Abstract. To clarify the hepatoprotective effects of tectoridin and tectorigenin from Puerariae Flos, their effects on tert-butyl hyperoxide (t-BHP)-injured HepG2 cells and mice were investigated. When tectorigenin at a dose of 50 mg / kg was intraperitoneally administered to mice injured by t-BHP, it significantly inhibited the increase the activities of plasma ALT and AST by 39% and 41%, respectively, in the t-BHP-treated group. The inhibitory effect of tectorigenin is much more potent than that of a commercially available dimethyl diphenyl bicarboxylate. Orally administered tectoridin showed hepatoprotective activity. However, when tectoridin was intraperitoneally administrated to mice, no hepatoprotective activity was observed. Tectorigenin also protected against the cytotoxicity of HepG2 cells induced by t-BHP. This protection may have originated from the inhibition of apoptosis. Tectorigenin may be hepatoprotective and tectoridin should be a prodrug that is transformed to tectorigenin.Keywords: tectorigenin, HepG2, hepatic injury t-Butyl hydroperoxide (t-BHP) can be metabolized to free radical intermediates by cytochrome P450 (hepatocytes) or hemoglobin (erythrocytes), which can subsequently initiate lipid peroxidation (1), affect cell integrity, and form covalent bonds with cellular molecules, resulting in cell injury (2). t-BHP is known to cause lactate dehydrogenase and alanine transferase (ALT) leakage in hepatocyte cells (3, 4). Therefore, t-BHP has been used as a chemical inducer for the preparation of a liver injured animal model (5, 6).In traditional Chinese medicine, Puerariae Flos has been used in therapy to counteract the problems associated with alcohol drinking and liver injury (7). Niiho et al. (8,9) reported that the isoflavonoid fraction of Puerariae Flos suppressed the increase in the concentration of blood ethanol, acetaldehyde, and ketones induced by ethanol administration and that its isoflavonoid and triterpenoid saponin fractions improved both the abnormal metabolism induced by ethanol and hepatic injuries induced by carbon tetrachloride or highfat food. Jang et al. (10) reported that Puerariae Flos protected against ethanol-induced apoptosis in the human neuroblastoma cell line SK-N-MC. Lee et al. (11) reported that tectorigenin isolated from Puerariae Flos as an inhibitor of b-glucuronidase showed hepatoprotective activity on the CCl 4 -induced hepatotoxicity in mice.To clarify the hepatoprotective effects of isoflavones tectorigenin and tectoridin (Fig. 1) from Puerariae Flos, tectoridin was isolated from Puerariae Flos and its metabolite tectorigenin from human fecal microflora, and then we investigated their effects in t-BHP-injured HepG2 cells and mice.*Corresponding author. FAX: +82-2-957-5030 E-mail: dhkim@khu.ac.kr