Estrogenic Activity of Chemical Constituents from Tephrosia candida

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• 作者：Mohamed-Elamir F. Hegazy ; Abou El-Hamd H. Mohamed ; Ali M. El-Halawany ; Pierre C. Djemgou ; Abdelaaty A. Shahat ; Paul W. Pare虂
• 刊名：Journal of Natural Products
• 出版年：2011
• 出版时间：May 27, 2011
• 年：2011
• 卷：74
• 期：5
• 页码：937-942
• 全文大小：798K
• 年卷期：v.74,no.5(May 27, 2011)
• ISSN：1520-6025

文摘

In a continued investigation of medicinal plants from the genus Tephrosia, phytochemical analysis of a methylene chloride鈥搈ethanol (1:1) extract of the air-dried aerial parts of Tephrosia candida afforded two new 8-prenylated flavonoids, namely, tephrocandidins A (1) and B (2), a new prenylated chalcone, candidachalcone (3), a new sesquiterpene (4), and a previously reported pea flavonoid phytoalexin, pisatin (5). The structures of 1鈥?b>4 were established by spectroscopic methods, including HREIMS, and ¹H, ¹³C, DEPT, HMQC, and HMBC NMR experiments. The most potent estrogenic activity of these isolated natural products in an estrogen receptor (ER伪) competitive-binding assay was for 3, which exhibited an IC₅₀ value of 80 渭M, compared with 18 nM for the natural steroid 17尾-estradiol. Results were interpreted via virtual docking of isolated compounds to an ER伪 crystal structure.