.

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There are four kinds of Cedar, three of them naturally present in the Mediterranean Sea region: Cedrus libani, in Lebanon, Syria and Turky, Cedrus atlantica in Algeria and Morocco, Cedrus brevifolia in Cyprus Island While Cedrus deodara in Himalaya Mountains . The wood essential oils of C. libani, C .atalantica and C. deodara inhibited the proliferation of k 562 cell line with IC50 Value of 23.38, 59.37 and 37.09 µg.ml-1 respectively. Meanwhile Cedrus libani wood oils showed a percentage of erythroide differentiation of 15% at the concentration of 5µg.ml-1another side Cedrus deodara wood oil was found a percentage of erythroide differentiation of 20% at the concentration 25µg.ml-1 and Cedrus atlantica wood oils indicated a percentage of erythroide differentiation of 12% at concentration 10µg.ml-1 The essential oils obtained from different officinal plants of Lebanon, belonging to the Magnoliophyta division, have been tested for their antiproliferative activity on humanerythroleukemic K562 cells. Satureja montana showed the most interesting biological activity in inhibiting the cell growth and inducing erythroid differentiation of K562 cells The essential oil of Satureja montana was therefore analyzed using a GC/MS (gas chromatography/mass spectrometry) system in order to identify the major constituents and compare them with analysis performed on Satureja hortensis. The major constituent of Satureja hortensis being carvacrol (50.61%) and that of Satureja montana being α-terpineol (12.66%). Satureja Montana essential oil displayed different natural derivatives characterized by higher activity than those present in Satureja hortensis. The common active principles are α-pinene, γ-terpinene, 4-terpineol, α-terpineol, τ-cadinene, τ-cadinol and caryophyllene. Both caryophyllene and α-terpineol showed important antiproliferative effects on K562 cells.
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Soares, Sarah Aparecida. "Isolamento biomonitorado de substâncias ativas de Croton pallidulus var. pallidulus (Euphorbiaceae)." Universidade de São Paulo, 2013. http://www.teses.usp.br/teses/disponiveis/41/41132/tde-31032014-104241/.

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Croton (Euphorbiaceae), é um gênero promissor para pesquisa de compostos bioativos, tanto pela variedade de compostos químicos encontrados, quanto pela diversidade de uso na medicina tradicional/popular. Estudos farmacológicos comprovaram atividades antimicrobianas, antivirais, anti-inflamatórias, antioxidantes e citotóxicas. Neste trabalho, foram obtidos extratos fracionados em Soxhlet (hexano, diclorometano, acetato de etila e metanol) de folhas e caules de C. pallidulus Baill var. pallidulus (Baill.) L.B. Smith & S.F. Smith. Esses extratos foram avaliados quanto às atividades 1) antibacteriana pelo método de microdiluição em caldo, utilizando Staphylococcus aureus - cepas sensível e resistente à vancomicina, Pseudomonas aeruginosa, Escherichia coli e Salmonella choleraesuis; 2) antioxidante (sequestro do radical livre DPPH); e quanto à toxicidade frente à Artemia salina. A fração mais ativa neste último ensaio foi selecionada para a avaliação da atividade citotóxica utilizando as células de sarcoma uterino humano. Os fenóis totais, e flavonóis e flavonas totais foram quantificados por métodos colorimétricos. O fracionamento dos extratos hexânico e diclorometânico foi feito por cromatografia em coluna de sílica, enquanto o dos extratos de acetato de etila e metanol, em coluna de PVPP. O isolamento das substâncias das frações ativas nos ensaios de atividade antibacteriana (S. aureus - sensível) e de toxicidade frente à A. salina foi realizado por CLAE semipreparativo. O teor de fenóis totais de C. pallidulus var. pallidulus foi de 1,95 g EAG/100g MS e de flavonóis e flavonas totais foi de 0,56 g EQ/100g MS. Todos os extratos apresentaram atividade contra S. aureus (sensível e resistente), com CBM de 2048 mg/L, exceto o extrato metanólico que apresentou atividade apenas contra S. aureus (sensível). Nenhum extrato apresentou atividade contra as demais cepas. As frações FH-5A - hexano (CBM de 256mg/L) e FA-7 - acetato de etila (CBM de 1024mg/L) foram as que apresentaram maior atividade antibacteriana. A fração FH-5A foi separada em coluna de sílica, e suas subfrações apresentaram atividades antibacterianas menores que a fração que lhe deu origem. Das sete substâncias majoritárias isoladas da fração FA-7, nenhuma apresentou atividade antibacteriana. Seis delas são flavonoides: três C-glicosídeos de apigenina, um O-glucosídeo de campferol, um O-galactosídeo de isoramnetina e um O-rutinosídeo de isoraminetina. Apenas o extrato diclorometânico apresentou atividade no ensaio de toxicidade frente à A. salina, com CL50 de 385mg/L. A fração com maior toxicidade foi a FD-4A, com CL50 de 101mg/L. As substâncias mais abundantes nesta fração foram isoladas e identificadas como 8,9-secocauranos, derivados da kongensina F. Quanto a atividade citotóxica, a atividade de FD-4A foi três vezes maior que a atividade do extrato diclorometânico. Os extratos de acetato de etila e de metanol apresentaram os maiores valores de atividade antioxidante: 12,11 e 11,77 gEQ/100g, respectivamente. Verificou-se que os flavonoides foram as substâncias fenólicas que mais influenciaram na atividade antioxidante das frações dos extratos de acetato de etila e de metanol. Com esses resultados verifica-se que C. pallidulus var. pallidulus possui ação antibacteriana, citotóxica e antioxidante, sendo uma potencial fonte para novos fármacos para tratamento de doenças infecciosas e câncer. Conseguiu-se também isolar três 8,9-secocauranos, derivados da kongensina F, que aparentemente não haviam ainda sido descritos
Croton (Euphorbiaceae), is a promising genre for investigation of bioactive compounds, both for the variety of compouds, as for the diversity of use in traditional medicine. Pharmacological studies have demonstrated antimicrobial, antiviral, anti-inflammatory, cytotoxic, and antioxidant activities. In this study, fractionated extracts of leaves and stems of C. pallidulus Baill var. pallidulus (Baill.) L.B. S.F. Smith & Smith were obtained throught Soxhlet (hexane, dichloromethane, ethyl acetate and methanol). The following activities of these extracts were tested: 1) antibacterial activity, through microbroth dilution assay using: Staphylococcus aureus - sensitive and vancomycin-resistant strains, Pseudomonas aeruginosa, Escherichia coli and Salmonella choleraesuis; 2) antioxidant activity (free radical DPPH scavenging) and Artemia salina toxicity evaluation. The most active fraction in the latter test was selected to evaluate the cytotoxic activity using human uterine sarcoma cells. The total phenols, and total flavonols and flavones were quantified by colorimetric methods. The fractionation of hexane and dichloromethane extracts was done through silica column chromatography, while PVPP column was used for the ethyl acetate and methanol extracts. The isolation of the active fractions major compounds in the antibacterial activity (S. aureus - sensitive) and A. saline toxicity assays were performed by semipreparative HPLC. The total phenolic content of C. pallidulus var. pallidulus was 1.95 g GAE/100g DM and total flavonols and flavones was 0.56 g QE/100g MS. All extracts showed activity against S. aureus (sensitive and resistant), with MBC of 2048 mg/L, except for the methanol extract, which showed activity only against S. aureus (sensitive). Extracts showed no activity against the other strains. Fractions FH-5A-hexane (MBC: 256mg/L) and FA-7-ethyl acetate (MBC: 1024mg/L) showed the highest antibacterial activity. The fraction FH-5A was separated on a silica column, and its subfractions showed smaller antibacterial activity than FH-5A. The seven major compounds isolated from the FA-7 fraction, showed no antibacterial activity. Six of them are flavonoids, three apigenin C-glycosides, one kaempferol O-glucoside, one isorhamnetin O-galactoside and one isorhamnetin O-rutinoside. Only the dichloromethane extract showed activity in the A. salina toxicity assay, LC50: 385mg/L. The fraction with the highest toxicity was the FD-4A, LC50: 101mg/L. The most abundant substances in this fraction were isolated and identified as 8,9 - secokauranes derived from kongensin F. As for the cytotoxic activity, the FD-4A activity was three times higher than the dichloromethane extract activity. The extracts of ethyl acetate and methanol showed the highest antioxidant activity: 12.11 and 11.77 gQE/100g, respectively. It was observed that flavonoids were the phenolic substances that most influenced the antioxidant activity of the fractions of the ethyl acetate and methanol extracts. With these results we suggest that C. pallidulus var. pallidulus has antibacterial activity, cytotoxic and antioxidant properties, being a potential source of new drugs for treatment of infectious diseases and cancer. We also isolated three 8,9-secokauranes derived from kongensin F, which apparently had not been described yet
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Abi, Aad Elizabeth. "Impact de la Détente Instantanée Contrôlée (DIC) sur l’extraction des molécules bioactives de rhizomes de Rheum ribes L." Electronic Thesis or Diss., La Rochelle, 2023. http://www.theses.fr/2023LAROS008.

