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Estrogenic effects of phytoestrogens from Flemingia strobilifera in MC…

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



Abstract

Phytoestrogen (PE) has received considerable attention due to the physiological signi？cance of its estrogenicity. Flemingia strobilifera(FS) has been used as a folk medicine in Asia for the treatment of in？ammation, 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 (hERa) binding, estrogen response element (ERE)-luciferase reporter assays, and uterotrophic assays. FSE and its compounds 1–5 showed binding af？nities for hERa 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, signi？cant increases in uterine weight and pS2 genewere observed in FSE-treated groups. We identi？ed 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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