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1.
Bioorg Med Chem Lett ; 23(3): 635-40, 2013 Feb 01.
Artigo em Inglês | MEDLINE | ID: mdl-23273518

RESUMO

Novel Aza-resveratrol analogs were synthesized, structurally characterized and evaluated for cytotoxic activity against MDA-MB-231 and T47D breast cancer cell lines, which exhibited superior inhibitory activity than parent resveratrol compound. The binding mechanism of these compounds with estrogen receptor-α was rationalized by molecular docking studies which indicated additional hydrogen binding interactions and tight binding in the protein cavity. Induction of Beclin-1 protein expression in breast cancer cell lines after treatment with newly synthesized resveratrol analogs indicated inhibition of growth of these cell lines through autophagy. The study highlighted the advantage of introducing the imino-linkage in resveratrol motif in enhancing the anticancer potential of resveratrol suggesting that these analogs can serve as better therapeutic agents against breast cancer and can provide starting point for building more potent analogs in future.


Assuntos
Compostos Aza/síntese química , Compostos Aza/farmacologia , Neoplasias da Mama/tratamento farmacológico , Receptor alfa de Estrogênio/metabolismo , Estilbenos/síntese química , Estilbenos/farmacologia , Compostos Aza/química , Compostos Aza/uso terapêutico , Linhagem Celular Tumoral , Proliferação de Células/efeitos dos fármacos , Simulação por Computador , Feminino , Regulação da Expressão Gênica/efeitos dos fármacos , Humanos , Ligação de Hidrogênio , Modelos Moleculares , Estrutura Molecular , Ligação Proteica/efeitos dos fármacos , Resveratrol , Estilbenos/química , Estilbenos/uso terapêutico
2.
J Med Humanit ; 41(3): 395-410, 2020 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31965464

RESUMO

This article experiments with multimedia storytelling to re-vision difference outside biomedical and humanistic frames by generating new understandings of living dis/artfully with illness. We present and analyze seven short videos created by women and trans people living with illness as part of an arts-based research project that aimed to speak back to hegemonic concepts of disability that create barriers to healthcare.1 We call for a welcoming in of disability studies' disruptive and re-imaginative orientations to bodily difference to unsettle medicine's humanistic accounts. In turn, we advance medical post-humanistic approaches that call on disability studies to re-embody its theories and approaches.


Assuntos
Comunicação , Pessoas com Deficiência , Feminino , Humanos
3.
Pharmacognosy Res ; 8(2): 97-104, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-27034599

RESUMO

BACKGROUND: An Indian origin, Celosia argentea is a weed growing during rainy season traditionally claimed for treating several ailments. Early researches on C. argentea were focused on the anti-cancer screening of seeds, with few reports on aerial parts. OBJECTIVE: To isolate and characterize bioactive compounds of aerial parts of C. argentea and evaluate their anticancer potential. MATERIALS AND METHODS: The methanolic aerial part extract was fractionated on column chromatography using chloroform: methanol mixture. The fractions; 80:20 and 95:5 were purified on MCI-HP20 HPLC column. Chromatographically pure compounds were pooled, concentrated and characterized spectroscopically. The compounds were further screened for anti-oxidant and cytotoxic potential. RESULTS: Isolated compounds were confirmed as: (1) Luteolin-7-O-glucoside and (2) phenolic, 1-(4-hydroxy-2-methoxybenzofuran-5-yl)-3-phenylpropane-1,3-dione. Both exhibited significant antioxidant potential with IC50 values of 20.80 and 21.30 µg/ml for 2,2-diphenyl-1-picrylhydrazyl assay (***P < 0.001) and significant Trolox equivalent antioxidant capacity (TEAC) values for 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid) (*P < 0.05) and ferric reducing antioxidant potential assay (****P < 0.0001). In 3(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-tetrazoliumbromide assay, Compound 1 and 2 showed potent cytotoxicity against SiHa, HCT, MCF-7 cancer cell lines at 20 µg/ml (****P < 0.0001) and 18 µg/ml (**P < 0.01), respectively, without affecting the normal Vero cells. Both compounds enabled maximum reduction in cell viability at 50 µg/ml against HT-29 (***P < 0.001) and MCF-7 cell lines (**P < 0.01) in try pan blue viability assay. Apoptosis occurred at concentrations of 47.33 ± 0.8 µg/ml and 56.28 ± 1.2 µg/ml for Compound 1 and 35.15 ± 0.4 µg/ml and 28.05 ± 0.3 µg/ml for Compound 2 for HT-29 and MCF-7 respectively. CONCLUSION: A novel anticancer phenolic compound; (1-(4-hydroxy-2-methoxybenzofuran-5-yl)-3-phenylpropane-1,3-dione), isolated from aerial parts of C. argentea was a valuable finding of the research. SUMMARY: The present study validated the potential of the plant C. argentea as an antioxidant, and anticancer remedy with two valuable isolations. Although one of them is a known compound: Luteolin 7-0 glycoside, the other isolated phenolic compound;-{1-(4-hydroxy-2-methoxybenzofuran-5-yl)-3-phenylpropane-1,3-dione}, is the first to be reported and thus can be considered as a valuable outcome of this research work.

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