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KMID : 0043320180410050519
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Archives of Pharmacal Research
2018 Volume.41 No. 5 p.519 ~ p.529
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Estrogenic effects of phytoestrogens derived from Flemingia strobilifera in MCF-7 cells and immature rats
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Jeong Si-Yeon
Chang Min-Sun
Choi Sang-Ho
Oh Sei-Ryang
Wu Hong-Hua
Zhu Yan
Gao Xiu-Mei
Wang Xiaoying
Zhang Baojin
Lim Da-Sol
Lee Joon-Young
Kim So-Dam
Song Yun-Seon
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Abstract
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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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KEYWORD
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Flemingia strobilifera, Phytoestrogen, Estrogen receptor, ERE transcription, Uterotrophic effect, Immature rat
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