Anti-tumor promoting effects of multiflorane-type triterpenoids and cytotoxic activity of karounidiol against human cancer cell lines.
Forty-nine multiflorane-type triterpenoids consisting of 11 compounds isolated from the seeds of Trichosanthes kirilowii (Cucurbitaceae) and 38 of their derivatives have been evaluated for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by the tumor promoter 12-O-tetradecanoylphorbol-13-acetate in Raji cells as a primary screening test for anti-tumor promoters. All of the compounds tested showed an inhibitory effect against EBV-EA activation, and among which 43 were revealed to possess remarkable activity with potencies either comparable to or stronger than that of glycyrrhetic acid, a known natural anti-tumor promoter. Their structure-activity relationship is discussed. Evaluation of the cytotoxic activity of karounidiol (27) against human cancer cell lines exhibited cytotoxicity especially against a human renal cancer.
Akihisa
T
T
College of Science and Technology, Nihon University, 1-8 Kanda Surugadai, Chiyoda-ku, Tokyo 101-8308, Japan. akihisa@chem.cst.nihon-u.ac.jp
Tokuda
H
H
Ichiishi
E
E
Mukainaka
T
T
Toriumi
M
M
Ukiya
M
M
Yasukawa
K
K
Nishino
H
H
D016588:Anticarcinogenic Agents / Q000737:chemistry / Q000494:pharmacology*; D000956:Antigens, Viral / Q000378:metabolism; D019662:Cucurbitaceae / Q000737:chemistry; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D009369:Neoplasms / Q000517:prevention & control*; D012639:Seeds / Q000737:chemistry; D013329:Structure-Activity Relationship; D013755:Tetradecanoylphorbol Acetate / Q000494:pharmacology; D014315:Triterpenes / Q000737:chemistry / Q000494:pharmacology*; D014407:Tumor Cells, Cultured
D016588:Anticarcinogenic Agents; D000956:Antigens, Viral; C033305:Epstein-Barr virus early antigen; D014315:Triterpenes; C088116:karounidiol; D013755:Tetradecanoylphorbol Acetate