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Rheum ribes L. (la rhubarbe) est l'une des plantes médicinales méditerranéennes les plus importantes. La préparation des décoctions aqueuses des rhizomes de cette plante est devenue une pratique courante chez les patients souffrant de diverses maladies. La Détente Instantanée Contrôlée (DIC) est un traitement à haute température et à courte durée (HTST high-temperature/short-time) suivi d'une chute brutale de pression vers le vide (Pression absolue de 5 kPa environ). Le traitement DIC induit l’expansion et réduit la tortuosité de la matrice traitée, et assure ainsi une meilleure diffusivité des solvants d’extraction et par la suite une plus grande disponibilité des molécules actives. D’une part, nos travaux de recherche ont visé l’identification de l’impact du traitement par DIC des rhizomes d’une espèce libanaise de R. ribes L. Les évaluations ont été basées sur les teneurs en polyphénols totaux (TPC) et en flavonoïdes (TFC) ainsi que sur les pouvoirs antioxydants des extraits aqueux de rhizomes traités. Les résultats ont montré qu’une corrélation négative existe entre la pression de vapeur saturée appliquée et les valeurs de TPC, TFC et les activités antioxydantes des échantillons traités. Cependant, il n'y avait pas d'influence significative du temps de traitement par DIC sur les variables réponses. A ces deux facteurs opératoires de la DIC, pression et temps de traitement, s’ajoute la teneur en eau (W) des rhizomes. Les résultats ont montré qu’une augmentation ne provoque pas des meilleurs rendements en composés phénoliques. D’autre part, ce travail inclut également l’étude de l’impact du traitement par DIC sur les activités biologiques (effets antibactériens et antiprolifératifs) des extraits de rhizomes. Les résultats ont mis en évidence que les extraits aqueux de rhizomes traités par DIC présentent, aux concentrations testées, de très faibles pouvoirs antibactériens sur E. coli et S. aureus, avec des résultats légèrement supérieurs au niveau de l’inhibition de la croissance de S. aureus. En ce qui concerne le test de viabilité des cellules cancéreuses du mélanome, les résultats ont montré que le traitement par DIC a un impact positif sur le pouvoir antiprolifératif des échantillons traités en comparaison avec une matrice non-traitée par DIC et extraite par voie aqueuse. En particulier, deux échantillons parmi ceux testés, ont enregistré un pouvoir antiprolifératif de 60%. Les dosages par HPLC et UHPLC ont révélé la présence de trois anthraquinones (l’émodine, le chrysophanol et le physcion) dans les extraits de rhizomes ainsi qu’une vingtaine de composés de la famille des flavonoïdes. Cependant, les quantités d’anthraquinones détectés ne sont pas significativement plus élevées dans les extraits traités par DIC que dans ceux non-traités. Finalement, il a été constaté que la teneur phénolique totale d'un échantillon aqueux traité avec les paramètres optimaux de la DIC est égale à celle d'un point hydroalcoolique non traité. Des expérimentations supplémentaires seront nécessaires pour la validation de ce résultat
Rheum ribes L. (rhubarb) is one of the most important Mediterranean medicinal plants. Preparing its rhizomes’ aqueous decoctions has become common among patients suffering from various diseases. Instant Controlled Pressure Drop (DIC) is a High-Temperature Short-Time treatment (HTST) followed by an abrupt pressure drop towards the vacuum (approximately 5 kPa). This technology increases the expansion and reduces the tortuosity of the treated matrix to ensure better diffusivity of the extraction solvents and greater availability of the active molecules. On the one hand, our research aimed at the impact of DIC treatment on the rhizomes of a Lebanese species of R. ribes L. The evaluations were based on the contents of total phenolics (TPC) and flavonoids (TFC) as well as the antioxidant capacities of aqueous extracts of the treated rhizomes. The results showed a negative correlation between the saturated steam pressure applied and the values of TPC, TFC, and the antioxidant activities of the samples. However, DIC treatment time had no significant influence on the response variables. In addition to these two DIC operating factors (pressure and treatment time), the effect of the rhizomes water content (W) was also studied. The results showed that the increase of “W” does not lead to better yields of phenolic compounds. On the other hand, this study presents the impact of DIC treatment on the biological activities (antibacterial and antiproliferative effects) of rhizome extracts. The results revealed that the aqueous extracts of DIC-treated rhizomes show weak antibacterial powers on E. coli and S. aureus, with slightly superior results in inhibiting the growth of S. aureus. Regarding the viability test of melanoma cancer cells, the results showed that the DIC treatment positively impacts the antiproliferative power of the treated samples compared with the untreated point (aqueous MP). In particular, two samples among those tested recorded an antiproliferative power of 60%. The HPLC and UHPLC assays revealed the presence of three anthraquinones (emodin, chrysophanol, and physcion) in the rhizome extracts and about twenty compounds from the flavonoid family. However, the amounts of anthraquinones detected are not significantly higher in the extracts treated with DIC than in the untreated ones. Finally, it was found that the total phenolic content of an aqueous sample treated with the optimal DIC parameters is equal to that of an untreated hydroalcoholic sample. Further experiments will be necessary to validate this result
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BASTIAS, VENEGAS JORGE EDUARDO ROMILIO. "Activites antiproliferative et antitumorale d'un dextrane fonctionalise (cmdbj) sur les cellules de melanome 1205 l-u." Paris 13, 1999. http://www.theses.fr/1999PA132034.

