Zhou Tong, Hong Hong, Zhang Lu, Qiao Yang, Jiang Yuan, Chen Ximing, Dong Zheng, Zhang Bo, Zhang Mingyu, Xu Chaoqian, Zhang Rong
Department of Pharmacology, State-Province Key Laboratories of Biomedicine-Pharmaceutics of China, Key Laboratory of Cardiovascular Medicine Research, Ministry of Education, College of Pharmacy, Harbin Medical University, Harbin, Heilongjiang, 150081, PR China; Department of Pharmacy, The First Affiliated Hospital of Harbin Medical University, Harbin, Heilongjiang, 150081, PR China.
Department of Pharmacology, State-Province Key Laboratories of Biomedicine-Pharmaceutics of China, Key Laboratory of Cardiovascular Medicine Research, Ministry of Education, College of Pharmacy, Harbin Medical University, Harbin, Heilongjiang, 150081, PR China.
Eur J Pharmacol. 2025 Sep 5;1002:177811. doi: 10.1016/j.ejphar.2025.177811. Epub 2025 Jun 6.
The protein IkappaB-Zeta (IκBζ), which is a member of the IkappaB (IκB) family, has been implicated in the onset and progression of immune-mediated inflammation and cancer. However, its role in cardiovascular disease remains totally unexplored. We employed advanced molecular techniques to investigate the upregulation of IκBζ protein in mouse models of acute myocardial infarction (AMI) and cellular oxygen-glucose deprivation (OGD), with a focus on nuclear localization. Our results indicate that inhibiting IκBζ protein expression both in vivo and in vitro can reduce cardiomyocyte apoptosis and alleviate cardiac hypoxic injury. Mechanistically, IκBζ influences cardiomyocyte apoptosis by binding to and regulating the activity of the intracellular signal transduction factor and transcriptional activator (STAT3). Upon AMI occurrence, the janus kinase 2-signal transducer and activator of transcription 3 (JAK2/STAT3) signaling pathway is activated, leading to STAT3 phosphorylation and its subsequent translocation into the nucleus. It interacts with activated IκBζ in the nucleus, resulting in decreased STAT3 activity and exacerbating cardiomyocyte apoptosis. Treatment with a STAT3-specific agonist mitigated the pro-apoptotic effects caused by IκBζ overexpression. In conclusion, our study describes for the first time the molecular link in IκBζ and STAT3 and reveals that pro-apoptotic IκBζ plays a crucial role in AMI pathogenesis by downregulating STAT3 activity. These findings suggest that targeting IκBζ may provide a foundation for developing novel therapeutic strategies for the prevention and treatment of myocardial infarction.
蛋白质IkappaB-泽塔(IκBζ)是IkappaB(IκB)家族的成员,与免疫介导的炎症和癌症的发生及发展有关。然而,其在心血管疾病中的作用仍完全未被探索。我们采用先进的分子技术,研究急性心肌梗死(AMI)小鼠模型和细胞氧-葡萄糖剥夺(OGD)中IκBζ蛋白的上调情况,重点关注其核定位。我们的结果表明,在体内和体外抑制IκBζ蛋白表达均可减少心肌细胞凋亡并减轻心脏缺氧损伤。机制上,IκBζ通过结合并调节细胞内信号转导因子和转录激活因子(STAT3)的活性来影响心肌细胞凋亡。AMI发生时,janus激酶2-信号转导子和转录激活子3(JAK2/STAT3)信号通路被激活,导致STAT3磷酸化并随后转运至细胞核。它在细胞核中与活化的IκBζ相互作用,导致STAT3活性降低并加剧心肌细胞凋亡。用STAT3特异性激动剂治疗可减轻IκBζ过表达引起的促凋亡作用。总之,我们的研究首次描述了IκBζ与STAT3之间的分子联系,并揭示促凋亡的IκBζ通过下调STAT3活性在AMI发病机制中起关键作用。这些发现表明,靶向IκBζ可能为开发预防和治疗心肌梗死的新型治疗策略提供基础。