School of Pharmacy, Nanchang University, 461 Bayi Road, Nanchang, 330006, China.
National Center for Drug Screening, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China.
Biochem Biophys Res Commun. 2019 Apr 2;511(2):387-393. doi: 10.1016/j.bbrc.2019.02.065. Epub 2019 Feb 20.
Liver fibrosis occurs in most types of chronic liver diseases. The understanding of the pathogenesis of liver fibrosis has grown considerably, but the effective treatments are still lacking. Alogliptin, a classical Dipeptidyl peptidase-4 (DPP4) inhibitor with great effects on type 2 diabetes, has shown the potential to protect liver, but its effects on the progression of liver fibrosis have not been clarified. Herein, we explored the anti-fibrosis effects of alogliptin. In vitro, we demonstrated that alogliptin suppressed the activation of LX-2 upon transforming growth factor-β (TGF-β) challenge. In vivo, chronic treatment with alogliptin alleviated hepatic steatosis and protected from the liver injury in ob/ob mice, which delayed the progression of liver fibrosis. Furthermore, alogliptin significantly relieved the hepatic fibrosis in CCl4-induced liver fibrosis mouse model. In conclusion, our results demonstrate that negatively modulation of alogliptin on hepatic stellate cell (HSC) activation might contribute to liver fibrosis alleviation. Our research provides the potential possibility of alogliptin on the application for liver fibrosis therapy and suggests that DPP4 may be a novel target for liver fibrosis therapy.
肝纤维化发生于大多数慢性肝病。人们对肝纤维化发病机制的认识已经有了很大的提高,但有效的治疗方法仍然缺乏。阿格列汀是一种经典的二肽基肽酶-4(DPP4)抑制剂,对 2 型糖尿病有很好的疗效,它具有保护肝脏的潜力,但它对肝纤维化进展的影响尚不清楚。在此,我们探讨了阿格列汀的抗纤维化作用。在体外,我们证明阿格列汀抑制了转化生长因子-β(TGF-β)刺激下 LX-2 的激活。在体内,慢性阿格列汀治疗可减轻 ob/ob 小鼠的肝脂肪变性并保护其免受肝损伤,从而延缓肝纤维化的进展。此外,阿格列汀还显著缓解了 CCl4 诱导的肝纤维化小鼠模型中的肝纤维化。总之,我们的研究结果表明,阿格列汀对肝星状细胞(HSC)激活的负调控可能有助于减轻肝纤维化。我们的研究为阿格列汀在肝纤维化治疗中的应用提供了潜在的可能性,并提示 DPP4 可能是肝纤维化治疗的一个新靶点。