The stem of Akebia quinata Decasisne (Lardizabalaceae) has been used to treat urinary tract inflammatory disease. It has been reported that saponins in medicinal plants may act as bioactive components after biodegradation to sapogenins in the gastrointestinal tract. To find the active components, we obtained the methanol (MeOH) extract from A. quinata stems and fractionated this extract into CHCl(3), butanol (BuOH), and H(2)O fractions. A saponin-containing BuOH fraction was refluxed in an acidic solution to yield the hydrolyzed fraction. Silica gel column chromatography separated kalopanaxsaponin A (1) from the BuOH fraction, and oleanolic acid (2) and hederagenin (3) were obtained from the hydrolyzed fraction. The antinociceptive effect was tested by hot plate-writhing and tail-flicks methods using mice, and the anti-inflammatory effect was assayed using carrageenan-induced rat edema against the following samples: the MeOH extract of A. quinata stems, its fractions, the isolated saponin, kalopanaxsaponin A, and the sapogenins hederagenin and oleanolic acid. The MeOH extract exhibited antinociceptive/anti-inflammatory effects by oral administration of 100 and 250 mg/kg doses, indicating that the MeOH extract has an antinociceptive/anti-inflammatory activity. The BuOH fraction (crude saponin) also significantly exhibited those bioactivities. Treatments with 10 and 30 mg/kg perorally of these two sapogenins produced significant antinociceptive/ anti-inflammatory effects in the rat, suggesting that the sapogenins may act as resultant active compounds. Compounds 2 and 3 inhibited dye leakage into the peritoneal cavity induced by acetic acid, and the latter was more active than the former. The anti-inflammtory effects were further supported by the reduction of carrageenan-induced lipid peroxidation and hydroxy radical content in serum. These results suggest that the antinociceptive/anti-inflammatory properties of the stem of A. quinata can be attributed to the sapogenins oleanolic acid and hederagenin.