Department of Pharmacy, The Third Xiangya Hospital, Central South University, Changsha, Hunan, 410013, China.
Center of Clinical Pharmacology, The Third Xiangya Hospital, Central South University, Changsha, Hunan, 410013, China.
Cell Death Dis. 2018 May 1;9(5):568. doi: 10.1038/s41419-018-0593-y.
Pharmacological inhibition of reactive oxygen species (ROS) is a potential strategy to prevent diabetes-induced cardiac dysfunction. This study was designed to investigate precise effects of antioxidant N‑acetylcysteine (NAC) in alleviating diabetic cardiomyopathy (DCM). Echocardiography and histologic studies were performed 12 weeks after streptozocin injection. Protein levels involved in endoplasmic reticulum stress (ERS) and apoptosis were analyzed by western blotting in diabetic hearts or high-glucose (HG, 30 mM)- and palmitic acid (PA, 300 μM)-cultured neonatal rat cardiomyocytes (NRCMs). ROS generation and structural alterations of mitochondria were also assessed. We report that NAC alleviated diabetes-induced cardiac abnormality, including restored ejection fraction (EF %), fraction shortening (FS %), peak E to peak A ratio (E/A) and reduced cardiac hypertrophy and fibrosis. These effects were concomitant with blocked ERS and apoptosis, as evidenced by inactivation of phosphorylated inositol-requiring enzyme-1α (IRE1α)/spliced X-box binding protein 1 (XBP1), phosphorylated protein kinase-like kinase (PERK)/phosphorylated eukaryotic initiation factor 2α (eIF2α) and glucose-regulated protein 78 (GRP78)/activating transcription factor 6 (ATF6α)/C/EBP homologous protein (CHOP) pathways, as well as suppressed Bcl-2-associated X protein (BAX)/B-cell lymphoma-2 (Bcl-2) and cleaved caspase 3 expressions. Mechanistically, PA mediated excessive mitochondrial ROS generation and oxidative stress, which were antagonized by NAC and Mito-TEMPO, a mitochondrial ROS inhibitor. No effects were noted by addition of apocynin, a nicotinamide adenine dinucleotide phosphate (NADPH) oxidase inhibitor, and NADPH oxidase 4 (NOX 4) and NOX 2 expressions were not altered, indicating that PA-induced ROS generation is independent of NADPH oxidases. Most intriguingly, HG failed to promote ROS production despite its ability to promote ERS and apoptosis in NRCMs. Collectively, these findings indicate that NAC primarily abrogates PA-mediated mitochondrial ROS through ERS and therefore alleviates myocardial apoptosis but has little effect on HG-induced cardiac injury. This uncovers a potential role for NAC in formulating novel cardioprotective strategies in DCM patients.
抑制活性氧(ROS)是预防糖尿病引起的心脏功能障碍的一种有潜力的策略。本研究旨在探讨抗氧化剂 N-乙酰半胱氨酸(NAC)在缓解糖尿病心肌病(DCM)中的确切作用。链脲佐菌素注射后 12 周进行超声心动图和组织学研究。通过 Western blot 分析糖尿病心脏或高葡萄糖(HG,30mM)和棕榈酸(PA,300μM)培养的新生大鼠心肌细胞(NRCMs)中涉及内质网应激(ERS)和细胞凋亡的蛋白水平。还评估了 ROS 的产生和线粒体的结构改变。我们报告 NAC 缓解了糖尿病引起的心脏异常,包括射血分数(EF%)、短轴缩短率(FS%)、峰值 E 与峰值 A 比(E/A)的恢复,以及心脏肥大和纤维化的减少。这些作用与 ERS 和细胞凋亡的阻断同时发生,这表明磷酸肌醇需要酶 1α(IRE1α)/剪接 X 盒结合蛋白 1(XBP1)、磷酸蛋白激酶样激酶(PERK)/磷酸真核起始因子 2α(eIF2α)和葡萄糖调节蛋白 78(GRP78)/激活转录因子 6(ATF6α)/C/EBP 同源蛋白(CHOP)途径的失活,以及 Bcl-2 相关 X 蛋白(BAX)/B 细胞淋巴瘤-2(Bcl-2)和裂解 caspase 3 的表达减少。在机制上,PA 介导过量的线粒体 ROS 产生和氧化应激,而 NAC 和线粒体 ROS 抑制剂 Mito-TEMPO 可以拮抗这些作用。添加烟酰胺腺嘌呤二核苷酸磷酸(NADPH)氧化酶抑制剂 apocynin 或 NADPH 氧化酶 4(NOX 4)和 NOX 2 表达无变化,表明 PA 诱导的 ROS 产生不依赖于 NADPH 氧化酶。最有趣的是,尽管 HG 能够促进 NRCMs 中的 ERS 和细胞凋亡,但它未能促进 ROS 的产生。总的来说,这些发现表明 NAC 主要通过 ERS 来消除 PA 介导的线粒体 ROS,从而减轻心肌细胞凋亡,但对 HG 诱导的心脏损伤几乎没有影响。这揭示了 NAC 在制定 DCM 患者新的心脏保护策略中的潜在作用。