PMID- 22467034 OWN - NLM STAT- MEDLINE DCOM- 20120807 LR - 20210816 IS - 1880-3989 (Electronic) IS - 0388-1350 (Linking) VI - 37 IP - 2 DP - 2012 TI - Evaluation of in vitro screening system for estrogenicity: comparison of stably transfected human estrogen receptor-alpha transcriptional activation (OECD TG455) assay and estrogen receptor (ER) binding assay. PG - 431-7 AB - 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 17beta-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 ERalpha 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 17beta-estradiol (IC(50), 2.45 x 10(-9) M) in competitive human ERalpha 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. FAU - Lee, Hae Kyung AU - Lee HK FAU - Kim, Tae Sung AU - Kim TS FAU - Kim, Chang Yeong AU - Kim CY FAU - Kang, Il Hyun AU - Kang IH FAU - Kim, Mi Gyeong AU - Kim MG FAU - Jung, Ki Kyung AU - Jung KK FAU - Kim, Hyung Sik AU - Kim HS FAU - Han, Soon Young AU - Han SY FAU - Yoon, Hae Jung AU - Yoon HJ FAU - Rhee, Gyu Seek AU - Rhee GS LA - eng PT - Letter PT - Research Support, Non-U.S. Gov't PL - Japan TA - J Toxicol Sci JT - The Journal of toxicological sciences JID - 7805798 RN - 0 (Benzhydryl Compounds) RN - 0 (ESR1 protein, human) RN - 0 (Estrogen Receptor alpha) RN - 0 (Estrogens) RN - 0 (Phenols) RN - 0 (Phthalic Acids) RN - 0 (Polybrominated Biphenyls) RN - 0 (Recombinant Proteins) RN - 79F6A2ILP5 (nonylphenol) RN - FQI02RFC3A (tetrabromobisphenol A) RN - MLT3645I99 (bisphenol A) SB - IM MH - Benzhydryl Compounds MH - Binding, Competitive MH - Biological Assay MH - Estrogen Receptor alpha/genetics/*metabolism MH - Estrogens/*metabolism MH - HeLa Cells MH - Humans MH - Phenols/*metabolism MH - Phthalic Acids/*metabolism MH - Polybrominated Biphenyls/*toxicity MH - Recombinant Proteins/metabolism MH - Transcriptional Activation EDAT- 2012/04/03 06:00 MHDA- 2012/08/08 06:00 CRDT- 2012/04/03 06:00 PHST- 2012/04/03 06:00 [entrez] PHST- 2012/04/03 06:00 [pubmed] PHST- 2012/08/08 06:00 [medline] AID - JST.JSTAGE/jts/37.431 [pii] AID - 10.2131/jts.37.431 [doi] PST - ppublish SO - J Toxicol Sci. 2012;37(2):431-7. doi: 10.2131/jts.37.431.