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L'etude des effets antiproliferatif et antitumoral du cmdbj sur la lignee de cellule de melanome humaine 1205 l-u, nous a permis de mettre en evidence l'effet inhibiteur d'un derive du dextrane : le carboxy-methyl-dextrane-benzylamide jorge. L'effet du cmdbj a ete aussi teste par comptage cellulaire dans d'autres lignees tumorales comme la lignee mda-mb 231, et dans des lignee pretumorales comme hbl 100. En comparant les inhibitions obtenues dans les differentes lignees, 1205 l-u presente un plus haut pourcentage d'inhibition que les autres lignees traitees au cmdbj. Cet effet a ete demontre aussi par l'inhibition de l'incorporation de la thymidine tritiee dans l'adn des cellules de melanome 1205 l-u. La comparaison des resultats obtenus par ces deux techniques montre une homologie presque total. Cette inhibition de la proliferation cellulaire par le cmdbj est dependante de la dose et du temps du traitement. Par analyse de cytofluorometrie, le cmdbj produit un blocage partiel de la phase s du cycle cellulaire. L'effet du cmdbj sur l'activite mitogenique des milieux conditionnes des lignees cellulaires nous a permis de comparer les inhibitions de cette activite mitogenique tres importante sur les cellules tumorales 1205 l-u, les cellules pretumorales hbl 100 et les cellules endotheliales huvec. Les resultats plus surprenant sont ceux obtenus in vivo. L'effet inhibiteur du cmdbj sur la taille des tumeurs est tres significative. Quelques tumeurs ont disparus dans deux echantillons d'un groupe compose de 6 souris nude. On a mis en evidence l'effet antitumoral du cmdbj a une concentration donne (5000 ug/100 l). Il n'y a pas l'effet du cmdbj sur la taille des tumeurs implantees dans la souris athymique a 2500 g/ml. L'analyse immunohistologique des poumons des souris nude traitee a 5000 ug/100 l de cmdbj met en evidence un pouvoir antimetastasiant du cmdbj. Les poumons des souris traitees a cette dose presentent une vascularisation bien irriguee comme un poumon normal. Les poumons des souris non traitees au cmdbj presentent des regions necrosees, envahies de cellules de melanome. Finalement nous avons eu une premiere approche par bioimagerie des tumeurs de souris traitees ou non au cmdbj pour le diagnostic de melanome humain comme le 1205 l-u. Le cmdbj pourrait faire l'objet d'une utilisation clinique dans l'tritement du melanome.
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Tomasi, Sophie. "Synthèse en solution et sur support solide de dérivés de polyamines : évaluation de leur activité antiproliférative." Rennes 1, 1999. http://www.theses.fr/1999REN10100.

