Nesaretnam K, Darbre P
School of Animal and Microbial Sciences, The University of Reading, Whiteknights, UK.
J Steroid Biochem Mol Biol. 1997 Aug;62(5-6):409-18. doi: 10.1016/s0960-0760(97)00062-9.
Polychlorinated biphenyls (PCBs) are widespread, persistent environmental contaminants of which some congeners can act as endocrine disrupters. Previous work has shown that 3,4,3',4'-tetrachlorobiphenyl (PCB77) can act as an oestrogen with actions mediated through the oestrogen receptor. Here, oestrogenic actions have been assessed for two further tetrachlorobiphenyl isomers. Assays of oestrogenic action have involved (1) ligand regulation of oestrogen-sensitive gene expression; (2) ligand regulation of cell growth in oestrogen-dependent human breast cancer cell lines MCF7 McGrath and ZR-75-1; and (3) ligand activity in the immature mouse uterine weight bioassay in vivo. These results demonstrate that 3,5,3',5'-tetrachlorobiphenyl (PCB 80) can be considered to be a weak oestrogen agonist, but the 2,5,2',5'-congener (PCB 52) revealed no oestrogenic properties in any of these assays. Implications of these results are discussed in relation to structure-activity predictions for environmental oestrogens.
多氯联苯（PCBs）是广泛存在且持久的环境污染物，其中一些同系物可作为内分泌干扰物。先前的研究表明，3,4,3',4'-四氯联苯（PCB77）可作为一种雌激素，其作用通过雌激素受体介导。在此，对另外两种四氯联苯异构体的雌激素作用进行了评估。雌激素作用的测定涉及：（1）雌激素敏感基因表达的配体调节；（2）雌激素依赖性人乳腺癌细胞系MCF7 McGrath和ZR-75-1中细胞生长的配体调节；以及（3）体内未成熟小鼠子宫重量生物测定中的配体活性。这些结果表明，3,5,3',5'-四氯联苯（PCB 80）可被视为一种弱雌激素激动剂，但2,5,2',5'-同系物（PCB 52）在任何这些测定中均未显示出雌激素特性。结合环境雌激素的构效预测对这些结果的意义进行了讨论。
