代谢活化作用对多溴代联苯类污染物类/抗甲状腺激素活性的影响

选用大鼠肝匀浆(S9)和鼠肝癌细胞(H4ⅡE)两种体系代谢活化多溴代联苯醚混标(BDEs)和十溴联苯醚(BDE209),采用重组甲状腺激素受体基因酵母检测BDEs和BDE209母体及其代谢产物的类/抗甲状腺激素效应.结果表明,BDEs和BDE209母体均不表现甲状腺激素效应(p>0.05);但是经S9和H4ⅡE细胞代谢活化后,其代谢产物表现出明显的类甲状腺激素活性和抗甲状腺激素活性(p<0.05),BDEs和BDE209的干扰甲状腺激素效应需要经过代谢活化步骤.比较不同代谢活化体系,重组酵母细胞本身的代谢活化作用并不显著,而H4ⅡE细胞和S9代谢活化体系均能够导致活性中间体.

Infection on Thyroid Hormone Agonistic and Antagonistic Activation of Polybrominated Diphenyl Ether by in Vitro Metabolism

In this study,polybrominated diphenyl ether mixture(BDEs)and deca-brominated diphenyl ether(BDE209)were metabolized by rat liver S9 and H4ⅡE cell line and the ant/agonistic activities of parent PBDE and their metabolites were detected using recombined two-hybrid TR gene yeast assay. Results showed that parent BDEs and BDE209 did not exhibit TR agonistic and antagonistic activities(p>0.05). After metabolized by S9 and H4ⅡE cell line,BDEs and BDE209 metabolites showed strong TR agonistic and antagonistic activities than BDEs and BDE209(p<0.05). It was found that the TR agonistic and antagonistic activities of BDEs and BDE209 needed metabolism in vitro. Compared the different metabolism methods,the recombined yeast assay did not show ability to metabolism,but rat liver S9 and H4ⅡE cell line could induce the activity metabolites.