Cancer chemopreventive agents (antitumor-promoters) from Ajuga decumbens.
Sixteen compounds (1-16) isolated from the flowering whole plant of Ajuga decumbens have been tested for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) induction by the tumor promoter, 12-O-tetradecanoylphorbol-13-acetate (TPA), as a primary screening test for antitumor-promoters (potential cancer chemopreventive agents). Five compounds (6, 9, and 12-14) showed strong inhibitory effects on EBV-EA induction. Of these active compounds, two major constituents of this plant, cyasterone (6) and 8-acetylharpagide (13), showed potent antitumor-promoting activities on a mouse-skin in vivo two-stage carcinogenesis procedure, using 7, 12-dimethylbenz[a]anthracene as initiator and TPA as promoter. Further, compound 13 also exhibited potent chemopreventive activity in a mouse pulmonary tumor model.
Takasaki
M
M
Kyoto Pharmaceutical University, Misasagi, Yamashina-ku, Kyoto 607-8414, and Kyoto Prefectural University of Medicine, Kamigyo-ku, Kyoto 602-0841, Japan.
Tokuda
H
H
Nishino
H
H
Konoshima
T
T
D015112:4-Nitroquinoline-1-oxide / Q000633:toxicity; D000818:Animals; D000972:Antineoplastic Agents, Phytogenic / Q000494:pharmacology*; D000998:Antiviral Agents / Q000494:pharmacology; D002273:Carcinogens / Q000037:antagonists & inhibitors*; D005260:Female; D005990:Glycerol / Q000037:antagonists & inhibitors / Q000633:toxicity; D004854:Herpesvirus 4, Human / Q000187:drug effects; D008175:Lung Neoplasms / Q000139:chemically induced / Q000517:prevention & control; D051379:Mice; D008813:Mice, Inbred ICR; D010212:Papilloma / Q000139:chemically induced / Q000517:prevention & control; D010946:Plants, Medicinal / Q000737:chemistry*; D012878:Skin Neoplasms / Q000139:chemically induced / Q000517:prevention & control; D013755:Tetradecanoylphorbol Acetate / Q000037:antagonists & inhibitors / Q000633:toxicity; D014407:Tumor Cells, Cultured
D000972:Antineoplastic Agents, Phytogenic; D000998:Antiviral Agents; D002273:Carcinogens; D015112:4-Nitroquinoline-1-oxide; D013755:Tetradecanoylphorbol Acetate; D005990:Glycerol