Effects of pentachlorophenol and hydroxylated polychlorinated biphenyls on thyroid hormone conjugation in a rat and a human hepatoma cell line

作者: A.G Schuur , Å Bergman , A Brouwer , T.J Visser

DOI: 10.1016/S0887-2333(99)00005-3

关键词:

摘要: Abstract It was previously demonstrated in our laboratory that hydroxylated metabolites of polychlorinated biphenyls (PCB-OHs) inhibit the sulfation iodothyronines rat liver cytosol. In this study, inhibition 3,3′-diiodothyronine (T2) by pentachlorophenol (PCP) and PCB-OHs investigated hepatoma cell lines relation to cellular uptake these compounds, providing a more appropriate model vivo situation. The human HepG2 line shown conjugate T2 almost exclusively sulfation, glucuronidation being negligible. FaO line, on other hand, produced 37% sulfate 63% glucuronide. PCP inhibited both lines, although it 103 times less potent cells than Remarkably, 10 μ m same extent. Micromolar concentrations 4-hydroxy-3,3′,4′,5-tetrachlorobiphenyl or 4-hydroxy-2′,3,3′,4′,5-pentachlorobiphenyl hardly affected conjugation cells, but reduced formation cells. Inhibition stronger using medium without foetal calf serum (FCS) with 5% FCS. This due lower inhibitor presence serum, as radiolabelled PCP. conclusion, study confirms observed cytosol line. Thus, seems reasonable assume iodothyronine is also PCB vivo.

参考文章(31)
Henk Koster, Ina Halsema, Egbert Scholtens, John H.N. Meerman, K. Sandy Pang, Gerard J. Mulder, SELECTIVE-INHIBITION OF SULFATE CONJUGATION IN THE RAT - PHARMACOKINETICS AND CHARACTERIZATION OF THE INHIBITORY EFFECT OF 2,6-DICHLORO-4-NITROPHENOL Biochemical Pharmacology. ,vol. 31, pp. 1919- 1924 ,(1982) , 10.1016/0006-2952(82)90498-1
E A Eaton, T Walle, A J Lewis, T Hudson, A A Wilson, U K Walle, Flavonoids, potent inhibitors of the human P-form phenolsulfotransferase. Potential role in drug metabolism and chemoprevention. Drug Metabolism and Disposition. ,vol. 24, pp. 232- 237 ,(1996)
Å. Bergman, E. Klasson Wehler, H. Kuroki, A. Nilsson, Synthesis and mass spectrometry of some methoxylated PCB Chemosphere. ,vol. 30, pp. 1921- 1938 ,(1995) , 10.1016/0045-6535(95)00073-H
E. Klasson Wehler, B. Brunström, U. Rannug, Å. Bergman, 3,3′,4,4′-Tetrachlorobiphenyl: Metabolism by the chick embryo in ovo and toxicity of hydroxylated metabolites Chemico-Biological Interactions. ,vol. 73, pp. 121- 132 ,(1990) , 10.1016/0009-2797(90)90112-Z
Theo J. Visser, Role of sulfation in thyroid hormone metabolism Chemico-Biological Interactions. ,vol. 92, pp. 293- 303 ,(1994) , 10.1016/0009-2797(94)90071-X
Dietmar Utesch, Franz Oesch, Dependency of the in vitro stabilization of differentiated functions in liver parenchymal cells on the type of cell line used for co-culture In Vitro Cellular & Developmental Biology – Animal. ,vol. 28, pp. 193- 198 ,(1992) , 10.1007/BF02631091
Paul G.J. van Stralen, Hans J. van der Hoek, Roel Docter, Marion de Jong, Eric P. Krenning, Chen F. Lim, Georg Hennemann, Reduced T3 deiodination by the human hepatoblastoma cell line HepG2 caused by deficient T3 sulfation. Biochimica et Biophysica Acta. ,vol. 1157, pp. 114- 118 ,(1993) , 10.1016/0304-4165(93)90086-N
Theo J Visser, Ellen Kaptein, Hansruedi Glatt, Ingrid Bartsch, Maria Hagen, Michael W.H Coughtrie, Characterization of thyroid hormone sulfotransferases Chemico-Biological Interactions. ,vol. 109, pp. 279- 291 ,(1998) , 10.1016/S0009-2797(97)00139-7
John H.N. Meerman, Henk M.J. Sterenborg, Gerard J. Mulder, Use of pentachlorophenol as long-term inhibitor of sulfation of phenols and hydroxamic acids in the rat in vivo. Biochemical Pharmacology. ,vol. 32, pp. 1587- 1593 ,(1983) , 10.1016/0006-2952(83)90332-5
Theo J. Visser, Joop C.J. van Buuren, Marja Rutgers, Sebo Jan Eelkman Rooda, Wouter W. de Herder, The role of sulfation in thyroid hormone metabolism Trends in Endocrinology and Metabolism. ,vol. 1, pp. 211- 218 ,(1990) , 10.1016/1043-2760(90)90055-8