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Le travail presente dans ce memoire concerne la synthese par chimie en solution ou sur support solide de derives de polyamines (putrescine, spermidine, spermine, norspermine, homospermine) a visee antiproliferative. Les activites recherchees sont : la cytotoxicite, l'affinite pour l'adn, l'inhibition du transport des polyamines, l'accumulation intracellulaire via ce transport et l'antagonisme de la calmoduline. Le chapitre i est consacre a des rappels bibliographiques concernant le role des pa et les indications therapeutiques des derives de ces molecules naturelles. Dans le chapitre ii, nous presentons les syntheses realises par chimie classique en solution de derives de polyamines. Les premiers composes sont des heterocycles de taille variable qui sont couples a des di-, tri- et tetramines par une fonction amidine. Les seconds sont des derives de l'acridine qui sont relies a des pentamines asymetriques par une liaison amide ou aniline. Une etude structurale approfondie a ete realisee en rmn haut champ. Le chapitre iii concerne le developpement de strategies de synthese de derives de polyamines sur support solide. Une premiere approche a consiste a greffer une putrescine ou une spermine diprotegee sur la resine wang par un linker de type carbamate et a fonctionnaliser l'amine primaire libre. Dans la seconde approche, nous avons construit la polyamine sur support solide en utilisant la methodologie des couronnes multipin< t m> proposee par la firme chiron. Dans le dernier chapitre, nous exposons les principaux resultats pharmacologiques in vitro et in vivo obtenus par nous-meme et par l'equipe du groupe de recherche en therapeutique anticancereuse (gretac) de la faculte de medecine de rennes. Le resultat le plus important est sans doute la decouverte du premier inhibiteur du transport des polyamines plus actif que la spermine elle-meme.
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Boisbrun, Michel. "Reactions selectives de l'acide de meldrum : application a la synthese de beta-carbolines et de pyrrolo(3'4':5,6)pyrido(3,4-b)indoles a activite antiproliferative (doctorat : sciences du medicament)." Reims, 2000. http://www.theses.fr/2000REIMP205.

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Hadj, Salem Jamila. "Extraction, identification, caractérisation des activités biologiques de flavonoïdes de Nitraria retusa et synthèse de dérivés acylés de ces molécules par voie enzymatique." Thesis, Vandoeuvre-les-Nancy, INPL, 2009. http://www.theses.fr/2009INPL057N/document.

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Ce travail a consisté, dans un premier temps, à extraire et à identifier les flavonoïdes majeurs contenus dans les feuilles de Nitraria retusa et à évaluer leurs activités biologiques. Quatre flavonoïdes ont été identifiés dans les extraits et les fractions obtenus : l’isorhamnétine, l’isorhamnétine-3-O-glucoside et les deux isomères isorhamnétine-3-O-rutinoside et isorhamnétine-3-O-robinobioside. L’étude des activités biologiques des extraits et des fractions de N. retusa a permis d’établir une relation linéaire entre leur teneur en flavonoïdes et leurs activités antioxydantes et antiprolifératives, les milieux les plus riches présentant les activités les plus importantes. Ces activités dépendent également de la nature des flavonoïdes présents ; ainsi, la très forte activité d’inhibition de la xanthine oxydase relevée pour la fraction au chloroforme et sa grande capacité à piéger le radical DPPH ont été attribuées à sa teneur élevée en isorhamnétine, flavonoïde aglycone présentant une grande analogie structurale avec la quercétine, molécule bien connue pour ses activités antioxydantes. Dans un deuxième temps, l’acylation enzymatique de l’isoquercitrine, flavonoïde modèle, et de l’isorhamnétine-3-O-glucoside a été étudiée pour tenter d’améliorer leurs propriétés. L’acylation enzymatique de l’isoquercitrine par des esters éthyliques d’acides gras de différentes longueurs de chaîne, catalysée par la lipase B de Candida antarctica, a montré que les performances de la réaction sont inversement proportionnelles à la longueur de la chaîne du donneur d’acyle. Des résultats similaires ont été obtenus lors de l’acylation de l’isorhamnétine-3-O-glucoside. Les activités des esters d’isoquercitrine et d’isorhamnétine-3-O-glucoside ont été évaluées et comparées à celles des flavonoïdes non acylés. Les esters ont montré des activités antiprolifératives vis-à-vis de cellules Caco2 et d’inhibition de la xanthine oxydase plus importantes que celles des molécules d’origine. Finalement, ce travail a permis d’apporter des éléments de compréhension de la relation structure-activité de flavonoïdes et de leurs dérivés acylés
The present work firstly consisted in studying the extraction and the identification of major flavonoids contained in Nitraria retusa leaves and evaluating their biological activities. Four flavonoids were identified in extracts and fractions: isorhamnetin, isorhamnetin-3-O-glucoside and the two isomers isorhamnetin-3-O-rutinoside and isorhamnetin-3-O-robinobioside. The evaluation of the biological activities of extracts and fractions of N. retusa allowed to establish a linear relationship between their antioxidant and antiproliferative activities and their total flavonoids content, the most enriched exhibiting the highest activities. The nature of the flavonoids present in the extracts and fractions was shown to be important too. Thus, the strong xanthine oxidase inhibition activity and the high DPPH radical scavenging capacity observed for the chloroform fraction can be attributed to its high content in the aglycone flavonoid isorhamnetin, a structural analogue of quercetin which is well known for its antioxidant activities. In a second part, the enzymatic acylation of isoquercitrin as a model compound and isorhamnetin-3-O-glucoside was studied in order to improve their properties. The enzymatic acylation of isoquercitrin by fatty acid ethyl esters of different chain lengths, catalyzed by the lipase B of Candida antarctica, showed that the performance of the reaction is inversely proportional to the acyl donor chain length. Similar results were obtained when acylating the isorhamnetin-3-O-glucoside. The activities of isoquercitrin and isorhamnetin-3-O-glucoside esters were determined and compared to that of initial flavonoids. Esters exhibited higher antiproliferative towards Caco2 cells and xanthine oxidase inhibition activities than original compounds. Finally, this work led to a better understanding of the structure-activity relationship of flavonoids and their acylated derivatives
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Filleur, Fabrice. "Etude phytochimique et structure de lignoides isolés du macis de myristica argentea warb. (myristicaceae)." Limoges, 2001. http://www.theses.fr/2001LIMO301A.

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"Antioxidant and antiproliferative activities of flower tea extracts." 2007. http://library.cuhk.edu.hk/record=b5896541.

