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. Epub 2021 Mar 9.

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Cell Line, Tumor
  • Chromatography, High Pressure Liquid
  • Drugs, Chinese Herbal / chemistry
  • Drugs, Chinese Herbal / metabolism
  • Estrogens
  • Estrone / chemistry*
  • Gallic Acid / analogs & derivatives*
  • Gallic Acid / chemistry
  • Gallic Acid / pharmacology
  • Glucosides / chemistry
  • Hormone Replacement Therapy
  • Humans
  • Monoterpenes / chemistry
  • Paeonia / chemistry
  • Paeonia / metabolism
  • Protein Binding
  • Structure-Activity Relationship

Substances

  • Drugs, Chinese Herbal
  • Estrogens
  • Glucosides
  • Monoterpenes
  • moutan cortex
  • peoniflorin
  • ethyl gallate
  • Estrone
  • benzoylpaeoniflorin
  • oxypaeoniflora
  • Gallic Acid