State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Key laboratory of Polymorphic Drugs of Beijing, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing, China.
Biomedical Engineering Research Center, Kunming Medical University, Kunming, China.
Basic Clin Pharmacol Toxicol. 2021 Jun;128(6):747-757. doi: 10.1111/bcpt.13573. Epub 2021 Mar 14.
The effects of the combination of bis (α-furancarboxylato) oxovanadium (IV) (BFOV) and metformin (Met) on hepatic steatosis were investigated in high-fat diet-induced obese C57BL/6J mice (HFC57 mice) for 6 weeks. Oral glucose tolerance test was performed to evaluate glucose metabolism. Moreover, blood and hepatic biochemical and histological indices were detected. Besides, Affymetrix-GeneChip analysis and Western blot of the liver were performed. Comparing to the monotherapy group, BFOV + Met showed more effective improvement in glucose metabolism, which decreased the fasting blood glucose, insulin levels and improved insulin sensitivity in HFC57 mice. BFOV + Met significantly decreased serum ALT and AST activities and reduced hepatic triglyceride content and iNOS activities, accompanied by ameliorating intrahepatic fat accumulation and hepatocellular vacuolation. Enhanced hepatic insulin signalling transduction and attenuated inflammation pathway were identified as the major pathways in the BFOV + Met group. BFOV + Met significantly down-regulated the protein expression levels of MMPs, NF-κB, iNOS and up-regulated phosphorylation of AKT and AMPK levels. We concluded that a combination of BFOV and metformin ameliorates hepatic steatosis in HFC57 mice via alleviating hepatic inflammation and enhancing insulin signalling pathway, suggesting that the combination of BFOV and metformin is a potential treatment for hepatic steatosis.
在高脂饮食诱导肥胖的 C57BL/6J 小鼠(HFC57 小鼠)中,研究了双(α-呋喃甲酰基)氧钒(IV)(BFOV)和二甲双胍(Met)联合使用对肝脂肪变性的影响,为期 6 周。进行口服葡萄糖耐量试验以评估葡萄糖代谢。此外,还检测了血液和肝脏生化及组织学指标。此外,还对肝脏进行了 Affymetrix-GeneChip 分析和 Western blot。与单药治疗组相比,BFOV+Met 对葡萄糖代谢的改善更为有效,降低了 HFC57 小鼠的空腹血糖、胰岛素水平并改善了胰岛素敏感性。BFOV+Met 显著降低血清 ALT 和 AST 活性,降低肝甘油三酯含量和 iNOS 活性,同时改善肝内脂肪堆积和肝细胞空泡化。增强的肝胰岛素信号转导和减弱的炎症途径被确定为 BFOV+Met 组的主要途径。BFOV+Met 显著下调 MMPs、NF-κB、iNOS 的蛋白表达水平,并上调 AKT 和 AMPK 水平的磷酸化。我们得出结论,BFOV 和二甲双胍的联合使用通过减轻肝炎症和增强胰岛素信号通路改善 HFC57 小鼠的肝脂肪变性,表明 BFOV 和二甲双胍的联合使用是治疗肝脂肪变性的潜在方法。