Inhibition of the tumor-promoting action of 12-O-tetradecanoylphorbol-13-acetate by some oleanane-type triterpenoid compounds

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 experi...

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Bibliographic Details
Published in:Cancer research (Chicago, Ill.) Ill.), 1988-09, Vol.48 (18), p.5210-5215
Main Authors: Nishino, H, Nishino, A, Takayasu, J, Hasegawa, T, Iwashima, A, Hirabayashi, K, Iwata, S, Shibata, S
Format: Article
Language:English
Subjects:
Animals
Cells, Cultured
Glycyrrhetinic Acid - pharmacology
Mice
Mice, Inbred C3H
skin
Skin Neoplasms - chemically induced
Structure-Activity Relationship
Tetradecanoylphorbol Acetate - antagonists & inhibitors
triterpenes
Triterpenes - pharmacology
tumours
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Summary: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 32Pi 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, 18 beta-olean-12-ene-3 beta,28-diol (= erythrodiol), 18 beta-olean-12-ene-3 beta,23,28-triol, 18 alpha-olean-12-ene-3 beta,28-diol, and 18 alpha-olean-12-ene-3 beta,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.
ISSN:0008-5472