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

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

  • Food Chem. 2011 Nov 15;129(2):408-416. doi: 10.1016/j.foodchem.2011.04.092.
Hong Wang 1 Ming-Cong Li 2 Jing Yang 3 Dan Yang 4 Yan-Fang Su 5 Guan-Wei Fan 3 Yan Zhu 6 Xiu-Mei Gao 7 Rodolfo Paoletti 8
Affiliations

Affiliations

  • 1 Key Laboratory of Pharmacology of Traditional Chinese Medical Formulae, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin, China; Tianjin State Key Laboratory of Modern Chinese Medicine, Tianjin, China. Electronic address: wanghongsys@126.com.
  • 2 Tianjin Key Laboratory of Traditional Chinese Medicine Pharmacology, Tianjin, China.
  • 3 Key Laboratory of Pharmacology of Traditional Chinese Medical Formulae, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
  • 4 Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, China.
  • 5 Key Laboratory of Pharmacology of Traditional Chinese Medical Formulae, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin, China; School of Pharmaceutical Science and Technology, Tianjin University, Tianjin, China.
  • 6 Key Laboratory of Pharmacology of Traditional Chinese Medical Formulae, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin, China; Tufts University School of Medicine, Boston, USA.
  • 7 Key Laboratory of Pharmacology of Traditional Chinese Medical Formulae, Ministry of Education, Tianjin University of Traditional Chinese Medicine, Tianjin, China. Electronic address: gaoxiumei@tjutcm.edu.cn.
  • 8 Department of Pharmacological Sciences, University of Milan, Italy.
Abstract

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-β-d-glucopyranoside, pinoresinol di-O-β-d-glucopyranoside, aucubin, wogonin, baicalein, and α-O-β-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 (α vs. β) selectivity. Cell proliferation and ER subcellular localisation analyses also demonstrated that they mediated the estrogenic effects by the genomic action of ERα. 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.

Keywords

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

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