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Leung, Yu Tim.
Thesis submitted in: November 2006.
Thesis (M.Phil.)--Chinese University of Hong Kong, 2007.
Includes bibliographical references (leaves 103-128).
Abstracts in English and Chinese.
Thesis Committee --- p.i
Acknowledgements --- p.ii
Abstract --- p.iii
摘要 --- p.iv
Table of Contents --- p.v
List of Tables --- p.ix
List of Figures --- p.x
Abbreviations --- p.xiii
Chapter 1. --- Introduction
Chapter 1.1 --- Flower herbal teas --- p.1
Chapter 1.2 --- R. rugosa --- p.3
Chapter 1.2.1 --- The phytochemistry of R. rugosa --- p.3
Chapter 1.3 --- Secondary metabolites --- p.4
Chapter 1.4 --- Classification of secondary metabolites --- p.6
Chapter 1.5 --- Phenolic compounds --- p.6
Chapter 1.5.1 --- Phenylpropanoid compounds --- p.6
Chapter 1.5.2 --- Lignins --- p.7
Chapter 1.5.3 --- Coumarins --- p.7
Chapter 1.5.4 --- Stilbenes --- p.8
Chapter 1.5.5 --- Tannins --- p.8
Chapter 1.5.6 --- Flavonoids --- p.9
Chapter 1.6 --- Oxidative Stress --- p.13
Chapter 1.6.1 --- Diseases related to ROS --- p.13
Chapter 1.6.2 --- Significant chemical or biochemical conversion of ROS --- p.14
Chapter 1.6.3 --- Sources of ROS --- p.15
Chapter 1.7 --- Natural dietary antioxidants --- p.15
Chapter 1.7.1 --- Vitamin C --- p.15
Chapter 1.7.2 --- Vitamin E --- p.16
Chapter 1.7.3 --- Carotenoids --- p.16
Chapter 1.7.4 --- Phenolic compounds --- p.16
Chapter 1.8 --- Cancinogenesis --- p.17
Chapter 1.9 --- Cell cycle --- p.18
Chapter 1.9.1 --- Cell cycle of eukaryotic cells --- p.18
Chapter 1.9.2 --- Checkpoints of cell cycle --- p.18
Chapter 1.10 --- Cancer cell lines --- p.19
Chapter 1.11 --- The growth phases of cancer cell lines --- p.20
Chapter 1.12 --- Antiproliferative effects of phenolic compounds --- p.21
Chapter 1.13 --- Genotoxicity of phenolic compounds --- p.22
Chapter 1.14 --- Objectives --- p.23
Chapter 2. --- Methods and Materials
Chapter 2.1 --- Extraction of active substances --- p.40
Chapter 2.2 --- Determination of antioxidant activities TEAC assay --- p.40
Chapter 2.3 --- Determination of hydroxy 1 radical scavenging activity by the deoxyribose assay --- p.41
Chapter 2.4 --- Determination of phenolic contents by Folin´ؤCiocalteu assay --- p.43
Chapter 2.5 --- Determination of total flavonoid by aluminum chloride colorimetric method --- p.43
Chapter 2.6 --- Determination of oxidative DNA damage by comet assay --- p.44
Chapter 2.7 --- Cell lines propagation --- p.49
Chapter 2.8 --- Determination of antiproliferative activities by MTT assay (colorimetric) --- p.50
Chapter 2.9 --- Determination of antiproliferative activities by BrdU labeling assay --- p.52
Chapter 2.10 --- Cell cycle analysis by flow cytometry --- p.55
Chapter 2.11 --- Determination of genotoxicity by SOS chromotest --- p.57
Chapter 3. --- Results
Chapter 3.1 --- Dermination of antioxidant activities by TEAC assay --- p.59
Chapter 3.1.1 --- Trolox Standard Reference --- p.59
Chapter 3.1.2 --- TEAC of the seven flower extracts --- p.59
Chapter 3.2 --- Hydroxyl radical scavenging activity by deoxyribose assay --- p.60
Chapter 3.3 --- Determination of phenolic contents by Folin´ؤCiocalteu assay --- p.60
Chapter 3.4 --- Determination of total flavonoids by colorimetirc aluminium chloride assay --- p.61
Chapter 3.5 --- "The Inter-correlation between the antioxidant activities, total phenolic and flavonoid contents of flower extraction powders" --- p.61
Chapter 3.6 --- Determination of oxidative DNA damage by comet assay --- p.62
Chapter 3.7 --- Determination of antiproliferative activities by MTT assay --- p.63
Chapter 3.7.1 --- Antiporoliferative activities on HepG2 --- p.63
Chapter 3.7.2 --- Antiproliferative activities on MCF7 --- p.63
Chapter 3.7.3 --- IC50 of R. rugosa extract on both HepG2 and MCF7 --- p.64
Chapter 3.8 --- "The Inter-correlation between antioxidant activities, total phenolic contents, flavonoid contents, and the antiproliferative activities of flower extraction Powders" --- p.64
Chapter 3.9 --- Determination of DNA synthesis by BrdU labeling analysis --- p.65
Chapter 3.10 --- Cell cycle analysis by flow cytometry --- p.65
Chapter 3.11 --- Determination of genotoxicity by SOS chromotest --- p.66
Chapter 4. --- Discussions
Chapter 4.1 --- Extraction method --- p.90
Chapter 4.2 --- Comparison of TEAC of the dry flowers with other foods --- p.90
Chapter 4.3 --- Correlation between ABTS+ and hydroxyl scavenging ability of flower extraction powder --- p.91
Chapter 4.4 --- Comparison of phenolic contents of the fry flowers with other foods --- p.92
Chapter 4.5 --- Correlation between total phenolic contents and flavonoid contents of flower Eextraction powders --- p.92
Chapter 4.6 --- "Correlation between total phenolic, flavonoid content and antioxidant activities of flower extraction powders" --- p.93
Chapter 4.7 --- Factors affecting the antioxidant power besides total phenolic contents --- p.94
Chapter 4.8 --- Synergistic effect of phenolic compounds --- p.94
Chapter 4.9 --- Toxicity of drinking flower herbal tea --- p.95
Chapter 4.10 --- Recommended dose of flower herbal teas --- p.96
Chapter 4.11 --- Antiproliferative activities of flower extracts by MTT assay --- p.97
Chapter 4.12 --- Antiproliferation activities of flower extraction Powders by Brdu labeling assay --- p.98
Chapter 4.13 --- Protective effects of flower extraction powder on oxidative DNA damage determined by comet assay --- p.99
Chapter 4.14 --- Cell cycle analysis --- p.100
Chapter 4.15 --- Further Studies --- p.101
Chapter 5. --- Conclusion --- p.102
Chapter 6. --- References --- p.103
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Book chapters on the topic "Antiproliferative activities"

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Anesini, Claudia A., María Rosario Alonso, and Renzo F. Martino. "Antiproliferative and Cytotoxic Activities." In Sesquiterpene Lactones, 303–23. Cham: Springer International Publishing, 2018. http://dx.doi.org/10.1007/978-3-319-78274-4_13.

