Biomolecules & Therapeutics

  • 제20권2호
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  • Pages.183-188
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  • 2012
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  • 1976-9148(pISSN)
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  • 2005-4483(eISSN)
한국응용약물학회 (The Korean Society of Applied Pharmacology)
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Activation of Estrogen Receptor by Bavachin from Psoralea corylifolia

  • Park, Joon-Woo (College of Life Science, Institute of Biotechnology, Department of Bioscience and Biotechnology, Sejong University) ;
  • Kim, Do-Hee (College of Pharmacy, Research Center for Cell Fate Control, Sookmyung Women's University) ;
  • Ahn, Hye-Na (College of Pharmacy, Research Center for Cell Fate Control, Sookmyung Women's University) ;
  • Song, Yun-Seon (College of Pharmacy, Research Center for Cell Fate Control, Sookmyung Women's University) ;
  • Lee, Young-Joo (College of Life Science, Institute of Biotechnology, Department of Bioscience and Biotechnology, Sejong University) ;
  • Ryu, Jae-Ha (College of Pharmacy, Research Center for Cell Fate Control, Sookmyung Women's University)
  • 투고 : 2011.10.25
  • 심사 : 2012.01.10
  • 발행 : 2012.03.31
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초록

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 [$^3H$] $E_2$ from recombinant ER. The estrogenic activity of bavachin was characterized in a transient transfection system using $ER{\alpha}$ or $ER{\beta}$ and estrogen-responsive luciferase plasmids in CV-1 cells with an $EC_{50}$ 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 $ER{\alpha}$ 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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