In vitro estrogenic activity of Achillea millefolium L

Phytomedicine. 2007 Feb;14(2-3):147-52. doi: 10.1016/j.phymed.2006.05.005. Epub 2006 Jul 24.

Abstract

Isolation and biological characterization of pure compounds was used to identify and characterize estrogenic activity and estrogen receptors (ER) preference in chemical components of Achillea millefolium. This medicinal plant is used in folk medicine as an emmenagogue. In vitro assay, based on recombinant MCF-7 cells, showed estrogenic activity in a crude extract of the aerial parts of A. millefolium. After fractionation of the crude extract with increasing polar solvents, estrogenic activity was found in the methanol/water fraction. Nine compounds were isolated and characterized by HR-MS spectra and 1D- and 2D-NMR techniques. In particular, dihydrodehydrodiconiferyl alcohol 9-O-beta-D-glucopyranoside - a glycosyl-neolignan - was isolated for the first time from the genus Achillea in addition to six flavone derivatives, apigenin, apigenin-7-O-beta-D-glucopyranoside, luteolin, luteolin-7-O-beta-D-glucopyranoside, luteolin-4'-O-beta-D-glucopyranoside, rutin, and two caffeic acid derivatives, 3,5-dicaffeoylquinic acid and chlorogenic acid. Apigenin and luteolin, the most important estrogenic compounds among those tested, were studied for their ability to activate alpha or beta estrogen receptors (ERalpha, ERbeta) using transiently transfected cells. Our results suggest that isolation and biological characterization of estrogenic compounds in traditionally used medicinal plants could be a first step in better assessing further (e.g. in vivo) tests of nutraceutical and pharmacological strategies based on phytoestrogens.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Achillea*
  • Cells, Cultured / drug effects
  • Estrogen Receptor alpha / drug effects*
  • Estrogen Receptor beta / drug effects*
  • Female
  • Humans
  • In Vitro Techniques
  • Phytoestrogens / administration & dosage
  • Phytoestrogens / chemistry
  • Phytoestrogens / pharmacology*
  • Phytoestrogens / therapeutic use
  • Phytotherapy*
  • Plant Components, Aerial
  • Plant Extracts / administration & dosage
  • Plant Extracts / chemistry
  • Plant Extracts / pharmacology*
  • Plant Extracts / therapeutic use

Substances

  • Estrogen Receptor alpha
  • Estrogen Receptor beta
  • Phytoestrogens
  • Plant Extracts