Polygunum cuspidatum has veen used as treatments of dermatitis, gonorrhea, inflammation, and hyperlipidaemia in traditional medicine. We examined liver protective effect on CCl4 inducing hepatotoxicity, and anti-oxidative activity by TBA method. Phytochemical examination of Polygunum cuspidatum led to the isolation and characterization of emodin 8-O-β-D-glucopyranoside (compound 1), and trans-resveratrol 3-O-β-D-glucopyranoside (compound 2). Compounds 1 and 2 enhanced the inhibition of anti-lipid peroxidative effects in liver homogenate. In chemical parameters obtained from serum analysis, compounds 1 and 2 also revealed significant decrease in hepatotoxicity. These results suggested that the analysis, compounds 1 and 2 also revealed significant decrease in hepatotoxicity. These results suggested that the anthraquinone and stilbene which were isolated from Polygunum cuspidatum might be used as therapeutic agent of hepatitis.