Arch Pharm Res. 2018 May;41(5):519-529. doi: 10.1007/s12272-018-1027-1. Epub 2018 May 24.
Jeong SY1, Chang M2, Choi SH3, Oh SR3, Wu HH4, Zhu Y4, Gao XM4, Wang X4,5, Zhang B1, Lim DS1, Lee JY1, Kim SD1, Song YS6.
Author information
- 1
- College of Pharmacy, Sookmyung Women's University, Seoul, 04310, Republic of Korea.
- 2
- Department of Biological Sciences, College of Science, Sookmyung Women's University, Seoul, 04310, Republic of Korea.
- 3
- Natural Medicine Research Center, KRIBB, Chungbuk, 363-883, Republic of Korea.
- 4
- Institute of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, 300193, China.
- 5
- Neuroprotection Research Laboratory, Departments of Radiology and Neurology, Massachusetts General Hospital, Harvard Medical School, Charlestown, MA, 02129, USA.
- 6
- College of Pharmacy, Sookmyung Women's University, Seoul, 04310, Republic of Korea. yssong@sookmyung.ac.kr.
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.
KEYWORDS:
ERE transcription; Estrogen receptor; Flemingia strobilifera; Immature rat; Phytoestrogen; Uterotrophic effect
- PMID:
- 29797242
- DOI:
- 10.1007/s12272-018-1027-1
- [Indexed for MEDLINE]
