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Title: Prenylflavonoid icariin induces estrogen response element-independent estrogenic responses in a tissue-selective manner
Authors: Zhou, L 
Poon, CCW 
Wong, KY 
Cao, S 
Yu, W 
Dong, X 
Lee, WYW
Zhang, Y
Wong, MS 
Issue Date: Feb-2020
Source: Journal of the Endocrine Society, Feb. 2020, v. 4, no. 2, bvz025, p. 1-17
Abstract: Icariin, a flavonoid phytoestrogen derived from Herba epimedii, has been reported to exert estrogenic effects in bone and activate phosphorylation of estrogen receptor (ER) a in osteoblastic cells. However, it is unclear whether icariin selectively exerts estrogenic activities in bone without inducing undesirable effects in other estrogen-sensitive tissues. The present study aimed to investigate the tissue-selective estrogenic activities of icariin in estrogen-sensitive tissues in vivo and in vitro. Longterm treatment with icariin effectively prevented bone of ovariectomized (OVX) rats from estrogen deficiency-induced osteoporotic changes in bone structure, bone mineral density, and trabecular properties. Moreover, icariin regulated the transcriptional events of estrogen-responsive genes related to bone remodeling and prevented dopaminergic neurons against OVX-induced changes by rescuing expression of estrogen-regulated tyrosine hydroxylase and dopamine transporter in the striatum. Unlike estrogen, icariin did not induce estrogenic effects in the uterus and breast in mature OVX rats or immature CD-1 mice. In vitro studies demonstrated that icariin exerted estrogen-like activities and regulated the expression of estrogen-responsive genes but did not induce estrogen response element- dependent luciferase activities in ER-positive cells. Our results support the hypothesis that icariin, through its distinct mechanism of actions in activating ER, selectively exerts estrogenic activities in different tissues and cell types.
Keywords: Phytoestrogens
Estrogenic activity
Estrogen receptor
Estrogen deficiency
Publisher: Oxford published on behalf of Endocrine Society
Journal: Journal of the Endocrine Society 
EISSN: 2472-1972
DOI: 10.1210/jendso/bvz025
Rights: © Endocrine Society 2019.
This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial-NoDerivs licence (, which permits non-commercial reproduction and distribution of the work, in any medium, provided the original work is not altered or transformed in any way, and that the work is properly cited. For commercial re-use, please contact
The following publication Liping Zhou, Christina Chui-Wa Poon, Ka-Ying Wong, Sisi Cao, Wenxuan Yu, Xiaoli Dong, Wayne Yuk-Wai Lee, Yan Zhang, Man-Sau Wong, Prenylflavonoid Icariin Induces Estrogen Response Element–Independent Estrogenic Responses in a Tissue-Selective Manner, Journal of the Endocrine Society, Volume 4, Issue 2, February 2020, bvz025 is available at
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