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 |
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Rok vydání: | 1998 |
Předmět: |
Salmonella typhimurium
Magnetic Resonance Spectroscopy Ethyl methanesulfonate Double bond Stereochemistry Chemical structure Pharmaceutical Science Mutagen medicine.disease_cause Chemical synthesis Mass Spectrometry Analytical Chemistry Ames test Structure-Activity Relationship chemistry.chemical_compound Drug Discovery medicine Mode of action Pharmacology chemistry.chemical_classification Molecular Structure Mutagenicity Tests Plant Extracts Organic Chemistry Antimutagenic Agents Acrylates Complementary and alternative medicine chemistry Molecular Medicine Antimutagen |
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 |
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