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J.Health Sci., 47(5), 495-501, 2001
Several Environmental Pollutants Have Binding Affinities for Both Androgen Receptor and Estrogen Receptor alpha
Kanako Satoh,* Fumiko Nagai, and Naoto Aoki
Department of Toxicology, The Tokyo Metropolitan Research Laboratory of Public Health, 24-1, Hyakunincho 3-chome, Shinjuku-ku, Tokyo 169-0073, Japan
We determined the binding affinities of some chemicals suspected of having endocrine-disrupting effects for androgen and/or estrogen receptors (ADR and ER alpha) 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 ER alpha. 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 ER alpha (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 ER alpha, 7.0×10-5 M). Although 4-octylphenol had a low affinity for ADR, it had a high affinity for ER alpha (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 ER alpha. 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 ER alpha. These findings suggest that some chemicals possess binding affinities for ADR and ER alpha. It is necessary to examine the effects of substances on various hormone receptors to elucidate their endocrine-disrupting activities.
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