Division of Nephrology and National Clinical Research Center for Geriatrics, Kidney Research Institute, West China Hospital of Sichuan University, Chengdu, 610041, China; Division of Pathology, West China Hospital of Sichuan University, Chengdu, 610041, China.
Division of Nephrology and National Clinical Research Center for Geriatrics, Kidney Research Institute, West China Hospital of Sichuan University, Chengdu, 610041, China.
Biomed Pharmacother. 2020 Jun;126:110056. doi: 10.1016/j.biopha.2020.110056. Epub 2020 Mar 4.
Activation of G protein-coupled receptor 120 (GPR120) could inhibit apoptosis and inflammation in cerebral ischemic injury and liver ischemia-reperfusion injury. However, whether GPR120 agonism exerted potential for cisplatin-induced acute kidney injury and the involved mechanisms remained unknown. In our study, pharmacological activation of GPR120 by TUG891 treatment remarkably reduced the elevated serum creatinine level and attenuated tubular injury. Cisplatin triggered ATF6, PERK and IRE1 pathways of unfolded protein response (UPR) of ER stress in the injured kidney tissue, as well as the downstream molecules eIF2α, ATF4 and XBP1. Protein of ER stress-mediated apoptosis, CHOP, was overexpressed in the cisplatin group. Oral application of TUG891 displayed effective inhibition of ER stress and apoptosis. TUG891 treatment significantly decreased the TUNEL positive cells and the flow cytometry of HK-2 cells delineated the similar results that the apoptosis rates were considerably reduced in the TUG891 group compared to cisplatin group. Collectively, activation of GPR120 by TUG891 exhibited renal protection against cisplatin-induced AKI via suppressing ER-associated apoptosis in tubular epithelial cells.
G 蛋白偶联受体 120(GPR120)的激活可抑制脑缺血损伤和肝缺血再灌注损伤中的细胞凋亡和炎症。然而,GPR120 激动剂是否对顺铂诱导的急性肾损伤有潜在作用及其涉及的机制尚不清楚。在我们的研究中,TUG891 处理通过激活 GPR120 显著降低了升高的血清肌酐水平并减轻了肾小管损伤。顺铂在损伤的肾脏组织中触发内质网应激(ERS)的未折叠蛋白反应(UPR)的 ATF6、PERK 和 IRE1 途径,以及下游分子 eIF2α、ATF4 和 XBP1。内质网应激介导的凋亡蛋白 CHOP 在顺铂组中过度表达。TUG891 的口服应用显示出对 ER 应激和细胞凋亡的有效抑制。TUG891 处理显著减少了 TUNEL 阳性细胞,并且 HK-2 细胞的流式细胞术描绘了类似的结果,与顺铂组相比,TUG891 组的细胞凋亡率明显降低。总之,通过抑制肾小管上皮细胞中 ER 相关的凋亡,TUG891 通过激活 GPR120 对顺铂诱导的 AKI 表现出肾脏保护作用。