In the course of searching for hepatoprotective agents from natural products, four compounds were isolated from the MeOH extract of Sanguisorbae Radix, as guided by their DPPH free radical scavenging activity. The structures were determined as 4,5-dimethoxy-3-hydroxybenzoic acid methyl ester (1), (+)-gallocatechin (2), methyl $6-O-galloyl-{eta}-D-glucopyranoside$ (3), and pomolic acid $3-O-[{alpha}-L-arabinopyranoside]-28-O-[{eta}-D-glucopyranosyl]$ ester (ziyu-glycoside I) (4). Compounds 2 and 3 showed significant DPPH free radical scavenging effects, exhibiting $IC_{50}$ values of 11.4 and $13.0;{mu}M$, respectively. L-Ascorbic acid was used as a positive control and exhibited the $IC_{50}$ value of $50.3;{mu}M$. In evaluation of the hepatoprotective activity of the isolated compounds on drug-induced cytotoxicity, compound 2 showed the significant hepatoprotective effect with the $EC_{50}$ value of $91.84;{pm};11.0;{mu}M$ on tacrine-induced cytotoxicity in Hep G2 cells, while silybin, a positive control, exhibited $EC_{50}$ value of $122.4;{pm};12.5;{mu}M$.