Anti-inflammatory and anti-tumor-promoting effects of triterpene acids and sterols from the fungus Ganoderma lucidum.
A series of lanostane-type triterpene acids, including eleven lucidenic acids (3, 4, 9, 10, 13-19) and six ganoderic acids (20-22, 24, 26, 27), as well as six sterols (28-33), all isolated from the fruiting bodies of the fungus Ganoderma lucidum, were examined for their inhibitory effects on the induction of Epstein-Barr virus early antigen (EBV-EA) by 12-O-tetradecanoylphorbol-13-acetate (TPA) in Raji cells, a known primary screening test for anti-tumor promoters. All of the compounds tested, except for ganolactone (27) and three sterols (29-31), showed potent inhibitory effects on EBV-EA induction, with IC(50) values of 235-370 mol ratio/32 pmol TPA. In addition, nine lucidenic acids (1, 2, 5-8, 11, 12, 18) and four ganoderic acids (20, 23-25) were found to inhibit TPA-induced inflammation (1 microg/ear) in mice, with ID(50) values of 0.07-0.39 mg per ear. Further, 20-hydroxylucidenic acid N (18) exhibited inhibitory effects on skin-tumor promotion in an in vivo two-stage mouse-skin carcinogenesis test based on 7,12-dimethylbenz[a]anthracene (DMBA) as initiator, and with TPA as promoter.
Akihisa
Toshihiro
T
College of Science and Technology, Nihon University, Kanda Surugadai, Chiyoda-ku, Tokyo, Japan. akihisa@chem.cst.nihon-u.ac.jp
Nakamura
Yuji
Y
Tagata
Masaaki
M
Tokuda
Harukuni
H
Yasukawa
Ken
K
Uchiyama
Emiko
E
Suzuki
Takashi
T
Kimura
Yumiko
Y
D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D000956:Antigens, Viral / Q000096:biosynthesis; D000970:Antineoplastic Agents / Q000494:pharmacology*; D005260:Female; D051379:Mice; D008813:Mice, Inbred ICR; D018632:Mice, Inbred SENCAR; D020940:Reishi / Q000737:chemistry*; D013261:Sterols / Q000494:pharmacology*; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D014315:Triterpenes / Q000494:pharmacology*
D000893:Anti-Inflammatory Agents; D000956:Antigens, Viral; D000970:Antineoplastic Agents; C033305:Epstein-Barr virus early antigen; D013261:Sterols; D014315:Triterpenes; D013755:Tetradecanoylphorbol Acetate