Anti-thyroid hormonal activity of tetrabromobisphenol A, a flame retardant, and related compounds: Affinity to the mammalian thyroid hormone receptor, and effect on tadpole metamorphosis
Anti-thyroid hormonal activity of tetrabromobisphenol A, a flame retardant, and related compounds: Affinity to the mammalian thyroid hormone receptor, and effect on tadpole metamorphosis
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DOI：
10.1016/j.lfs.2004.08.030
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发表时间：
2005-02-18
期刊：
影响因子：
6.1
通讯作者：
Kashiwagi, A
中科院分区：
文献类型：
--
作者：
Kitamura, S;Kato, T;Kashiwagi, A
研究了阻燃剂四溴双酚A（TBBPA）及其相关化合物的甲状腺功能破坏活性。TBBPA、四氯双酚A（TCBPA）、四甲基双酚A（TMBPA）和3，3 '-二甲基双酚A（DMBPA）在1 x 10（-7）-1 x 10（-4）M的浓度范围内显着抑制三碘甲状腺原氨酸（T-3; 1 x 10（-10）M）与甲状腺激素受体的结合，而双酚A和2，2-二苯丙烷则无活性。TBBPA、TCBPA、TMBPA和DMBPA在使用甲状腺激素受体α 1或β 1转染的中国仓鼠卵巢细胞系（CHO-K1）进行的甲状腺激素反应性报告基因测定中未显示甲状腺激素活性，TBBPA和TCBPA对T-3活性有明显的抗甲状腺激素作用（1 x 10（-8）M），浓度范围为3 x 10（-6）-5 x 10（-5）M。TBBPA的甲状腺激素干扰活性也被检查在由甲状腺激素刺激的两栖动物变态的影响。TBBPA在1 × 10~（-8）~1 × 10~（-6）M浓度范围内对T-3（5 × 10~（-8）M）-增强的皱纹蛙蝌蚪尾部缩短有抑制作用。这些事实表明，TBBPA，TCBPA，TMBPA和DMBPA可以作为甲状腺激素干扰剂。(C)2004年爱思唯尔公司All rights reserved.
The thyroid hormone-disrupting activity of tetrabromobisphenol A (TBBPA), a flame retardant, and related compounds was examined. TBBPA, tetrachlorobisphenol A (TCBPA), tetramethylbisphenol A (TMBPA) and 3,3'-dimethylbisphenol A (DMBPA) markedly inhibited the binding of triiodothyronine (T-3; 1 x 10(-10) M) to thyroid hormone receptor in the concentration range of 1 x 10(-7)-1 x 10(-4) M, while bisphenol A and 2,2-diphenylpropane were inactive. TBBPA, TCBPA, TMBPA and DMBPA did not exhibit thyroid hormonal activity in a thyroid hormone-responsive reporter assay using a Chinese hamster ovary cell line (CHO-K1) transfected with thyroid hormone receptor alpha1 or beta1, but TBBPA and TCBPA showed significant anti-thyroid hormone effects on the activity of T-3 (1 x 10(-8) M) in the concentration range of 3 x 10(-6) - 5 x 10(-5) M. The thyroid hormone-disrupting activity of TBBPA was also examined in terms of the effect on amphibian metamorphosis stimulated by thyroid hormone. TBBPA in the concentration range of 1 x 10(-8) to 1 x 10(-6) M showed suppressive action on T-3 (5 x 10(-8) M)-enhancement of Rana rugosa tadpole tail shortening. These facts suggest that TBBPA, TCBPA, TMBPA and DMBPA can act as thyroid hormone-disrupting agents. (C) 2004 Elsevier Inc. All rights reserved.