Evaluation of <i>in vitro</i> screening system for estrogenicity: comparison of stably transfected human estrogen receptor-α transcriptional activation (OECD TG455) assay and estrogen receptor (ER) binding assay

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  • Lee Hae Kyung
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea
  • Kim Tae Sung
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea
  • Kim Chang Yeong
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea
  • Kang Il Hyun
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea
  • Kim Mi Gyeong
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea
  • Kyung Jung Ki
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea
  • Kim Hyung Sik
    College of Pharmacy, Pusan National University, Korea
  • Han Soon Young
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea
  • Yoon Hae Jung
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea
  • Rhee Gyu Seek
    Health Effects Analysis Team, National Institute of Food and Drug Safety Evaluation, Korea

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  • 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

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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 (PC50, 4.32 x 10-6 M), 5,000-fold (PC50, 1.26 x 10-7 M) and 120,000-fold (PC50, 2.92 x 10-6 M) less than 17β-estradiol (PC50, 2.43 x 10-11M), 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 (IC50, 4.91 x 10-4 M), 8000-fold (IC50, 1.92 x 10-5 M) and 1400-fold (IC50, 3.34 x 10-6 M) less than 17β-estradiol (IC50, 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.

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