Structure−Antimutagenic Activity Relationship Study of Plicatin B

Autor: Sanjay R. Menon, Peter Shih, Lester A. Mitscher, Segaran P. Pillai, Delbert M. Shankel, Vishal K. Patel
Rok vydání: 1998
Předmět:
Zdroj: Journal of Natural Products. 62:102-106
ISSN: 1520-6025
0163-3864
DOI: 10.1021/np980304n
Popis: A systematic structure-activity relationship study of plicatin B (1), an antimutagenic constituent of Psoralea juncea, was undertaken with a view toward elucidating its chemical mode of action and possibly optimizing its antimutagenic activity during the process. Compound 1 and its related analogues were examined for their antimutagenic activity against mutations induced by ethyl methanesulfonate, a direct acting mutagen and alkylating agent, in Salmonella typhimurium strain TA100, utilizing the modified Ames test protocol. The dihydro analogue 3 resulting from saturation of the conjugated alkene double bond of 1 was found to exhibit reduced cytotoxicity and enhanced efficacy relative to the parent compound. This result serves preliminarily to exclude a Michael acceptor role of the alpha,beta-unsaturated carbonyl moiety in connection with its antimutagenic activity.
Databáze: OpenAIRE