Department of Pharmacology & Therapeutics, McGill University, Montreal, QC, H3G 1Y6, Canada.
Department of Obstetrics & Gynecology, McGill University, Montreal, QC, H3G 1Y6, Canada.
Endocrinology. 2023 Jun 6;164(7). doi: 10.1210/endocr/bqad089.
Organophosphate esters (OPEs) are used extensively as flame retardants and plasticizers and are found ubiquitously in the environment and human matrices. Previous studies suggested that exposure to some of these chemicals may disrupt the homeostasis of female sex hormones and have detrimental effects on female fertility. Here, we determined the effects of OPEs on the function of KGN ovarian granulosa cells. We hypothesized that OPEs alter the steroidogenic ability of these cells by dysregulating the expression of transcripts involved in steroid and cholesterol biosynthesis. KGN cells were exposed for 48 hours to 1 of 5 OPEs (1-50μM): triphenyl phosphate (TPHP), tris(methylphenyl) phosphate (TMPP), isopropylated triphenyl phosphate (IPPP), tert-butylphenyl diphenyl phosphate (BPDP), and tributoxyethyl phosphate (TBOEP), or to a polybrominated diphenyl ether flame retardant, 2,2',4,4' tetrabromodiphenyl ether (BDE-47), in the presence or absence of Bu2cAMP. OPEs increased the basal production of progesterone (P4) and 17β-estradiol (E2) and had either no effect or inhibited Bu2cAMP-stimulated P4 and E2 synthesis; exposure to BDE-47 had no effect. Quantitative real-time polymerase chain reaction (qRT-PCR) analyses revealed that OPEs (≥5μM) increased the basal expression of critical genes (STAR, CYP11A1, CYP19A1, HSD3B2, and NR5A1) involved in steroidogenesis; upon stimulation, the expression of all genes tested was downregulated. An overall inhibition in cholesterol biosynthesis was induced by OPEs, characterized by a downregulation in HMGCR and SREBF2 expression. TBOEP consistently showed the least effect. Therefore, OPEs perturbed steroidogenesis in KGN granulosa cells by targeting the expression of steroidogenic enzymes and cholesterol transporters; these effects may have an adverse impact on female reproduction.
有机磷酸酯(OPEs)被广泛用作阻燃剂和增塑剂,并在环境和人体基质中广泛存在。先前的研究表明,接触其中一些化学物质可能会破坏女性性激素的内稳态,并对女性生育能力产生不利影响。在这里,我们确定了 OPEs 对 KGN 卵巢颗粒细胞功能的影响。我们假设 OPEs 通过调节参与类固醇和胆固醇生物合成的转录本的表达来改变这些细胞的甾体生成能力。将 KGN 细胞暴露于 5 种 OPEs(1-50μM)中的 1 种(1-50μM)48 小时:三苯基磷酸酯(TPHP),三(甲基苯基)磷酸酯(TMPP),异丙基三苯基磷酸酯(IPPP),叔丁基二苯基磷酸酯(BPDP)和三丁氧基乙基磷酸酯(TBOEP),或多溴二苯醚阻燃剂 2,2',4,4'四溴二苯醚(BDE-47),存在或不存在 Bu2cAMP 的情况下。OPEs 增加了孕酮(P4)和 17β-雌二醇(E2)的基础产量,并且没有影响或抑制 Bu2cAMP 刺激的 P4 和 E2 合成;暴露于 BDE-47 没有影响。定量实时聚合酶链反应(qRT-PCR)分析显示,OPEs(≥5μM)增加了参与类固醇生成的关键基因(STAR、CYP11A1、CYP19A1、HSD3B2 和 NR5A1)的基础表达;在刺激下,所有测试基因的表达均下调。OPEs 诱导胆固醇生物合成的整体抑制,其特征是 HMGCR 和 SREBF2 表达下调。TBOEP 始终表现出最小的作用。因此,OPEs 通过靶向类固醇生成酶和胆固醇转运蛋白的表达来扰乱 KGN 颗粒细胞中的类固醇生成;这些影响可能对女性生殖产生不利影响。