Kodama Goh, Taguchi Kensei, Ito Sakuya, Nishino Yuri, Mori Kayo, Taguchi Satomi, Mitsuishi Yuta, Yamashita Yuya, Yamagishi Sho-Ichi, Fukami Kei
Division of Nephrology, Department of Medicine, Kurume University School of Medicine, 67, Asahi-machi, Kurume city, 830-0011, Fukuoka, Japan.
Research Institute of Medical Mass Spectrometry, Kurume University School of Medicine, Kurume, 830-0011, Japan.
Sci Rep. 2025 Apr 3;15(1):11486. doi: 10.1038/s41598-025-95673-9.
Diabetic kidney disease (DKD) is a leading cause of end stage kidney disease. Elevated salt sensitivity by epithelial sodium channel (ENaC) overexpression may be a residual risk factor for DKD. We found that combination therapy of linagliptin (LINA) to empagliflozin (EMPA), but not EMPA alone decreased phosphorylated Nedd4-2 (p-Nedd4-2) and ENaC levels in DKD rats in association with the increased urinary sodium excretion (USE). More extensive renoprotective effects were observed by the combination therapy of LINA and EMPA in deoxycorticosterone and high salt-treated mice. Acute injection experiments showed time-lagged administration of LINA to EMPA increased USE, and its effect sustained until 3 h. High salt and high glucose increased p-Nedd4-2 and ENaC levels in cultured distal tubules, which was inhibited by LINA or glucagon like peptide-1 (GLP-1), but there were no additive effects of LINA on GLP-1, the latter of which was blocked by GLP-1 receptor agonist. USE was higher and ENaC expression was lower in DKD patients received SGLT2is and DPP4is than those without. Our present findings suggest that addition of LINA to EMPA decreases p-Nedd4-2 and ENaC levels via the activation of GLP-1-receptor axis, which could ameliorate salt sensitivity and help prevent kidney injury in DKD.
糖尿病肾病(DKD)是终末期肾病的主要病因。上皮钠通道(ENaC)过表达导致的盐敏感性升高可能是DKD的一个残留危险因素。我们发现,利格列汀(LINA)与恩格列净(EMPA)联合治疗可降低DKD大鼠的磷酸化Nedd4-2(p-Nedd4-2)和ENaC水平,同时尿钠排泄(USE)增加,而单独使用EMPA则无此效果。在脱氧皮质酮和高盐处理的小鼠中,LINA与EMPA联合治疗观察到更广泛的肾脏保护作用。急性注射实验表明,LINA与EMPA的时间滞后给药可增加USE,其作用可持续至3小时。高盐和高糖可增加培养的远端小管中的p-Nedd4-2和ENaC水平,LINA或胰高血糖素样肽-1(GLP-1)可抑制此作用,但LINA对GLP-1无相加作用,后者可被GLP-1受体激动剂阻断。接受钠-葡萄糖协同转运蛋白2抑制剂(SGLT2is)和二肽基肽酶4抑制剂(DPP4is)治疗的DKD患者的USE较高,ENaC表达较低。我们目前的研究结果表明,LINA与EMPA联合使用可通过激活GLP-1受体轴降低p-Nedd4-2和ENaC水平,这可能改善盐敏感性并有助于预防DKD中的肾损伤。