Laboratory of Veterinary Biochemistry and Molecular Biology, College of Veterinary Medicine, Chungbuk National University, Cheongju, Chungbuk, Republic of Korea.
Int J Mol Med. 2012 Nov;30(5):1233-40. doi: 10.3892/ijmm.2012.1122. Epub 2012 Sep 6.
Various endocrine-disrupting chemicals (EDCs) such as bisphenol A (BPA), alkylphenols [4-nonylphenol (NP) and 4-tert octylphenol (OP)] and isobutylparaben (IBP) are a constant concern due to their widespread distribution. It has been reported that some combinations of hormone-disrupting chemicals are much more powerful than any of the chemicals alone. In this study, we measured the expression of an estrogenic biomarker gene, calbindin-D9k (CaBP-9k), and progesterone receptor (PR) to evaluate the individual or combined estrogenic activity of BPA, NP, OP and IBP in GH3 rat pituitary cells. Most doses of the individual compounds and all the doses of the combined chemicals significantly increased CaBP-9k and PR mRNA and protein expression compared to the vehicle (except for PR expression after treatment with OP and NP at 10-7 M). Of note, high doses (10-6 and 10-5 M) of the EDC combinations increased the translational and transcriptional levels of CaBP-9k by 1.3- to 2.4-fold compared to each individual equivalent concentrations of EDCs. To determine whether the increased CaBP-9k gene expression was induced via intracellular estrogen receptor (ER), we blocked ER signaling using fulvestrant, an ER antagonist. The results showed that fulvestrant significantly reversed the CaBP-9k and PR upregulation following treatment with individual EDCs or their combinations. Taken together, we conclude that combinations of BPA, NP, OP and IBP in GH3 rat pituitary cells have synergistic estrogenic activities mediated by ER signaling. In addition, the expression of the CaBP-9k gene may be used as a biomarker to assess the synergistic effects of EDCs in vitro.
各种内分泌干扰化学物质(EDCs),如双酚 A(BPA)、烷基酚[壬基酚(NP)和叔辛基酚(OP)]和异丁基对苯二酚(IBP),由于其广泛分布,一直是人们关注的焦点。据报道,一些激素干扰化学物质的组合比任何单一化学物质的作用都更强大。在这项研究中,我们测量了雌激素生物标志物基因钙结合蛋白-9k(CaBP-9k)和孕激素受体(PR)的表达,以评估 BPA、NP、OP 和 IBP 单独或联合的雌激素活性在 GH3 大鼠垂体细胞中的作用。与载体相比,大多数单一化合物的剂量和所有联合化学物质的剂量均显著增加了 CaBP-9k 和 PR mRNA 和蛋白的表达(用 OP 和 NP 处理 10-7 M 时除外)。值得注意的是,高剂量(10-6 和 10-5 M)的 EDC 组合使 CaBP-9k 的翻译和转录水平比每个 EDC 的单独等效浓度增加了 1.3-2.4 倍。为了确定 CaBP-9k 基因表达的增加是否是通过细胞内雌激素受体(ER)诱导的,我们使用了 ER 拮抗剂氟维司群阻断了 ER 信号。结果表明,氟维司群显著逆转了用单个 EDC 或其组合处理后 CaBP-9k 和 PR 的上调。总之,我们得出结论,BPA、NP、OP 和 IBP 在 GH3 大鼠垂体细胞中的组合具有通过 ER 信号转导介导的协同雌激素活性。此外,CaBP-9k 基因的表达可以用作评估 EDCs 在体外协同作用的生物标志物。