Chemical and Pharmaceutical Bulletin
Online ISSN : 1347-5223
Print ISSN : 0009-2363
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Anti-estrogenic Activity of Mansorins and Mansonones from the Heartwood of Mansonia gagei DRUMM.
Ali Mahmoud El-HalawanyMi Hwa ChungChao-Mei MaKatsuko KomatsuTsutomu NishiharaMasao Hattori
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2007 Volume 55 Issue 9 Pages 1332-1337

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Abstract

Through an anti-estrogenic bioassay-guided fractionation of the methanol extract of Mansonia gagei, three new coumarins, called mansorins I (1), II (2) and III (3) and a new naphthoquinone, mansonone I (4), were isolated. Their structures were determined based on their NMR data and CD spectroscopy. The anti-estrogenic activity of the fractions and the isolated compounds were investigated using a yeast two-hybrid assay method expressing estrogen receptors α (ERα) and β (ERβ). In addition, an ERα competitor screening system (ligand binding screen) was used to verify the binding affinities of the isolated compounds to the estrogen receptor. 1,2-Naphthoquinones (mansonones) showed more binding affinities to ER in both assay systems. All the tested compounds showed higher binding affinities to ERβ than to ERα in the yeast two-hybrid assay. Mansonones F and S showed the most potent estrogen binding and estrogen antagonistic effects.

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© 2007 The Pharmaceutical Society of Japan
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