Potent inhibition of estrogen sulfotransferase by hydroxylated PCB metabolites: A novel pathway explaining the estrogenic activity of PCB's

Monique H.A. Kester; Sema Bulduk; Dick Tibboel; Walter Meinl; Hansruedi Glatt; Charles N. Falany; Michael W.H. Coughtrie; A. K.E. Bergman; Stephen H. Safe; George G.J.M. Kuiper; A. Gerlienke Schuur; Abraham Brouwer; Theo J. Visser

doi:10.1210/endo.141.5.7530

Potent inhibition of estrogen sulfotransferase by hydroxylated PCB metabolites: A novel pathway explaining the estrogenic activity of PCB's

Monique H.A. Kester, Sema Bulduk, Dick Tibboel, Walter Meinl, Hansruedi Glatt, Charles N. Falany, Michael W.H. Coughtrie, A. K.E. Bergman, Stephen H. Safe, George G.J.M. Kuiper, A. Gerlienke Schuur, Abraham Brouwer, Theo J. Visser

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353 Scopus citations

Abstract

Polychlorinated biphenyls (PCBs) are persistent environmental pollutants which exert a variety of toxic effects in animals, including disturbances of sexual development and reproductive function. The estrogenic effects of PCBs may be mediated in part by hydroxylated PCB metabolites (PCB-OHs), but the mechanisms by which they are brought about are not understood. PCBs as well as PCB-OHs show low affinities for both α and β estrogen receptor isoforms. In the present study we demonstrate that various environmentally relevant PCB-OHs are extremely potent inhibitors of human estrogen sulfotransferase, strongly suggesting that they indirectly induce estrogenic activity by increasing estradiol bioavailability in target tissues.

Original language	English (US)
Pages (from-to)	1897-1900
Number of pages	4
Journal	Endocrinology
Volume	141
Issue number	5
DOIs	https://doi.org/10.1210/endo.141.5.7530
State	Published - 2000

ASJC Scopus subject areas

Endocrinology

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Kester, M. H. A., Bulduk, S., Tibboel, D., Meinl, W., Glatt, H., Falany, C. N., Coughtrie, M. W. H., Bergman, A. K. E., Safe, S. H., Kuiper, G. G. J. M., Schuur, A. G., Brouwer, A., & Visser, T. J. (2000). Potent inhibition of estrogen sulfotransferase by hydroxylated PCB metabolites: A novel pathway explaining the estrogenic activity of PCB's. Endocrinology, 141(5), 1897-1900. https://doi.org/10.1210/endo.141.5.7530

Kester, MHA, Bulduk, S, Tibboel, D, Meinl, W, Glatt, H, Falany, CN, Coughtrie, MWH, Bergman, AKE, Safe, SH, Kuiper, GGJM, Schuur, AG, Brouwer, A & Visser, TJ 2000, 'Potent inhibition of estrogen sulfotransferase by hydroxylated PCB metabolites: A novel pathway explaining the estrogenic activity of PCB's', Endocrinology, vol. 141, no. 5, pp. 1897-1900. https://doi.org/10.1210/endo.141.5.7530

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AU - Tibboel, Dick

AU - Meinl, Walter

AU - Glatt, Hansruedi

AU - Falany, Charles N.

AU - Coughtrie, Michael W.H.

AU - Bergman, A. K.E.

AU - Safe, Stephen H.

AU - Kuiper, George G.J.M.

AU - Schuur, A. Gerlienke

AU - Brouwer, Abraham

AU - Visser, Theo J.

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AB - Polychlorinated biphenyls (PCBs) are persistent environmental pollutants which exert a variety of toxic effects in animals, including disturbances of sexual development and reproductive function. The estrogenic effects of PCBs may be mediated in part by hydroxylated PCB metabolites (PCB-OHs), but the mechanisms by which they are brought about are not understood. PCBs as well as PCB-OHs show low affinities for both α and β estrogen receptor isoforms. In the present study we demonstrate that various environmentally relevant PCB-OHs are extremely potent inhibitors of human estrogen sulfotransferase, strongly suggesting that they indirectly induce estrogenic activity by increasing estradiol bioavailability in target tissues.

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Potent inhibition of estrogen sulfotransferase by hydroxylated PCB metabolites: A novel pathway explaining the estrogenic activity of PCB's

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