Zhang Qiang, Wang Jingyuan, Hu Xiaojin, Lu Wei, Cao Yang, Niu Chunyan, Yue Hongqin
Department of Gastroenterology, Yancheng Third People's Hospital (The Yancheng School of Clinical Medicine of Nanjing Medical University), Yancheng, Jiangsu Province 224000, PR China.
Department of Rhematology and Immunology, Xiang'an Hospital of Xiamen University, Xiamen, Fujian Province 361000, PR China.
Prostaglandins Other Lipid Mediat. 2025 Apr 1;178:106987. doi: 10.1016/j.prostaglandins.2025.106987.
Non-alcoholic fatty liver disease (NAFLD) is a leading cause of cirrhosis and a major risk factor for hepatocellular carcinoma and liver-related death. Diabetes medications have been studied as potential treatments for NAFLD. Glucagon-like peptide-1 agonists (GLP-1RAs) have been rarely reported in the treatment of NAFLD alone as an anti-diabetic drug, and its specific mechanism of action is unknown. We investigated whether the therapeutic effect of liraglutide (LRG, a representative drug of GLP-1RAs) on hepatic steatosis is related to regulating lipid metabolism and enhancing autophagy in the hepatocytes.
We examined the effect of LRG on fat accumulation in fatty hepatocytes, and discussed its effects on enzymes related to lipid metabolism and autophagy. Meanwhile, knockdown of SIRT1 in free fatty acids(FFA)-treated cells was used to detected the influence of LRG on lipid metabolism and autophagy by regulating of AMPK/SIRT1 signaling.
Our findings showed that free fatty acids (FFA) induced hepatocyte steatosis, which was significantly reversed by LRG. Meanwhile, LRG significantly regulated the expression of hepatocyte lipogenesis and cytosolic lipolysis-related proteins (FAS, ACC1, ATGL, HSL, LAL). Furthermore, LRG enhanced FFA-induced suppression of autophagy and SIRT1 expression, reducing intracellular lipid accumulation. It is evident that LRG regulates lipid metabolism and induces autophagy in an (AMPK)-dependent manner. Moreover, SIRT1 knockdown inhibited the autophagy-inducing and lipid-lowering effects of LRG.
GLP-1RAs may lower hepatic steatosis by regulating lipid metabolism and enhancing autophagy in an AMPK/SIRT1-dependent manner, providing a new target for the treatment of NAFLD.
非酒精性脂肪性肝病(NAFLD)是肝硬化的主要病因,也是肝细胞癌和肝脏相关死亡的主要危险因素。糖尿病药物已被研究作为NAFLD的潜在治疗方法。胰高血糖素样肽-1激动剂(GLP-1RAs)作为一种抗糖尿病药物单独用于治疗NAFLD的报道很少,其具体作用机制尚不清楚。我们研究了利拉鲁肽(LRG,一种GLP-1RAs的代表性药物)对肝脂肪变性的治疗作用是否与调节脂质代谢和增强肝细胞自噬有关。
我们研究了LRG对脂肪性肝细胞脂肪积累的影响,并探讨了其对脂质代谢和自噬相关酶的作用。同时,在游离脂肪酸(FFA)处理的细胞中敲低SIRT1,以检测LRG通过调节AMPK/SIRT1信号通路对脂质代谢和自噬的影响。
我们的研究结果表明,游离脂肪酸(FFA)诱导肝细胞脂肪变性,而LRG可显著逆转这一过程。同时,LRG显著调节肝细胞脂肪生成和胞质脂肪分解相关蛋白(FAS、ACC1、ATGL、HSL、LAL)的表达。此外,LRG增强了FFA诱导的自噬抑制和SIRT1表达,减少了细胞内脂质积累。显然,LRG以AMPK依赖的方式调节脂质代谢并诱导自噬。此外,SIRT1敲低抑制了LRG的自噬诱导和降脂作用。
GLP-1RAs可能通过以AMPK/SIRT1依赖的方式调节脂质代谢和增强自噬来降低肝脂肪变性,为NAFLD的治疗提供了新的靶点。