title: Evaluation of in vitro screening system for estrogenicity: comparison of stably transfected human estrogen receptor-α transcriptional activation (OECD TG455) assay and estrogen receptor (ER) binding assay.
abstract: The estrogenic activity of industrial chemicals, di(2-ethylhexyl) phthalate (DEHP), di(n-butyl) phthalate (DBP), benzylbutyl phthalate (BBP), diethyl phthalate (DEP), tetrabromobisphenol A (TBBPA), bisphenol A (BPA), and nonylphenol (NP), was compared using OECD test guideline 455(TG455), stably transfected transcriptional activation (STTA) and estrogen receptor (ER) binding assays. The estrogenic activity of BBP, BPA and NP were approximately 180,000-fold (PC(50), 4.32 x 10(-6 )M),  5,000-fold (PC(50), 1.26 x 10(-7) M) and 120,000-fold (PC(50), 2.92 x 10(-6 )M) less than 17β-estradiol (PC(50), 2.43 x 10(-11)M), whereas DEHP, DBP and DEP did not show any estrogenicity activity in the STTA assay. Moreover, binding affinities to human ERα of BBP, BPA, and NP were approximately 200,000-fold (IC(50), 4.91 x 10(-4) M), 8000-fold (IC(50), 1.92 x 10(-5) M) and 1400-fold (IC(50), 3.34 x 10(-6) M) less than 17β-estradiol (IC(50), 2.45 x 10(-9) M) in competitive human ERα binding assay. The relative potencies of STTA assay were very similar to ER binding, E-screen, and Yeast screening assays. Therefore, our results suggested that OECD test guideline TG455 may be useful as a screening test for potential endocrine disruptors.
authors.forename: Hae Kyung
authors.initials: HK
authors.lastname: Lee
authors.forename: Tae Sung
authors.initials: TS
authors.lastname: Kim
authors.forename: Chang Yeong
authors.initials: CY
authors.lastname: Kim
authors.forename: Il Hyun
authors.initials: IH
authors.lastname: Kang
authors.forename: Mi Gyeong
authors.initials: MG
authors.lastname: Kim
authors.forename: Ki Kyung
authors.initials: KK
authors.lastname: Jung
authors.forename: Hyung Sik
authors.initials: HS
authors.lastname: Kim
authors.forename: Soon Young
authors.initials: SY
authors.lastname: Han
authors.forename: Hae Jung
authors.initials: HJ
authors.lastname: Yoon
authors.forename: Gyu Seek
authors.initials: GS
authors.lastname: Rhee
mesh_terms: D001559:Benzhydryl Compounds; D001667:Binding, Competitive; D001681:Biological Assay; D047628:Estrogen Receptor alpha / Q000235:genetics / Q000378:metabolism*; D004967:Estrogens / Q000378:metabolism*; D006367:HeLa Cells; D006801:Humans; D010636:Phenols / Q000378:metabolism*; D010795:Phthalic Acids / Q000378:metabolism*; D011075:Polybrominated Biphenyls / Q000633:toxicity*; D011994:Recombinant Proteins / Q000378:metabolism; D015533:Transcriptional Activation; D000098826:Bisphenol A Compounds
chemical_list: D001559:Benzhydryl Compounds; D047628:Estrogen Receptor alpha; D004967:Estrogens; D010636:Phenols; D010795:Phthalic Acids; D011075:Polybrominated Biphenyls; D011994:Recombinant Proteins; C506487:ESR1 protein, human; C025256:nonylphenol; C020806:tetrabromobisphenol A; C006780:bisphenol A; D000098826:Bisphenol A Compounds