Natural Product Sciences

  • 제25권1호
  • /
  • Pages.28-33
  • /
  • 2019
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  • 1226-3907(pISSN)
  • /
  • 2288-9027(eISSN)
한국생약학회 (The Korean Society of Pharmacognosy)
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Estrogenic Activity of Sanguiin H-6 through Activation of Estrogen Receptor α Coactivator-binding Site

  • Trinh, Tuy An (College of Korean Medicine, Gachon University) ;
  • Park, Eun-Ji (Department of Obstetrics and Gynaecology, College of Korean Medicine, Daejeon University) ;
  • Lee, Dahae (School of Pharmacy, Sungkyunkwan University) ;
  • Song, Ji Hoon (Department of Medicine, University of Ulsan College of Medicine) ;
  • Lee, Hye Lim (Department of Pediatrics, College of Korean Medicine, Daejeon University) ;
  • Kim, Ki Hyun (School of Pharmacy, Sungkyunkwan University) ;
  • Kim, Younghoon (Pharminogene Inc.) ;
  • Jung, Kiwon (Institute of Pharmaceutical Sciences, College of Pharmacy, CHA University) ;
  • Kang, Ki Sung (College of Korean Medicine, Gachon University) ;
  • Yoo, Jeong-Eun (Department of Obstetrics and Gynaecology, College of Korean Medicine, Daejeon University)
  • 투고 : 2018.04.30
  • 심사 : 2018.10.03
  • 발행 : 2019.03.31
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초록

A popular approach for the study of estrogen receptor ${\alpha}$ inhibition is to investigate the protein-protein interaction between the estrogen receptor (ER) and the coactivator surface. In our study, we investigated phytochemicals from Rubus coreanus that were able to disrupt $ER{\alpha}$ and coactivator interaction with an $ER{\alpha}$ antagonist. The E-screen assay and molecular docking analysis were performed to evaluate the effects of the estrogenic activity of R. coreanus extract and its constituents on the MCF-7 human breast cancer cell line. At $100{\mu}g/mL$, R. coreanus extract significantly stimulated cell proliferation ($574.57{\pm}8.56%$). Sanguiin H6, which was isolated from R. coreanus, demonstrated the strongest affinity for the $ER{\alpha}$ coactivator-binding site in molecular docking analysis, with a binding energy of -250.149. The initial results of the study indicated that sanguiin H6 contributed to the estrogenic activity of R. coreanus through the activation of the $ER{\alpha}$ coactivator-binding site.

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