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

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Abstract

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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Acknowledgements

This research was supported by the National Research Foundation of Korea (NRF) Grant funded by the Korean government (MRC, No. 2011-0030074; NRF-2016K1A1A8A01939090; NRF-2016K2A9A2A06004949).

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Authors and Affiliations

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

    Si-Yeon Jeong, Baojin Zhang, Da-Sol Lim, Joon Young Lee, So-Dam Kim & Yun Seon Song

  2. Department of Biological Sciences, College of Science, Sookmyung Women’s University, Seoul, 04310, Republic of Korea

    Minsun Chang

  3. Natural Medicine Research Center, KRIBB, Chungbuk, 363-883, Republic of Korea

    Sang-ho Choi & Sei-Ryang Oh

  4. Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China

    Hong-Hua Wu, Yan Zhu, Xiu-mei Gao & Xiaoying Wang

  5. Neuroprotection Research Laboratory, Departments of Radiology and Neurology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA, 02129, USA

    Xiaoying Wang

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  1. Si-Yeon Jeong
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Correspondence to Yun Seon Song.

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Jeong, SY., Chang, M., Choi, Sh. et al. Estrogenic effects of phytoestrogens derived from Flemingia strobilifera in MCF-7 cells and immature rats. Arch. Pharm. Res. 41, 519–529 (2018). https://doi.org/10.1007/s12272-018-1027-1

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  • DOI: https://doi.org/10.1007/s12272-018-1027-1

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