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: 3.63). 07/2007; 221(3):278-84. DOI: 10.1016/j.taap.2007.03.015
Source: PubMed

ABSTRACT 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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    ABSTRACT: A homeostasis of the glucocorticoid and androgen endocrine system is essential to human health. Their disturbance can lead to various diseases, for example cardiovascular, inflammatory and autoimmune diseases, infertility, cancer. Fifteen widely used industrial chemicals that disrupt endocrine activity were selected for evaluation of potential (anti)glucocorticoid and (anti)androgenic activities. The human breast carcinoma MDA-kb2 cell line was utilized for reporter gene assays, since it expresses both the androgen and the glucocorticoid-responsive reporter. Two new antiandrogens, 4,4′-sulfonylbis(2-methylphenol) (dBPS) and 4,4′-thiodiphenol (THIO), and two new antiglucocorticoids, bisphenol Z and its analog bis[4-(2-hydroxyethoxy)phenyl] sulfone (BHEPS) were identified. Moreover, four new glucocorticoid agonists (methyl paraben, ethyl paraben, propyl paraben and bisphenol F) were found. To elucidate the structure-activity relationship of bisphenols, we performed molecular docking experiments with androgen and glucocorticoid receptor. These docking experiments had shown that bulky structures such as BHEPS and bisphenol Z act as antiglucocorticoid, because they are positioned towards helix H12 in the antagonist conformation and could therefore be responsible for H12 conformational change and the switch between agonistic and antagonistic conformation of receptor. On the other hand smaller structures cannot interact with H12. The results of in vitro screening of fifteen industrial chemicals as modulators of the glucocorticoid and androgen receptor activities demand additional in vivo testing of these chemicals for formulating any relevant hazard identification to human health.
    Toxicology in Vitro 09/2014; 29(1):8-15. DOI:10.1016/j.tiv.2014.08.009 · 3.21 Impact Factor
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    ABSTRACT: In this presentation, results from screening of biocides in the Swedish environment performed by the Swedish Environmental Protection Agency (Naturvårdsverket) between the years 2000-2013 have been compiled, analysed and discussed. The biocides have been divided into General biocides, Rodenticides and Organic tin compounds. A biocide can be defined as a substance that can kill living organisms and is often assigned a prefix addressing the target organism. Biocides can be divided into pesticides [e.g. fungicides (fungi), herbicides (plants), rodenticides (rodents)] and antimicrobial micro-biocides [e.g. bactericides (bacteria)]. The use of biocides is broad in the community, e.g. in industrial applications, in consumer products and as pesticides. Biocidal substances are defined in legislation as chemical or biological products that are used to protect or suppress organisms that are harmful to human or animal health, or that cause damage to natural or manufactured materials. Biocides can be used either in biocidal products or in plant protection products. Examples of biocidal products are insect repellents, disinfectants and industrial chemicals like anti-fouling paints for ships and material preservatives. However, because of their intrinsic properties biocides can pose risks to humans, animals and the environment. This compilation shows data from investigations between the years 2000-2013 of the presence of 56 different biocides used in biocidal products in the Swedish environment. Some of the biocidal products are also used as plant protection products. The different biocides have also been thoroughly described concerning use, legislation/ regulation, physical and environmental properties, dissemination and health concerns. If risks from the former or present use of biocides have been identified for man and/or environment fully detailed propositions for actions are presented.
    1st 10/2014; Swedish Environmental Protection Agency, Naturvårdsverket., ISBN: 978-91-620-6634-5

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