Several environmental pollutants have binding affinities for both androgen receptor and estrogen receptor alpha | Health & Environmental Research Online (HERO)

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Citation
Tags

HERO ID

1337854

Reference Type

Journal Article

Title

Several environmental pollutants have binding affinities for both androgen receptor and estrogen receptor alpha

Author(s)

Satoh, K; Nagai, F; Aoki, N

Year

2001

Is Peer Reviewed?

Yes

Journal

Journal of Health Science
ISSN: 1344-9702
EISSN: 1347-5207

Publisher

Pharmaceutical Society of Japan, Nihon Yakugakkai

Location

Tokyo

Volume

Issue

Page Numbers

495-501

Language

English

DOI

10.1248/jhs.47.495

Web of Science Id

WOS:000171263000012

URL

https://search.proquest.com/docview/18255929?accountid=171501
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Abstract

We determined the binding affinities of some chemicals suspected of having endocrine-disrupting effects for androgen and/or estrogen receptors (ADR and ERα) by a non-radioisotope (RI) receptor binding assay. Tributyltin had the highest binding affinity for ADR with an IC50 of 7.6 × 10-6 M, but no affinity for ERα. Bisphenol A and 4-nonylphenol strongly bound to both ADR (IC50 values of 7.9 × 10-6 and 1.3 × 10-5 M, respectively) and ERα (IC50 values of 7.8 × 10-6 and 7.2 × 10-7 M, respectively). Octachlorostyrene had affinity for both receptors (IC50 for ADR, 2.7 × 10-5 M; and for ERα, 7.0 × 10-5 M). Although 4-octylphenol had a low affinity for ADR, it had a high affinity for ERα (IC50 of 9.8 × 10-6 M). Di-n-butyl phthalate, dicyclohexyl phthalate, and di(2-ethylhexyl)phthalate had low affinities for both ADR and ERα. The affinity of benzophenone was low for both receptors and n-butylbenzene had no affinity for either. Styrene trimers such as 1a-phenyl-4a-(1'-phenylethyl)tetralin (ST-2), 1a-phenyl-4e-(1'-phenylethyl)tetralin (ST-3), 1e-phenyl-4a-(1'-phenylethyl)tetralin (ST-4), and 1e-phenyl-4e-(1'-phenylethyl)tetralin (ST-5) had relatively high affinities, with IC50 values of 1.2-3.1 × 10-5 M. Styrene dimers showed lower affinities for ADR than the trimers. Some styrene oligomers have been previously reported to have binding affinities for ERα. These findings suggest that some chemicals possess binding affinities for ADR and ERα. It is necessary to examine the effects of substances on various hormone receptors to elucidate their endocrine-disrupting activities.

Keywords

endocrine disrupter; androgen receptor; estrogen receptor; tributyltin; styrene oligomer