Author/Authors :
Akihisa، نويسنده , , Toshihiro and Tokuda، نويسنده , , Harukuni and Ichiishi، نويسنده , , Eiichiro and Mukainaka، نويسنده , , Teruo and Toriumi، نويسنده , , Masakazu and Ukiya، نويسنده , , Motohiko and Yasukawa، نويسنده , , Ken and Nishino، نويسنده , , Hoyoku، نويسنده ,
Abstract :
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.
Keywords :
Trichosanthes kirilowii , Cucurbitaceae , Epstein–Barr virus early antigen , Anti-tumor promoter , Multiflorane-type triterpenoids , structure–activity relationships , cytotoxicity
