Abstract: In this study,silicagel, Sephagex LH-20 and thin layer chromatography were used to screen and isolate active anti-hepatitis B virus compounds from Hypericum japonicum Thunb.ex Murray extracted with 60% ethanol. Four compounds were isolated from the ethyl acetate extract of H.japonicum and their structures were characterized by spectral, chemical and structural analyses. In addition, using HepG22.2.15 cell line, the cytotoxicity and inhibitory effect on secretion of HBeAg and HBsAg of the 4 isolated compounds were examined by MTT and enzyme-linked immunosorbent assays. The 4 isolated compounds were determined to be vincetoxicoside (1), (2R,3R) double hydrogen quercetin-7-O-α-L-rhamnoside (2), quercitrin (3) and 1,3,6,7-tetrahydorxxynahtnoni (4). Among these 4 compounds, compound 4 exhibited highest activity in inhibiting secretion of HBeAg in HepG 22.2.15 cells, with inhibition rate of 67.66%,IC₅₀ of 40.25 μg/mL and therapeutic index TI > 2.

Key words: Hypericum japonicum, HBV, HBeAg, TI