4.7 Article

Estrogenic properties of six compounds derived from Eucommia ulmoides Oliv. and their differing biological activity through estrogen receptors α and β

Journal

FOOD CHEMISTRY
Volume 129, Issue 2, Pages 408-416

Publisher

ELSEVIER SCI LTD
DOI: 10.1016/j.foodchem.2011.04.092

Keywords

Eucommia ulmoides Oliv.; Phytoestrogen; Estrogen receptor (ER); Nutraceutical supplement; Herbal medicine

Funding

  1. National Science Foundation of China [30701093]
  2. Science and Technology Ministry [2008DFB30070]
  3. National Program for Key Basic Research Projects [2005CB523404]
  4. International Science and Technology supportive Project of China [2009ZX09311-002]
  5. Tianjin S&T Development Fund projects for Colleges and Universities [20090223]
  6. Tianjin Applied Basic Research and Frontier Technological Program [11JCZDJC21100]
  7. National Natural Science Foundation of China [81001659]

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Eucommia ulmoides Oliv. (Du-zhong), a well known Chinese herbal medicine, has been increasingly used as a nutraceutical supplement. The aim of this study was to identify and characterise novel estrogenic compounds in E. ulmoides. We report that six compounds, namely pinoresinol 4'-O-beta-D-glucopyranoside, pinoresinol di-O-beta-D-glucopyranoside, aucubin, wogonin, baicalein, and alpha-O-beta-D-glucopyranosyl-4,2',4'-trihydroxydihydrochalcone, activated estrogen receptor (ER)-dependent transcription of both transfected and endogenous target genes. Strikingly, these compounds exhibited significant difference in ER subtype (alpha vs. beta) selectivity. Cell proliferation and ER subcellular localisation analyses also demonstrated that they mediated the estrogenic effects by the genomic action of ER alpha. This study suggests that E. ulmoides is a rich source of new selective estrogen receptor modulators and evaluations of its health benefit and safety as a food additive should take into account the diverse phytoestrogen activities of the individual components. (C) 2011 Elsevier Ltd. All rights reserved.

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