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Mumtaz, Peerzada Tajamul, Showkeen Muzamil Bashir, Muzafar Ahmad Rather, Khalid Bashir Dar, Qamar Taban, Saima Sajood, Aarif Ali, Zubair Ahmad Rather, Insha Amin, and Mashooq Ahmad Dar. "Antiproliferative and Apoptotic Activities of Natural Honey." In Therapeutic Applications of Honey and its Phytochemicals, 345–60. Singapore: Springer Singapore, 2020. http://dx.doi.org/10.1007/978-981-15-6799-5_18.

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Franěk, F., M. Strnad, L. Havlíček, and V. Siglerová. "Antiproliferative and Growth-Stimulating Activities of Synthetic Cytokinin Analogs." In Animal Cell Technology: Basic & Applied Aspects, 315–19. Dordrecht: Springer Netherlands, 2002. http://dx.doi.org/10.1007/978-94-017-0728-2_56.

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Wong, Jack Ho, Tzi Bun Ng, Evandro Fei Fang, and He-Xiang Wang. "Defense Proteins with Antiproliferative and Antimicrobial Activities from Fungi and Bacteria." In Antitumor Potential and other Emerging Medicinal Properties of Natural Compounds, 359–73. Dordrecht: Springer Netherlands, 2013. http://dx.doi.org/10.1007/978-94-007-6214-5_24.

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Ng, Tzi-Bun, Jack H. Wong, Randy C. F. Cheung, Patrick H. K. Ngai, He-Xiang Wang, Xiujuan Ye, Sze-Kwan Lam, Yau-Sang Chan, and Evandro F. Fang. "Antiproliferative Activities of Chinese Cabbage (Brassica parachinensis) Seeds." In Nuts and Seeds in Health and Disease Prevention, 317–23. Elsevier, 2011. http://dx.doi.org/10.1016/b978-0-12-375688-6.10038-6.

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Cascaes, Márcia M., Giselle M. S. P. Guilhon, Lidiane D. Nascimento, Angelo A. B. de Moraes, Sebastião G. Silva, Jorddy Neves Cruz, Oberdan O. Ferreira, Mozaniel S. Oliveira, and Eloisa H. A. Andrade. "Volatile Terpenoids of Annonaceae: Occurrence and Reported Activities." In Terpenoids: Recent Advances in Extraction, Biochemistry and Biotechnology, 105–28. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9781681089645122010007.

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Annonaceae includes 2,106 species. Some species of this family have an economic interest in the international fresh fruit market and are often used as raw materials for cosmetics, perfumes and folk medicine. The most cited species are mainly those belonging to the genera Annona, Guatteria and Xylopia. Chemical investigations indicate that the characteristic constituents of the Annonaceae are terpenoids, including mono and sesquiterpenoids, such as α-pinene, β-pinene, limonene, (E)-caryophyllene, bicyclogermacrene, caryophyllene oxide, germacrene D, spathulenol and β-elemene. Antimicrobial, antioxidant, larvicidal, antiproliferative, trypanocidal, antimalarial and anti-inflammatory effects have been described in these terpenes. This work is an overview of the chemical properties and biological effects of the volatile terpenoids from Annonaceae species.
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Peeri, Hadar, and Hinanit Koltai. "Phytocannabinoids have cytotoxic, antiproliferative, and antimigratory activities on cancer cells and cancer stem cells." In Cannabis Use, Neurobiology, Psychology, and Treatment, 555–64. Elsevier, 2023. http://dx.doi.org/10.1016/b978-0-323-89862-1.00030-1.

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lzotova, Lara, and Sidney Pestka. "Receptor binding studies." In Cytokine Molecular Biology, 89–104. Oxford University PressOxford, 2000. http://dx.doi.org/10.1093/oso/9780199638581.003.0005.

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Abstract The interferons (IFNs) are a family of proteins which elicit a multitude of cellular responses including antiviral, antiproliferative, and immunoregulatory activities. There are four classes of interferons that have been isolated and characterized (1-11). These are the leucocyte or interferon alpha (IFN-a), fibroblast or interferon beta (IFN-13), immune or interferon gamma (IFN-y), and interferon omega (IFN-w). Binding to a specific cell-surface receptor is a necessary, but not sufficient, condition for cellular activation in the case of the IFN-y system (12-16). IFN-a, IFN-13, and IFN-w share a common receptor complex that is distinct from the IFN-y receptor complex (5, 10, 11, 16, 17).
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Ayembilla, Jacob Apibilla, Phyllis Naa Yarley Otu, Eunice A. Dotse, Abigail Aning, Emmanuel Kweku Ofori, Regina Appiah-Opong, and Henry Asare-Annane. "Antioxidant and Anticancer Potential of Natural Cocoa Extract." In Technological Innovation Driving Sustainable Entrepreneurial Growth in Developing Nations, 156–75. IGI Global, 2023. http://dx.doi.org/10.4018/978-1-6684-9843-9.ch007.

