The stem bark of Kalopanax pictus is an anti-rheumatoidal arthritis drug in Oriental medicine. In the rheumatoidal rat, induced by Freund's complete adjuvant (FCA) reagent, we investigated the effects of hederagenin monodesmosides of K. pictus on oxidative stress and hepatic drug-metabolizing enzymes. Kalopanaxsaponin-A (KPS-A) significantly decreased malondialdehyde formation and the activities of xanthine oxidase and aldehyde oxidase of hepatic non-microsomal systems in FCA reagent-treated rats. In addition, increased activity levels of superoxide dismutase, catalase and glutathione peroxidase were also observed. The effects of KPS-A were more potent than the effects of KPS-I. These results suggested that KPS-A, extracted from K. pictus, could reduce rheumatoidal syndromes through antioxidative mechanisms.