Antihepatotoxic chemical constituents from the roots of Ampelopsis sinica var. hancei (pl.) W.T. Wang was investigated- Chromatography was used to isolate chemical constituents and their structures were elucidated on the basis of spectroscopic analysis. Antihepatotoxic activity of these compounds in rats was carried out after the establishment of CCl4 induced liver injury. Phytochemical investigation on the roots of Ampelopsis sinica var. hancei (pl.) W. T. Wang resulted in the isolation of eight compounds including β-sitosterol (1), β-daucosterol (2), lupeol (3), trans-resveratrol (4), piceid (5), gallic acid (6), n-butyl gallate (7) and (+)-catechin (8). Rats treated with the compounds 6-8 showed significant (p < 0.05) protection of liver as evidence from normal AST and ALT levels. LDH levels were significantly (p < 0.05) reduced by the treatment with the compounds 5, 7 and 8. In addition, MDA levels were significantly (p < 0.05) increased with gallic acid (6) and (+)-catechin (8). All the chemical constituents were isolated from Ampelopsis sinica var. hancei (pl.) W.T. Wang for the first time. Compounds 5-8 showed significantly antihepatotoxtic activity in CCl4 -induced liver damage rats.