Establishment of a luciferase assay-based screening system for detecting estrogen receptor agonists in plant extracts

In order to effectively treat osteoporosis and other bone-loss disorders, small compounds that could induce bone formation are needed. The present study attempted to establish a screening system for detecting estrogenic activity of compounds, which probably have anti-osteoporosis effects. For this purpose, we established osteoblastic-like MG63 cells stably transfected with the PGL3 reporter gene driven by a promoter consisting of three estrogen response elements (EREs). Using this system, we screened numerous plant extracts, and found several which displayed bioactivity. We conclude that the MG63 cells with estrogen-specific reporter plasmids (MG63-pERE) are useful for high-throughput screening of estrogen receptor agonists from plants which may have favorable potency and could be developed into novel anti-osteoporosis drugs.

► This study established a high-throughput screening system based on estrogen receptors. ► 11 extracts with high ERE-luciferase activity were detected from 500 plant extracts. ► Among them eight extracts were substantiated to possess estrogen activity. ► This system is useful for screening of phytoestrogens.