Anti-estrogenic Activity of Mansorins and Mansonones from the Heartwood of Mansonia gagei DRUMM

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Abstract

Through an anti-estrogenic bioassay-guided fractionation of the methanol extract of <i>Mansonia gagei</i>, 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.

Journal

  • Chemical and Pharmaceutical Bulletin

    Chemical and Pharmaceutical Bulletin 55(9), 1332-1337, 2007-09-01

    The Pharmaceutical Society of Japan

References:  25

Codes

  • NII Article ID (NAID)
    110006379653
  • NII NACSIS-CAT ID (NCID)
    AA00602100
  • Text Lang
    ENG
  • Article Type
    ART
  • ISSN
    00092363
  • NDL Article ID
    8877649
  • NDL Source Classification
    ZS51(科学技術--薬学) // ZP1(科学技術--化学・化学工業)
  • NDL Call No.
    Z53-D167
  • Data Source
    CJP  NDL  NII-ELS  J-STAGE 
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