Department of Psychiatry, First Hospital of Shanxi Medical University, Taiyuan, China; Department of Ophthalmology, First Hospital of Shanxi Medical University, Taiyuan, China; Department of Emergency Medicine, Thomas Jefferson University, Philadelphia, PA, United States; Key Laboratory of Cellular Physiology at Shanxi Medical University, Ministry of Education, China.
Department of Orthopedics, Shanxi Medical University Second Affiliated Hospital, Taiyuan, China.
Biochem Pharmacol. 2022 Jan;195:114745. doi: 10.1016/j.bcp.2021.114745. Epub 2021 Aug 27.
The repair of vascular endothelial cell dysfunction is an encouraging approach for the treatment of vascular complications associated with diabetes. It has been demonstrated that members of C1q/tumor necrosis factor-related protein (CTRP) family may improve endothelial function. Nevertheless, the protective properties of CTRPs in diabetic microvascular complications continue to be mostly unknown. Here, we demonstrate that the C1q-like globular domain of CTRP3, CTRP5, and CTRP9 (gCTRP3, 5, 9) exerted a vasorelaxant effect on the microvasculature, of which gCTRP3 was the most powerful one. In a murine model of type 2 diabetes mellitus, serum gCTRP3 level and endothelial function decreased markedly compared with controls. Two weeks of gCTRP3 treatment (0.5 μg/g/d) enhanced endothelium-dependent relaxation in microvessels, increased nitric oxide (NO·) production, and reduced retinal vascular leakage. In addition, Western blotting in human retinal microvascular endothelial cells indicated that gCTRP3 triggered AMP-activated protein kinase-α (AMPKα), hence increasing the endothelial NO synthase (eNOS) level and NO· production. In addition, incubation with gCTRP3 in vitro ameliorated the endothelial dysfunction induced by high glucose in the branch of the mesenteric artery. Blockade of either eNOS or AMPKα completely abolished the effects of gCTRP3 described above. Taken together, we demonstrate for the first time that gCTRP3 improves impaired vasodilatation of microvasculature in diabetes by ameliorating endothelial cell function through the AMPK/eNOS/NO· signaling pathway. This finding may suggest an effective intervention against diabetes-associated microvascular complications.
血管内皮细胞功能障碍的修复是治疗与糖尿病相关的血管并发症的一种有希望的方法。已经证明 C1q/肿瘤坏死因子相关蛋白(CTRP)家族的成员可以改善内皮功能。然而,CTRP 在糖尿病微血管并发症中的保护特性仍然大多未知。在这里,我们证明 CTRP3、CTRP5 和 CTRP9 的 C1q 样球状结构域(gCTRP3、5、9)对微血管具有血管舒张作用,其中 gCTRP3 的作用最强。在 2 型糖尿病小鼠模型中,与对照组相比,血清 gCTRP3 水平和内皮功能明显降低。两周的 gCTRP3 治疗(0.5 μg/g/d)增强了微血管中的内皮依赖性松弛,增加了一氧化氮(NO·)的产生,并减少了视网膜血管渗漏。此外,人视网膜微血管内皮细胞中的 Western blot 分析表明,gCTRP3 触发了 AMP 激活蛋白激酶-α(AMPKα),从而增加了内皮型一氧化氮合酶(eNOS)水平和 NO·的产生。此外,体外孵育 gCTRP3 可改善高葡萄糖诱导的肠系膜动脉分支内皮功能障碍。eNOS 或 AMPKα 的阻断完全消除了上述 gCTRP3 的作用。总之,我们首次证明 gCTRP3 通过改善 AMPK/eNOS/NO·信号通路来改善糖尿病中小血管舒张功能障碍。这一发现可能为治疗与糖尿病相关的微血管并发症提供了一种有效的干预措施。