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《Chinese Journal of Pathophysiology》 2010-06
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Anti-HIV-1 activity of five anthraquinone derivatives

OUYANG Dong-yun,LIU Chun-yong,ZENG Yao-ying,HE Xian-hui,ZENG Xiang-feng(Institute of Tissue Transplantation and Immunology,College of Life Science and Technology,Jinan University,Guangzhou 510632,China.)  
AIM: To investigate the anti-HIV-1 activity of five anthraquinone derivatives(emodin,rhein,chrysophanol,physcion and aloe-emodin) in vitro.METHODS: Viral replication was estimated by observation of cytopathogenesis and measurement of HIV-1 p24 antigen production in HIV-1ⅢB acutely infected C8166 cells.The anti-HIV-1 activity was evaluated by the 50% effective concentrations(EC50) and selective indexes(SI) of these derivatives.RESULTS: These anthraquinone derivatives inhibited HIV-1ⅢB replication on syncytia formation induced by HIV-1ⅢB infection with EC50 mean values of(11.44±0.93)μmol/L(emodin),(51.28±2.86)μmol/L(rhein),(90.58±2.30)μmol/L(chrysophanol),(8.59±0.38)μmol/L(physcion) and(0.89±0.08)μmol/L(aloe-emodin),respectively.The p24 antigen production with EC50 mean values were(11.61±0.56)μmol/L(emodin),(12.35±4.73)μmol/L(rhein),(39.63±2.87)μmol/L(chrysophanol),250 μmol/L(physcion) and(2.75±0.20)μmol/L(aloe-emodin) respectively.CONCLUSION: These structurally-related chemicals show different anti-HIV-1 activity in vitro.Among them,aloe-emodin is the most potent inhibitor to HIV-1 replication.
【Fund】: Supported by the National 973 Project of China(No.2006CB504200);; Natural Science Fund of Guangdong Province(No.8451063201000340)
【CateGory Index】: R285.5
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