Anti-HIV-1 activity of five anthraquinone derivatives / 中国病理生理杂志

ABSTRACT

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.