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The aim of this study was to investigate antioxidant and anticancer potentials of natural cocoa extracts. Antioxidant properties of the extracts were evaluated by DPPH assay, total phenolic content by Folin-Ciocalteau and reduced glutathione content by O-phthalaldehyde assays. Antiproliferative activity was also evaluated on leukaemia and prostate cancer cell lines using MTT assay. The hydroethanolic extracts of cocoa roots and beans and aqueous cocoa leaves showed high total antioxidant activities with the root extract having the strongest scavenging effect on DPPH and the highest total phenolics content. The hydroethanolic cocoa bean crude extract showed the highest anticancer activity against LNCaP cells, whiles the ethyl acetate fraction of hydroethanolic cocoa leaf exhibited the highest anticancer against PC3. Jurkat and PC3 cells had similar susceptibilities to the natural cocoa extracts. Thus, cocoa has antioxidant and anticancer activity, and the specific bioactive compounds responsible for these activities need to be elucidated in future research.
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Bonardi, Alessandro, Claudiu T. Supuran, and Alessio Nocentini. "Phenols and Polyphenols as Carbonic Anhydrase Inhibitors." In Flavonoids and Phenolics, 330–83. BENTHAM SCIENCE PUBLISHERS, 2022. http://dx.doi.org/10.2174/9789815079098122010014.

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Thousands of phenolic derivatives have been identified in the plant kingdom, which exert crucial roles in plant physiology. Many such derivatives were shown to produce pharmacological effects in humans which address their use in medicine as antiaging, anti-inflammatory, antioxidant, antidiabetic, and antiproliferative agents among others. Numerous such pharmacological activities are likely to derive from the inhibition of human carbonic anhydrase (CAs, EC 4.2.1.1) isoforms. Phenols, in fact, are able to anchor to the zinc-bound nucleophile present in the enzyme active site, blocking the catalytic action of CAs in humans and/or encoded in various microorganisms. This chapter discusses natural, semisynthetic and synthetic phenol derivatives that exhibited a CA inhibitory action. The discussion over the CA inhibition profiles is categorized as the inhibition of human CAs and inhibition of CAs from microorganisms. Multiple types of inhibition mechanisms by phenolic derivatives are discussed according to X-ray crystallographic resolutions and in silico studies.<br>
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Conference papers on the topic "Antiproliferative activities"

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Mottaghipisheh, Javad, Márta Nové, Gabriella Spengler, Norbert Kúsz, Judit Hohmann, and Dezső Csupor. "Antiproliferative and cytotoxic activities of furocoumarins of Ducrosia anethifolia." In Fiatal Gyógynövénykutatók Fóruma. Szeged: Magyar Gyógyszerésztudományi Társaság Gyógynövény Szakosztálya, 2018. http://dx.doi.org/10.14232/fgykf.2018.b1.

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Garbuz, Olga, Ion Toderas, Ianina Ulchina, Vasile Graur, Nadejda Railean, and Аurelian Gulea. "The Antiproliferative, Antioxidant Activities and Toxicity of Mixed-Ligand Amine-Containing Copper (II) Coordination Compounds with 2-(2-Hydroxybenzylidene)-N-(Prop-2-En-1-Yl) Hydrazinecarbothioamide." In Xth International Conference of Zoologists. Institute of Zoology, Republic of Moldova, 2021. http://dx.doi.org/10.53937/icz10.2021.20.

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Five compounds 2-(2-Hydroxybenzylidene)-N-(prop-2-en1-yl)hydrazinecarbothioamide (H2L), bis[μ2-2-({2-[(prop-2-en-1-yl) carbamothioyl] hydrazinylidene}methyl) phenolatoS,N,O:O] diaquadicopper (II) nitrate (1), bis [μ2-2-({2-[(prop-2-en-1-yl) carbamothioyl] hydrazinylidene}methyl)phenolato-S,N,O:O]d iimidazoldicopper(II) nitrate (2), bis[μ2-2-({2-[(prop-2en-1-yl)carbamothioyl]-hydrazinylidene}methyl)phenolato-S,N,O:O]bis-(3,5-dibromopyridine)dicopper( II) nitrate hexahydrate (3), bis[μ2-2-({2-[(prop-2-en-1-yl)carbamothioyl]-hydrazinylidene}methyl) phenolato-S,N,O:O]bis(4-methylpyridine)dicopper(II) nitrate hexahydrate (4) were synthesized. The antiproliferative properties of these compounds towards cancer cell lines HeLa, RD and normal cell line MDCK have been investigated. The tested compounds demonstrated high antioxidant and antiproliferative, selective activities towards cancer cells. Direct toxic evaluation of compounds was performed by Daphnia magna bioassay.
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Tavares, Clint D. J., Jiney Jose, Ashwini K. Devkota, Jihyun Park, Tamer S. Kaoud, Eric V. Anslyn, and Kevin N. Dalby. "Abstract 5462: Antiproliferative and cytotoxic activities of 5-(nonyloxy)tryptamine derivatives in breast cancer cells." In Proceedings: AACR Annual Meeting 2014; April 5-9, 2014; San Diego, CA. American Association for Cancer Research, 2014. http://dx.doi.org/10.1158/1538-7445.am2014-5462.

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Larson, Mathew, Jennifer H. Carlson, Yuliang Sun, Tonia Bucholz, Casey Williams, Nandini Dey, Brian Leyland-Jones, and Pradip De. "Abstract 3506: Carfilzomib demonstrates antiproliferative and proapoptotic activities in preclinical triple-negative breast cancer models." In Proceedings: AACR 107th Annual Meeting 2016; April 16-20, 2016; New Orleans, LA. American Association for Cancer Research, 2016. http://dx.doi.org/10.1158/1538-7445.am2016-3506.

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5

Segun Peter, A., MD Ismail Fyaz, OO Ogbole, L. Nahar, AR Evans, and D. Sarker Satyajit. "Antiproliferative activities of Citrus aurantium against breast (MCF7), cervix (HeLa) and urinary bladder (EJ138) carcinoma cells." In GA 2017 – Book of Abstracts. Georg Thieme Verlag KG, 2017. http://dx.doi.org/10.1055/s-0037-1608385.

