Estrogenic effects of phytoestrogens derived from Flemingia strobilifera in MCF-7 cells and immature rats.

Authors:
Si-Yeon Jeong
Si-Yeon Jeong
Sookmyung Women's University
Minsun Chang
Minsun Chang
College of Pharmacy
United States
Sang-Ho Choi
Sang-Ho Choi
University of Ulsan College of Medicine
South Korea
Sei-Ryang Oh
Sei-Ryang Oh
Korea Research Institute of Bioscience and Biotechnology
South Korea
Hong-hua Wu
Hong-hua Wu
Beijing Jishuitan Hospital
China
Yan Zhu
Yan Zhu
Zhejiang University
China
Xiu-Mei Gao
Xiu-Mei Gao
Tianjin University of Traditional Chinese Medicine
China
Xiaoying Wang
Xiaoying Wang
Peking University First Hospital
China

Arch Pharm Res 2018 May 24;41(5):519-529. Epub 2018 May 24.

College of Pharmacy, Sookmyung Women's University, Seoul, 04310, Republic of Korea.

Phytoestrogen (PE) has received considerable attention due to the physiological significance of its estrogenicity. Flemingia strobilifera (FS) has been used as a folk medicine in Asia for the treatment of inflammation, cancer, and infection; however, the estrogenic effects and chemical components of FS have not yet been reported. We aimed to uncover the estrogenic properties and PEs derived from FS using phytochemical and pharmacological evaluation. PEs from FS extract (FSE) were analyzed by NMR, HPLC, and MS. To evaluate estrogenic activity, FSE and its compounds were evaluated by in vitro and in vivo assays, including human estrogen receptor alpha (hERα) binding, estrogen response element (ERE)-luciferase reporter assays, and uterotrophic assays. FSE and its compounds 1-5 showed binding affinities for hERα and activated ERE transcription in MCF-7 cells. Additionally, FSE and compounds 1-5 induced MCF-7 cell proliferation and trefoil factor 1 (pS2) expression. In immature female rats, significant increases in uterine weight and pS2 gene were observed in FSE-treated groups. We identified estrogenic activities of FSE and its bioactive compounds, suggesting their possible roles as PEs via ERs. PEs derived from FSE are promising candidates for ER-targeted therapy for post-menopausal symptoms.

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http://link.springer.com/10.1007/s12272-018-1027-1
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May 2018
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