Antiandrogenic properties of parabens and other phenolic containing small molecules in personal care products

Center for Health and the Environment, University of California, Davis, CA 95616, USA.
Toxicology and Applied Pharmacology (Impact Factor: 3.71). 07/2007; 221(3):278-84. DOI: 10.1016/j.taap.2007.03.015
Source: PubMed


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 microM, 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 microM, and 38.8% at a concentration of 1.0 microM (P<0.05). Thirty-four percent of T-induced transcriptional activity was inhibited by thymol at 10 microM (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.

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Available from: Shirley J Gee, Sep 22, 2014
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    • "Based on the results from simultaneous exposure of MDA-kb2 cells to BuPB and 250 pM DHT an IC 01 of 17.3 μM was reported (Orton et al., 2014). BuPB at 10 μM (highest concentration evaluated) inhibited the testosterone (T) (125 pM) induced transcriptional activity in HEK293 cells (human embryonic kidney cells) by 19% (Chen et al., 2007). The AR binding affinity of BuPB (190 μM BuPB) partially prevented the binding of T to the AR (Satoh et al., 2005). "
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    • "BiomolTher 24(1), 99-107 (2016).2015.164 al., 2004Jacobs et al., 2005;Veldhoen et al., 2006;Chen et al., 2007;Ahn et al., 2008;Paul et al., 2010;Rodriguez and Sanchez, 2010) may offer hints that it may actually occur in humans, especially with regular exposures to various products with direct contact or entry to the body. Triclosan was found in the plasma and milk in nursing mothers regularly consuming products containing this ingredient (Allmyr et al., 2006). "
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    • "Public interest has been steadily increasing in the ubiquitous sources of exposure to this chemical. The hormonal activity of triclosan has not been clearly established owing to conflicting results from different investigations, including evidence of weak estrogenic (Chen et al. 2007; Svobodová et al. 2009) and androgenic activity (Chen et al. 2007), estrogen receptor antagonism (Ahn et al. 2008), and antiandrogenic properties (Chen et al. 2007). The excretion half-life of triclosan has been estimated as 11 hr for urine and 21 hr for plasma (Sandborgh-Englund et al. 2006). "
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