For the elucidation of the antimutagenic and cytotoxic principles from the stem bark of Kalopanax pictus, seven isolated components of this crude drug were tested in the Ames test and the MTT test. Hederagenin and its monodesmosides, kalopanaxsaponin A and I in addition to its bisdesmosides, kalopanaxsaponin B and H, showed potent antimutagenic activities against aflatoxin B 1 (AFB 1 ). However, they had no inhibitory effects on mutagenicity induced by the direct mutagen, N-methyl-N¢ ¢-nitro-N-nitrosoguanidine (MNNG). This suggested that hederagenin glycosides might effectively prevent the metabolic activation of AFB 1 or scavenge the electrophilic intermediate capable of inducing mutation. Hederagenin was found to be an essential moiety for the exhibition of antimutagenicity. Moreover, hederagenin and its 3-O-glycosides were found to be cytotoxic on various tumor cell lines, P-388, L-1210, U-937, HL-60, SNU-5 and HepG2, while 3,28-di-O-glycosides of hederagenin were not cytotoxic. Hence, hederagenin and its 3-O-glycosides could be suitable for cancer treatment chemopreventive drugs.

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Cytotoxic compounds, oleuropein (1) and a phenylethanoid glycoside (2) were isolated from the stem bark of Syringa velutina KOM. along with coniferylaldehyde 4-O-glucoside, syringin, ligstroside, (+)-syringaresinol 4-O-glucoside, (+)-medioresinol 4"-O-glucoside and (-)-olivil 4"-O-glucoside. Phenylethanoid glycoside (2) was identified to be 3,4-dihydroxyphenylethyl alcohol 8-O-beta-D-glucopyranoside. This compound showed the most potent cytotoxic effect on several tumor cell lines (P-388, L-1210, SNU-5 and HL-60) among eight compounds isolated in the present study. We suggest that the 3,4-dihydroxyphenylethoxy moiety of this compound contributes to cytotoxicity.