The objective of this study was to compare estrogenic properties of fifteen known phytoestrogens using an estrogen receptor-α (ER-α) dimerization assay and OECD standardized methods including in vitro ER transactivation assay using VM7Luc4E2 cells a...
The objective of this study was to compare estrogenic properties of fifteen known phytoestrogens using an estrogen receptor-α (ER-α) dimerization assay and OECD standardized methods including in vitro ER transactivation assay using VM7Luc4E2 cells and in vivo uterotrophic assay using an immature rat model. Human ER-α dimerization assay and luciferase reporter assay showed consistent results for their estrogenecity. In vivo assay showed increases in uterine weights after treatments with biochanin A, 8-prenylnaringenin, and coumestrol. Their uterotrophic effects were lost when animals were co-treated with antagonist of ER, indicating their ER-dependent effects in the uterus. In addition, analysis of estrogen responsive genes revealed that these phytoestrogens regulated uterine gene expressions differently compared to estrogens. Test methods used in this study could be used as effective screening tools for phytoestrogens. In a separated study, coumestrol prevented OVX-induced adiposity and hepatic lipid accumulation and promoted browning of white fats, demonstrating its beneficial effects for the regulation of postmenopausal metabolic homeostasis.