Biochemistry Department, Faculty of Pharmacy, Zagazig University, Zagazig, 44519, Egypt.
Pathology Department, Faculty of Veterinary Medicine, Zagazig University, Zagazig, 44519, Egypt.
Naunyn Schmiedebergs Arch Pharmacol. 2024 May;397(5):3449-3459. doi: 10.1007/s00210-023-02826-6. Epub 2023 Nov 14.
Non-alcoholic steatohepatitis (NASH) may be associated with tissue fibrotic changes and can be treated via different therapeutic tools which may however either initiate weak or long-term side effects that minimize its use. Empagliflozin (EMPA) is an oral anti-diabetic drug which has characteristic effects during hepatic steatosis regarding lipid accumulation and insulin resistance. In this study, we aimed to investigate an additional mechanism through which EMPA can exert and potentiate its anti-inflammatory and anti-fibrotic effects in NASH rat model. Male Wistar albino rats fed on high fat diet (HFD) and 20% fructose in drinking water for 18 weeks and received EMPA (30 mg/kg/day, orally) starting from week 11. Body and liver weights, homeostatic model assessment of insulin resistance (HOMA-IR), lipid profile, liver function tests, other biochemical and histological parameters were determined. HFD joined with fructose intake significantly increased body and liver weights, HOMA-IR value, hepatic inflammatory and fibrotic markers, liver transaminases, hepatic expression of nuclear factor-kappa B (NF-κB), sex determining region Y box 9 (SOX 9), and osteopontin (OPN) with significant decrease in hepatic osteocalcin (OCN). Intense hepatic lesions with severe microsteatosis and deposition of collagen fibers were clearly observed. Effectively, EMPA restored the normal liver functions, downregulated hepatic inflammatory cytokines, NF-κB, SOX 9, OPN, and increased OCN level. These results highlight another pathway illustrated the anti-fibrotic effects of EMPA against liver fibrosis probably through downregulation of NF-κB/SOX 9/OPN signaling along with upregulation of hepatic OCN which may potentiate the valuable anti-inflammatory and anti-fibrotic effects of EMPA.
非酒精性脂肪性肝炎(NASH)可能与组织纤维化改变有关,可以通过不同的治疗手段进行治疗,但这些手段可能会引起轻微或长期的副作用,从而限制了其应用。恩格列净(EMPA)是一种口服抗糖尿病药物,在肝脂肪变性方面具有特征性的脂质蓄积和胰岛素抵抗作用。在这项研究中,我们旨在研究 EMPA 发挥其抗炎和抗纤维化作用的另一种机制,即在 NASH 大鼠模型中的作用。雄性 Wistar 白化大鼠给予高脂肪饮食(HFD)和 20%果糖饮用水 18 周,并从第 11 周开始给予 EMPA(30mg/kg/天,口服)。测定体重和肝脏重量、稳态模型评估的胰岛素抵抗(HOMA-IR)、血脂谱、肝功能试验、其他生化和组织学参数。HFD 联合果糖摄入显著增加体重和肝脏重量、HOMA-IR 值、肝炎症和纤维化标志物、肝转氨酶、核因子-κB(NF-κB)、性别决定区 Y 盒 9(SOX 9)和骨桥蛋白(OPN)的肝表达,肝骨钙素(OCN)水平显著降低。明显观察到肝脏严重脂肪变性和胶原纤维沉积的严重肝损伤。EMPA 有效恢复了正常的肝功能,下调了肝炎症细胞因子、NF-κB、SOX 9、OPN,并增加了 OCN 水平。这些结果突出了 EMPA 抗纤维化作用的另一种途径,可能是通过下调 NF-κB/SOX 9/OPN 信号通路,同时上调肝 OCN,从而增强 EMPA 的抗炎和抗纤维化作用。