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Khan, Jesmine, Wan Nor I’zzah Wan Mohamad Zain, Nurul Suhaili Amirah Mamat, Raja Nurfirzanah Syaza Raja Sharin, Noor Masyitah Jumahat, and Jamal Houssaini. "Vitamin C and E contents and antioxidant, antibacterial, and antiproliferative activities of Citrus suhuiensis peel." In 5th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecmc2019-06296.

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Wan Mohamad Zain, Wan Nor I'zzah, Taufiq Yap, Fauziah Othman, and Asmah Rahmat. "Nutrient composition, antioxidant and antiproliferative activities of Clausena excavata and Murraya koenigii leaves." In 5th International Electronic Conference on Medicinal Chemistry. Basel, Switzerland: MDPI, 2019. http://dx.doi.org/10.3390/ecmc2019-06332.

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Ahmed, Elham, Abdul Khan, Kirti S. Prabhu, Kodappully Siveen, Zafar Nawaz, Hatem Zayed, and Shahab Uddin. "Sanguinarine Mediated Anti-Tumor activity Via Targeting JAK/STAT3 Pathway in Thyroid Cancer." In Qatar University Annual Research Forum & Exhibition. Qatar University Press, 2020. http://dx.doi.org/10.29117/quarfe.2020.0155.

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Sanguinarine (SNG), a natural compound with an array of pharmacological activities, has promising therapeutic potential against a number of pathological conditions, including malignancies. This research aimed to investigate the antiproliferative and anti-cancer potential of SNG against two well characterized papillary thyroid cancer (PTC) cell lines, BCPAP and TPC-1 .In both cell lines , SNG was able to inhibit cell proliferation in time and dose dependent manner. Western blot analysis revealed increased expression of apoptosis and autophagy markers , caspase-3,cleaved caspase-3 , P62, and LC3. SNG modulate its anticancer effect through ROS production, because NAC was able to reverse SNG effect. Interestingly, co-treatment of PTC with SNG and cisplatin amplified anticancer activity. Finally, SNG treatment of PTC spheroid suppressed its growth with downregulation of stemness markers including ALDH2 and SOX2 markers. In conclusion, SNG enhanced the anti cancer activity against PTC cells and the effect is amplified when cisplatin is added.
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Blaja, Svetlana, Lidia Lungu, Kaleria Kuchkova, Alexandru Ciocarlan, and Aculina Aricu. "Synthesis of new molecular hybrids with phenothiazine fragment from norambreinolide." In Scientific seminar with international participation "New frontiers in natural product chemistry". Institute of Chemistry, Republic of Moldova, 2023. http://dx.doi.org/10.19261/nfnpc.2023.ab10.

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The known phenothiazine derivatives exhibit a wide spectrum of biological activities, including such as antiparasitic, antioxidant, anticancer, antiproliferative, antineoplastic, antimicrobial, etc. [1]. For this reason, terpeno-phenothiazine molecular hybrids represent one of the priority strategies of organic synthesis in the design of new bioactive compounds. Here are reported the results of the synthesis of new homodrimane hybrids with a phenothiazine fragment. Starting from (+)-sclareolide 1 the Δ8,13-bicyclohomofarnesoic acid 2 and 11-homodrim-6(8)-dien-12-oic acid 3 were synthesized in 6 and 5 steps in 62% and 81% overall yields, respectively [2,3]. Intermediate acyl chlorides 4 and 5 were generated in situ by treating acids 2 and 3 with oxalyl chloride in anhydrous benzene and then coupled with phenothiazine in the presence of triethylamine in methylene chloride on stirring to give hybrid phenothiazines 6 and 7 in depicted yields (see Scheme). The structures of all synthesized compounds were fully confirmed by spectral methods of analysis (IR, 1H, 13C and 15N NMR).
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Hussein, Ola, Feras Alali, Ala‐Eddin Al Mustafa, and Ashraf Khalil. "Development of Novel Chalcone Analogs as Potential Multi-Targeted Therapies for Castration-Resistant Prostate Cancer." In Qatar University Annual Research Forum & Exhibition. Qatar University Press, 2021. http://dx.doi.org/10.29117/quarfe.2021.0114.

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Abstract:
Prostate cancer (PCa) is the second most frequently diagnosed malignancy, as well as a leading cause of cancer-related mortality in men globally. Despite the initial response to hormonal targeted therapy, the majority of patients ultimately progress to a lethal form of the disease, castration-resistant prostate cancer (CRPC). Therefore, the objective of this study was to discover and develop novel treatment modalities for CRPC. Chalcones are among the highly attractive scaffolds being investigated for their antitumor activities. A library of 26 chalcone analogs were designed, synthesized and evaluated as potential therapies for CRPC. The design was guided by in-silico ADMET prediction in which analogs with favorable drug-likeness properties were prioritized. The new compounds were synthesized, purified and characterized by extensive structural elucidation studies. The compounds in vitro cytotoxicity was evaluated against two androgen receptor (AR)-negative prostate cancer cell lines (PC3 and DU145). Among the tested compounds, pyridine containing analogs (13, 15 and 16) showed potent antiproliferative activities with IC50 values ranging between 4.32-6.47 µM against PC3 and DU145 cell lines. Detailed biological studies of the lead molecule 16 revealed that it can significantly induce apoptosis through upregulation of Bax and downregulation of Bcl-2. In addition, compound 16 potently inhibited colony formation and reduced cell migration of AR-negative PCa cell lines (PC3 and DU145). The molecular pathway analysis showed that the anticancer activity of compound 16 is associated with blocking of ERK1/2 and Akt activities. Furthermore, compound 16 inhibited angiogenesis in the chick chorioallantoic membrane (CAM) model as compared to control. Structure-activity relationship study revealed that the cytotoxicity could dramatically improve via changing the methoxylation pattern by more than 2-folds (IC50 << 2.5 μM). These results indicate that pyridine-based chalcones could serve as promising lead molecules for the treatment of CRPC; thus, further in vitro and in vivo studies are warranted.
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