Affinity for Thyroid Hormone and Estrogen Receptors of Hydroxylated Polybrominated Diphenyl Ethers
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概要
- 論文の詳細を見る
The affinity for thyroid hormone receptor (TR) of polybromodiphenyl ethers (PBDEs) and hydroxylated PBDEs was examined. 4-Hydroxy-2,2',3,4',5-pentabromodiphenyl ether (4-OH-BDE-90) and 3-hydroxy-2,2',4,4'-tetrabromodiphenyl ether (3-OH-BDE-47) markedly inhibited the binding of triiodothyronine (1×10^<-10>M) to TR in the concentration range of 1×10^<-6>-1×10^<-4>M. 2,3,4,5,6-Pentabromophenol (PBP) also showed an inhibitory effect at 1×10^<-5>-1×10^<-4>M. However, 2,2',3,4,4',5'-hexabromodiphenyl ether (BDE-138), decabromodiphenyl ether (DBDE), 4-methoxy-2,2',3,4',5-pentabromodiphenyl ether (4-MeO-BDE-90), 4'-hydroxy-2,2',4,5'-tetrabromodiphenyl ether(4'-OH-BDE-49), 4-hydroxy-2,2',3,4'-tetrabromodiphenyl ether (4-OH-BDE-42), 4'-hydroxy-2,2',4-tribromodiphenyl ether (4'-OH-BDE-17), 3'-hydroxy-2,4-dibromodiphenyl ether(3'-OH-BDE-7), 2,4,6-tribromophenol (TBP) and tetrabromohydroquinone (TBHQ) did not show affinity for TR. In contrast,4'-OH-BDE-17 and 3'-OH-BDE-7 exhibited estrogenic activity in estrogen-responsive reporter assay using MCF-7 cells at the concentration of 1×10^<-5>M. However, adjacent bromo substitution of 3- or 4-hydroxylated PBDEs markedly decreased the estrogenic activity. These results suggest that hydroxylated PBDEs act as thyroid hormone-like agents, as well as estrogens, that a 4- or 3-hydroxyl group in PBDEs is essential for thyroid hormonal and estrogenic activities, and that adjacent dibromo substitution favors thyroid hormonal activity, but not estrogenic activity.
- 公益社団法人日本薬学会の論文
- 2008-10-01
著者
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OHTA Shigeru
Graduate School of Biomedical Sciences, Hiroshima University
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FURUNO Nobuaki
Institute for Amphibian Biology, Graduate School of Science, Hiroshima University
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Shigeyuki Kitamura
Nihon Pharmaceutical University
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Kitamura Shigeyuki
広島大学 医学部総合薬学科生体機能分子動態学
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Kitamura Shigeyuki
広島大学 総合薬
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Kitamura Shigeyuki
広島大学原爆放射能医学研究所
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KITAMURA Shigeyuki
Graduate School of Biomedical Science, Hiroshima University
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Furuno Nobuaki
Institute For Amphibian Biology Graduate School Of Science Hiroshima University
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Sanoh Seigo
Graduate School Of Biomedical Sciences Hiroshima University
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Sugihara Kazumi
Graduate School of Biomedical Sciences, Hiroshima University
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Sugihara K
Graduate School Of Biomedical Sciences Hiroshima University
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Fujimoto Nariaki
Research Institute For Radiation Biology And Medicine Hiroshima University
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Shinohara Seiji
Graduate School of Biomedical Sciences, Hiroshima University
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Iwase Eri
Graduate School of Biomedical Sciences, Hiroshima University
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Uramaru Naoto
Graduate School of Biomedical Sciences, Hiroshima University
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Shigematsu Hidenari
Nihon Pharmaceutical University
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Fujimoto Nariaki
Graduate School of Biomedical Sciences, Hiroshima University
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Ohta S
Graduate School Of Biomedical Sciences Hiroshima University
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Kitamura Shigeyuki
Institute Of Pharmaceutical Science. Hiroshima University School Of Medicine
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Iwase Eri
Graduate School Of Biomedical Sciences Hiroshima University
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Uramaru Naoto
Graduate School Of Biomedical Sciences Hiroshima University:nihon Pharmaceutical University
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Fujimoto N
Research Institute For Radiation Biology And Medicine Hiroshima University
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Ohta Shigeru
Graduate School Of Biomedical Sciences Hiroshima Univ.
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Kitamura Shigeyuki
Graduate School Of Bioagricultural Sciences Nagoya University
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SUGIHARA Kazumi
Graduate School of Biomedical and Health Sciences, Hiroshima University
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