Hepatoprotective activity-guided fractionation of the MeOH extract of Equisetum arvense L. (Equisetaceae) resulted in the isolation of two phenolic petrosins, onitin (1) and onitin-9-O-glucoside (2), along with four flavonoids, apigenin (3), luteolin (4), kaempferol-3-O-glucoside (5), and quercetin-3-O-glucoside (6). Among these, compounds 1 and 4 exhibited hepatoprotective activities on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells, displaying EC(50) values of 85.8 +/ -9.3 microM and 20.2 +/- 1.4 microM, respectively. Silybin, used as a positive control, showed the EC(50) value of 69.0 +/- 3.3 microM. Compounds 1 and 4 also showed superoxide scavenging effects (IC(50) = 35.3 +/- 0.2 microM and 5.9 +/- 0.3 microM, respectively) and DPPH free radical scavenging effect (IC(50) of 35.8 +/- 0.4 microM and 22.7 +/- 2.8 microM, respectively). These results support the use of this plant for the treatment of hepatitis in oriental traditional medicine.