KMID : 0606920120200020183
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Biomolecules & Therapeutics 2012 Volume.20 No. 2 p.183 ~ p.188
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Activation of Estrogen Receptor by Bavachin from Psoralea corylifolia
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Park Joon-Woo
Kim Do-Hee Ahn Hye-Na Song Yun-Seon Lee Young-Joo Ryu Jae-Ha
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Abstract
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In this study, we examined the estrogenic activity of bavachin, a component of Psoralea corylifolia that has been used as a traditional medicine in Asia. Bavachin was purified from ethanolic extract of Psoralea corylifolia and characterized its estrogenic activity by ligand binding, reporter gene activation, and endogenous estrogen receptor (ER) target gene regulation. Bavachin showed ER ligand binding activity in competitive displacement of [3H] E2 from recombinant ER. The estrogenic activity of bavachin was characterized in a transient transfection system using ER¥á or ER¥â and estrogen-responsive luciferase plasmids in CV-1 cells with an EC50 of 320 nM and 680 nM, respectively. Bavachin increased the mRNA levels of estrogen-responsive genes such as pS2 and PR, and decreased the protein level of ER¥á by proteasomal pathway. However, bavachin failed to activate the androgen receptor in CV-1 cells transiently transfected with the corresponding receptor and hormone responsive reporter plasmid. These data indicate that bavachin acts as a weak phytoestrogen by binding and activating the ER.
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KEYWORD
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Psoralea corylifolia, Bavachin, Estrogen receptor, Phytoestrogen
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