1Faculty of Pharmacy, Meijo University, Nagoya, Japan
2Tokai Gakuen University, Aichi, Japan
3Department of Botany, National University of Singapore, Singapore
4Department of Biochemistry, Kyoto Prefectural University of Medicine, Kyoto, Japan
This study was supported in part by Grants-in-Aid for Scientific Research (C) from the Japan Society for the Promotion of Science, and the High-Tech Research Center Project from the Ministry of Education, Culture, Sports, Science and Technology (MEXT) of Japan. This study was also supported in part by a grant from the National Cancer Institute (CA17625).
A study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) led to the isolation and identification of one new rotenoid, 6aα,12aα-12a-hydroxyelliptone (3), together with five other known rotenoids. In a search for novel cancer chemopreventive agents (anti-tumor promoters), we carried out a primary screening of five of the rotenoids isolated from the plant for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-O-tetradecanoylphorbol 13-acetate (TPA) in Raji cells. The inhibitory activity of 3 was found to be equivalent to that of β-carotene without any cytotoxicity. Deguelin (4) and α-toxicarol (5) exhibited a marked inhibitory effect on mouse skin tumor promotion in an in vivo two-stage carcinogenesis test. This investigation indicated that rotenoids might be valuable anti-tumor promoters.
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