Assessment of androgen receptor agonistic/antagonistic effects on 25 chemicals in household applicants by OECD in vitro stably transfected transcriptional activation assays

Chemosphere. 2018 Jan:191:589-596. doi: 10.1016/j.chemosphere.2017.10.084. Epub 2017 Oct 14.

Abstract

The aim of this study is to assess the androgen receptor (AR) agonistic/antagonistic effects on various chemicals, which are used in household products including cleaning agents and wetted tissues by in vitro OECD test guideline No. 458 (using AR-EcoScreen™ cell line) and the me-too test method (using 22Rv1cell line), which was adopted as OECD project No. 4.99. All chemicals were not determined as AR agonists. However α-dodecyl-ω-hydroxypoly (oxyethylene) and 3-iodo-2-propynyl butylcarbamate have shown a weak AR antagonistic effects with IC50 values of 2.18 ± 0.12 and 4.26 ± 0.17 μg/ml via binding affinity to AR in only 22Rv1/mouse mammary tumor virus using AR transcriptional activation assay, because of their different cytotoxicity on each applied cell line. This report firstly provides information about agonistic/antagonistic effects against human AR of various chemicals including surfactants and biocides by OECD in vitro stably transfected transcriptional activation assays. However, further in vivo and human model studies are needed to confirm their adverse effects.

Keywords: Agonist; Antagonist; Human androgen receptor; OECD test guideline; Transcriptional activation assay.

MeSH terms

  • Androgen Receptor Antagonists / pharmacology*
  • Androgens / pharmacology*
  • Animals
  • Biological Assay / methods
  • Cell Line
  • Household Products / analysis*
  • Humans
  • Organisation for Economic Co-Operation and Development
  • Receptors, Androgen / drug effects*
  • Transcriptional Activation*
  • Transfection

Substances

  • AR protein, human
  • Androgen Receptor Antagonists
  • Androgens
  • Receptors, Androgen