Journal
TOXICOLOGY AND APPLIED PHARMACOLOGY
Volume 221, Issue 3, Pages 278-284Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.taap.2007.03.015
Keywords
androgen receptor; bioassay; parabens; phenolic moiety; triclosan; thymol
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Funding
- NCRR NIH HHS [P51 RR000169, P51 RR000169-390017] Funding Source: Medline
- NIEHS NIH HHS [R37ES02710, P42 ES004699, P01 ES006198, P30 ES005707, R37 ES002710-26, P42 ES004699-20, P01ES06198, P01 ES006198-10, P42ES04699, P30 ES005707-15, P30ES005707, R37 ES002710] Funding Source: Medline
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To identify the androgenic potency of commonly used antimicrobials, an in vitro androgen receptor-mediated transcriptional activity assay was employed to evaluate the androgenic/antiandrogenic activity of parabens and selected other antimicrobials containing a phenolic moiety. This cell-based assay utilizes a stably transfected cell line that lacks critical steroid metabolizing enzymes and is formatted in a 96-well format. At a concentration of 10 mu M, methyl-, propyl- and butyl-4-hydroxybenzoate (parabens) inhibited testosterone (T)-induced transcriptional activity by 40%, 33% and 19%, respectively (P < 0.05), while 4-hydroxybenzoic acid, the major metabolite of parabens, had no effect on T-induced transcriptional activity. Triclosan inhibited transcriptional activity induced by T by more than 92% at a concentration of 10 mu M, and 38.8% at a concentration of 1.0 pM (P < 0.05). Thirty-four percent of T-induced transcriptional activity was inhibited by thymol at 10 mu M (P < 0.05). Cell proliferation and/or cytotoxicity were not observed in any of the treatments. None of the compounds appeared to be androgenic when tested individually without T. The data presented in this report demonstrate that some widely used antimicrobial compounds have antiandrogenic properties and warrant further investigation to fully understand their potential impact on human reproductive health. (c) 2007 Elsevier Inc. All rights reserved.
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