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[Cancer Research 48, 5210-5215, September 15, 1988]
© 1988 American Association for Cancer Research
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Inhibition of the Tumor-promoting Action of 12-O-Tetradecanoylphorbol-13-acetate by Some Oleanane-type Triterpenoid Compounds

Hoyoku Nishino, Atsuko Nishino, Junko Takayasu, Teiko Hasegawa, Akio Iwashima, Kazuhiro Hirabayashi, Susumu Iwata and Shoji Shibata

Department of Biochemistry, Kyoto Prefectural University of Medicine, Kawaramachi-dori, Kamigyo-ku, Kyoto 602 [H. N., A. N., J. T., T. H., A. I.]; Research Laboratory, Minophagen Pharmaceutical Co., Komatsubara 2-5233, Zama, Kanagawa-ken 228 [K. H., S. I.]; Meiji College of Pharmacy, Nozawa 1-35-23, Setagaya-ku, Tokyo 154 [S. S.], Japan

Since glycyrrhetinic acid was proved to suppress tumor promoter effects, several oleanane-type triterpenes which were chemically derived from oleanolic acid and hederagenin were tested in vitro and in vivo against the action of tumor promoter, 12-O-tetradecanoylphorbol 13-acetate.

By in vitro experiment monitoring with 12 - O - tetradecanoylphorbol-13-acetate-induced stimulation of 32P1 incorporation into phospholipids and an in vivo test on skin tumor formation in mice initiated with 7,12-dimethylbenz[a]anthracene and promoted with 12-O-tetradecanoylphorbol-13-acetate, 18ß-olean-12-ene-3ß,28-diol, (=erythrodiol), 18ß-olean-12-ene-3ß,23,28-triol, 18{alpha}-olean-12-ene-3ß,28-diol, and 18{alpha}-olean-12-ene-3ß,23,28-triol showed remarkable suppressive effects. Especially 18{alpha}-oleanane derivatives having a CH2OH grouping converted from the COOH group initially allocated at C-17 were 100 times more effective than glycyrrhetinic acid both in vitro and in vivo.

Received 3/ 2/88. Revised 6/17/88. Accepted 6/21/88.




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Copyright © 1988 by the American Association for Cancer Research.