Essential moiety for antimutagenic and cytotoxic activity of hederagenin monodesmosides and bisdesmosides isolated from the stem bark of Kalopanax pictus

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 monodes mosides, kalopanaxsaponin A and I in addition to its bisdesmosides, kalopan axsaponin B and H, showed potent antimutagenic activities against aflatoxin B-1 (AFB(1)). However, they had no inhibitory effects on mutagenicity indu ced by the direct mutagen, N-methyl-N'-nitro-N-nitrosoguanidine (MNNG). Thi s suggested that hederagenin glycosides might effectively prevent the metab olic activation of AFB(1) or scavenge the electrophilic intermediate capabl e of inducing mutation. Hederagenin was found to be an essential moiety for the exhibition of antimutagenicity. Moreover, hederagenin and its 3-O-glyc osides were found to be cytotoxic on various tumor cell lines, P-388, L-121 0, 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 sui table for cancer treatment chemopreventive drugs.