Primary Study Of Anti-HBV Activities Of Phyllocoumarin And (-)-epicatechin From Schisandra Lancifolia In Vitro

【Objective】Although the combination of the chemical drugs in the antiviral therapy more effectively reduce morbidity and mortality in HBV infected individuals than the use of single drug, emergence of HBV drugs resistance and side effects for long-term antiretroviral treatment limited the use of these drugs. So continuously development of new anti-HBV drugs appears to be inevitable. Presently, drugs of the anti-HBV therapy used clinically are nucleoside analogues.such as lamivudine, adefovir dipivoxil,ganciclovir, famciclovir and entecavir,emtricitabine. Natural products as the most consistently successful source in drug discovery may offer opportunities for finding anti-HBV drugs or lead compounds. In past 20 years, many natural compounds with anti-HBV activity have been isolated and indentified, In this study, we tested the anti-HBV effects of compounds isolated from Schisandra lancifolia. Scientists in China have found that compouds and many effective ingredients from Schisandra chinensis, with the function of protecting liver and decreasing levels of ALT, antioxidant and anti-HBV activity, tagarted many sites of virus. They have succeeded in developing two anti-HBV drugs, Bifendate and bicyclol. To confirm chemical compositions from Schisandra lancifolia and to evaluate its antiviral therapy,we have found many compouds, such as Lancifodilactone F and Lancifodilactone G, were against HIV-1. Here, we primarily studied that compouds phyllocoumarin (1) and (-)-epicatechin (2) from Schisandra lancifolia were anti-HBV activity.【Methods】To evaluate anti-HBV activities of phyllocoumarin (1) and (-)-epicatechin (2) from Schisandra lancifolia in vitro,we used HepG2.2.15 cells as HBV model in vitro. Different concentrations of compounds (1) and compounds (2) were added to the wells with the growth of HepG2.2.15 cells and the supernatant was collected at the third day. The cytotoxic activity on the growth of HepG2.2.15 cells was detected by MTT. ELISA for HBsAg and HBeAg assays were used to evaluate effects of compounds 1 and 2 on HBV replication.【Result】Both coupound 1 and compound 2 showed anti-HBV activity and exerted cytotoxicity against HepG2.2.15 cells with CC50>200μg/ml. But coupound 1 more effectively decreased levels of secretion of HBsAg and HBeAg than compound 2. Compared with Adefovir Dipivoxil (ADV), compound 1 inhibited the secretion of HBsAg and HBeAg more effective at the same concentration (1.6μg/ml).【Conclusion】phyllocoumarin and (-)-epicatechin are two potential anti-HBV agents and show lower cytotoxicity.