Assessment of thyroid hormone activity of halogenated bisphenol A using a yeast two-hybrid assay

作者：Terasaki Masanori^*; Kosaka Koji; Kunikane Shoichi; Makino Masakazu; Shiraishi Fujio

来源：Chemosphere, 2011, 84(10): 1527-1530.

DOI：10.1016/j.chemosphere.2011.04.045

• Halogenated bisphenol A
• Thyroid hormone activity
• Yeast two-hybrid assay
• Rat liver S9

The thyroid hormone agonist/antagonist activities of halogenated derivatives of bisphenol A (BPA) were assessed using a yeast two-hybrid assay incorporating the human thyroid hormone alpha (TR alpha), both with and without possible metabolic activation by rat liver S9 preparation. In the absence of the rat liver S9 preparation, 3,3',5,5'-tetrabromobisphenol A (TBBPA), 3,3',5,5'-tetrachlorobisphenol A (TCBPA), and 3,3',5-trichlorobisphenol A (3,3',5-triCIBPA) exhibited agonist activity, whereas 3-chlorobisphenol A (3-CIBPA), 3,5-dichlorobisphenol A (3,5-diCIBPA), 3,3'-dichlorobisphenol A (3,3'-diCIBPA), and BPA did not. The activities of TBBPA and TCBPA increased markedly (7.6-fold and 3.1-fold, respectively) after their metabolic activation with the rat liver S9 preparation. TBBPA, TCBPA, and 3,3',5-triCIBPA inhibited the binding of triiodothyronine (T3) to TR alpha at 2 x 10(-5) M without rat liver S9 treatment and 4 x 10(-6) M with rat liver S9 treatment, demonstrating their T3 antagonist activity. These results revealed that metabolic activation by rat liver S9 significantly increased the agonist/antagonist potential of some halogenated BPAs.

• 出版日期2011-9