Chain elongation analog of resveratrol as potent cancer chemoprevention agent
J. physiol. biochem
; 72(3): 445-452, sept. 2016. tab, graf
Artigo
em Inglês
| IBECS
| ID: ibc-168287
Biblioteca responsável:
ES1.1
Localização: BNCS
ABSTRACT
Resveratrol is identified as a natural cancer chemoprevention agent. There has been a lot of interest in designing and developing resveratrol analogs with cancer chemoprevention activity superior to that of parent molecule and exploring their action mechanism in the past several decades. In this study, we have synthesized resveratrol analogs of compounds A-C via conjugated chain elongation based on isoprene unit retention strategy. Remarkably, cytotoxic activity analysis results indicated that compound B possesses the best proliferation inhibition activity for NCI-H460 cells in all the test compounds. Intriguingly, compound B displayed a higher cytotoxicity against human non-small cell lung cancer cells (NCI-H460) compared to normal human embryonic lung fibroblasts (MRC-5). Afterward, flow cytometry analysis showed that compound B would induce cell apoptosis. We further researched the action mechanism. When NCI-H460 cells were incubated by compound B for 6 or 9 h, respectively, the intracellular reactive oxygen species (ROS) level was enhanced obviously. With elevation of intracellular ROS level, flow cytometry measurement verified mitochondrial transmembrane potential collapse, which was accompanied by the up-regulation of Bax and down-regulation of Bcl-2. More interestingly, compound B increased the expression of caspase-9 and caspase-3, which induced cell apoptosis. Moreover, compound B arrested cell cycle in G0/G1 phase. These are all to provide useful information for designing resveratrol-based chemoprevention agent and understanding the action mechanism (AU)
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Coleções:
Bases de dados nacionais
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Espanha
Contexto em Saúde:
ODS3 - Meta 3.4 Reduzir as mortes prematuras devido doenças não transmissíveis
Problema de saúde:
Outras Doenças Respiratórias
Base de dados:
IBECS
Assunto principal:
Fenóis
/
Polienos
/
Desenho de Fármacos
/
Apoptose
/
Carcinoma Pulmonar de Células não Pequenas
/
Pulmão
Tipo de estudo:
Estudo prognóstico
Limite:
Humanos
Idioma:
Inglês
Revista:
J. physiol. biochem
Ano de publicação:
2016
Tipo de documento:
Artigo
Instituição/País de afiliação:
Hebei North University/China