Ma Jianyong, Hong Kui, Wang Hong-Sheng
Department of Cardiology, Second Affiliated Hospital of Nanchang University, Nanchang, Jiangxi, China.
Department of Pharmacology, University of Cincinnati College of Medicine, Cincinnati, Ohio.
Endocrinology. 2017 Apr 1;158(4):778-790. doi: 10.1210/en.2016-1702.
Bisphenol A (BPA) is an estrogenic endocrine-disrupting chemical (EDC) that has a range of potential adverse health effects. Previously we showed that acute exposure to BPA promoted arrhythmias in female rat hearts through estrogen receptor rapid signaling. Progesterone (P4) and estrogen have antagonistic or complementary actions in a number of tissues and systems. In the current study, we examined the influence and possible protective effect of P4 on the rapid cardiac actions of BPA in female rat cardiac myocytes. Preincubation with physiological concentration (1 nM) of P4 abolished BPA-induced triggered activities in female cardiac myocytes. Further, P4 abrogated BPA-induced alterations in Ca2+ handling, including elevated sarcoplasmic reticulum Ca2+ leak and Ca2+ load. Key to the inhibitory effect of P4 is its blockade of BPA-induced increase in the phosphorylation of phospholamban. At myocyte and protein levels, these inhibitory actions of P4 were blocked by pretreatment with the nuclear P4 receptor (nPR) antagonist RU486. Analysis using membrane-impermeable bovine serum albumin-conjugated P4 suggested that the actions of P4 were mediated by membrane-initiated signaling. Inhibitory G (Gi) protein and phophoinositide-3 kinase (PI3K), but not tyrosine protein kinase activation, were involved in the observed effects of P4. In conclusion, P4 exerts an acute protective effect against BPA-induced arrhythmogenesis in female cardiac myocytes through nPR and the Gi/PI3K signaling pathway. Our findings highlight the importance of considering the impact of EDCs in the context of native hormonals and may provide potential therapeutic strategies for protection against the cardiac toxicities associated with BPA exposure.
双酚A(BPA)是一种具有雌激素活性的内分泌干扰化学物质(EDC),具有一系列潜在的不良健康影响。此前我们发现,急性暴露于BPA会通过雌激素受体快速信号传导促进雌性大鼠心脏的心律失常。孕酮(P4)和雌激素在许多组织和系统中具有拮抗或互补作用。在本研究中,我们研究了P4对雌性大鼠心肌细胞中BPA快速心脏作用的影响及可能的保护作用。用生理浓度(1 nM)的P4预孵育可消除BPA诱导的雌性心肌细胞触发活动。此外,P4消除了BPA诱导的钙处理改变,包括肌浆网钙泄漏增加和钙负荷增加。P4抑制作用的关键在于其阻断了BPA诱导的受磷蛋白磷酸化增加。在心肌细胞和蛋白质水平上,P4的这些抑制作用被核P4受体(nPR)拮抗剂RU486预处理所阻断。使用膜不可渗透的牛血清白蛋白偶联P4的分析表明,P4的作用是由膜起始信号传导介导的。抑制性G蛋白(Gi)和磷脂酰肌醇-3激酶(PI3K),而非酪氨酸蛋白激酶激活,参与了P4的观察到的效应。总之,P4通过nPR和Gi/PI3K信号通路对BPA诱导的雌性心肌细胞心律失常发生发挥急性保护作用。我们的研究结果突出了在天然激素背景下考虑EDC影响的重要性,并可能为预防与BPA暴露相关的心脏毒性提供潜在的治疗策略。