Cancer chemopreventive activity of rotenoids from Derris trifoliata.
A study of the chemical constituents of the stems of Derris trifoliata Lour. (Leguminosae) led to the isolation and identification of one new rotenoid, 6aalpha,12aalpha-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 beta-carotene without any cytotoxicity. Deguelin ( 4) and alpha-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.
Ito
Chihiro
C
Faculty of Pharmacy, Meijo University, Nagoya, Japan.
Itoigawa
Masataka
M
Kojima
Naoki
N
Tan
Hugh T-W
HT
Takayasu
Junko
J
Tokuda
Harukuni
H
Nishino
Hoyoku
H
Furukawa
Hiroshi
H
D000818:Animals; D016588:Anticarcinogenic Agents / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D000956:Antigens, Viral / Q000187:drug effects; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D029866:Derris; D004354:Drug Screening Assays, Antitumor; D005260:Female; D051379:Mice; D008813:Mice, Inbred ICR; D008517:Phytotherapy; D010936:Plant Extracts / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D018547:Plant Stems; D012402:Rotenone / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D012878:Skin Neoplasms / Q000517:prevention & control
D016588:Anticarcinogenic Agents; D000956:Antigens, Viral; C033305:Epstein-Barr virus early antigen; D010936:Plant Extracts; D012402:Rotenone