摘要:To evaluate the hepatoprotective effect of Red Ginseng (RG), we isolated a main constituent 20( S )-ginsenoside Rg3 from RG, and its metabolite 20( S )-ginsenoside Rh2 by human intestinal microflora, and investigated their hepatoprotective activities in tert -butyl hydroperoxide ( t -BHP)-induced hepatotoxicity of HepG2 cells and mice. When HepG2 cells were treated with t -BHP, its cytotoxicity was significantly increased. 20( S )-Ginsenoside Rh2 potently protected its cytotoxicity, but 20( S )-ginsenoside Rg3 weakly protected it. Intraperitoneally and orally administered 20( S )-ginsenoside Rh2 to t -BHP-injured mice significantly inhibited the increase of serum alanine aminotransferase (ALT) and aspartate aminotransferase (AST) activities. Orally administered 20( S )-ginsenoside Rg3 also showed the inhibition against the increase of ALT and AST of t -BHP-induced mice. However, intraperitoneally administered 20( S )-ginsenoside Rg3 could not inhibit the elevation of serum ALT and AST activities. These results suggest that 20( S )-ginsenoside Rg3 a main component of RG may be a prodrug for hepatotoxicity.