1. Academic Validation
  2. Estrogenic activity of ethyl gallate and its potential use in hormone replacement therapy

Estrogenic activity of ethyl gallate and its potential use in hormone replacement therapy

  • Bioorg Med Chem Lett. 2021 May 15:40:127919. doi: 10.1016/j.bmcl.2021.127919.
Hesol Lee 1 Sullim Lee 2 Ji Yun Baek 3 Chang-Seob Seo 4 Hwayoung Yun 5 Su-Nam Kim 6 Ki Sung Kang 7 You-Kyung Choi 8
Affiliations

Affiliations

  • 1 Department of Korean International Medicine, College of Korean Medicine, Gachon University, Seongnam 13120, South Korea; Clinical Medicine Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea. Electronic address: haesol89@naver.com.
  • 2 Department of Life Science, College of Bio-Nano Technology, Gachon University, Seongnam 13120, South Korea. Electronic address: sullimlee@gachon.ac.kr.
  • 3 Department of Preventive Medicine, College of Korean Medicine, Gachon University, Seongnam 13120, South Korea. Electronic address: wldbsttn@naver.com.
  • 4 Herbal Medicine Research Division, Korea Institute of Oriental Medicine, Daejeon 34054, South Korea. Electronic address: csseo0914@kiom.re.kr.
  • 5 College of Pharmacy, Pusan National University, Busan 46241, Republic of Korea. Electronic address: hyun@pusan.ac.kr.
  • 6 Natural Products Research Institute, Korea Institute of Science and Technology, Gangneung 25451, Republic of Korea. Electronic address: snkim@kist.re.kr.
  • 7 Department of Preventive Medicine, College of Korean Medicine, Gachon University, Seongnam 13120, South Korea. Electronic address: kkang@gachon.ac.kr.
  • 8 Department of Korean International Medicine, College of Korean Medicine, Gachon University, Seongnam 13120, South Korea. Electronic address: kosmos@gachon.ac.kr.
Abstract

We aimed to compare the estrogenic activities of compounds isolated from Moutan Cortex Radicis (MRC, Paeonia suffruticosa Andrews) and identify their potential use in hormone replacement therapy. We quantified seven marker components (gallic acid, oxypaeoniflorin, paeoniflorin, ethyl gallate, benzoic acid, benzoylpaeoniflorin, and paeonol) in MRC using a high-performance liquid chromatography simultaneous analysis assay. To investigate the estrogenic activity of MRC and the seven marker components, an E-screen assay was conducted using the Estrogen Receptor (ER)-positive MCF-7 human breast Cancer cell line. Among them, ethyl gallate caused cell proliferation in a concentration-dependent manner at concentrations above 25 µM and was clearly suppressed by combination treatment with the ER antagonist ICI 182,780. Therefore, ethyl gallate may be a compound of MRC that can increase the estrogenic effect in ER-positive MCF-7 cells.

Keywords

Estrogen receptor; Ethyl gallate; Hormone replacement therapy.

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