title: Establishment of a luciferase assay-based screening system for detecting estrogen receptor agonists in plant extracts.
abstract: 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.
authors.affiliation: Department of Pharmacognosy, School of Pharmacy, Second Military Medical University, Shanghai 200433, PR China.
authors.forename: Jian
authors.initials: J
authors.lastname: Du
authors.forename: Yan-Jie
authors.initials: YJ
authors.lastname: Wei
authors.forename: Cheng
authors.initials: C
authors.lastname: Peng
authors.forename: Xia
authors.initials: X
authors.lastname: Ran
authors.forename: Hong
authors.initials: H
authors.lastname: Zhang
authors.forename: Yi-Ping
authors.initials: YP
authors.lastname: Jiang
authors.forename: Khalid
authors.initials: K
authors.lastname: Rahman
authors.forename: Lu-Ping
authors.initials: LP
authors.lastname: Qin
mesh_terms: D000818:Animals; D002460:Cell Line; D049109:Cell Proliferation / Q000187:drug effects; D004353:Drug Evaluation, Preclinical / Q000379:methods*; D004958:Estradiol / Q000031:analogs & derivatives / Q000494:pharmacology; D017930:Genes, Reporter / Q000187:drug effects; D057166:High-Throughput Screening Assays / Q000379:methods*; D006801:Humans; D008156:Luciferases / Q000378:metabolism*; D051379:Mice; D010024:Osteoporosis / Q000188:drug therapy; D010936:Plant Extracts / Q000737:chemistry* / Q000494:pharmacology; D011960:Receptors, Estrogen / Q000819:agonists*; D020218:Response Elements / Q000187:drug effects; D014162:Transfection
chemical_list: D010936:Plant Extracts; D011960:Receptors, Estrogen; D004958:Estradiol; D008156:Luciferases