Tianjin Medical University, Tianjin Key Laboratory on Technologies Enabling Development Clinical Therapeutics and Diagnostics, School of Pharmaceutical Sciences, Research Center of Basic Medical Sciences, China.
Eur J Med Chem. 2011 Oct;46(10):5189-95. doi: 10.1016/j.ejmech.2011.07.059. Epub 2011 Aug 7.
A series of new tiliroside derivatives were synthesized and characterized by analytical (1)H NMR, (13)C NMR and mass spectrometry. All of the compounds were evaluated for anti-diabetic properties in vitro using HepG2 cells. Compounds 3c, 3d, and 3i-l caused significant enhancements in glucose consumption by insulin-resistant HepG2 cells compared with control cells and cells that were exposed to metformin (an anti-diabetic drug). Moreover, compound 3l significantly activated adenosine 5'-monophosphate-activated protein kinase activity and reduced acetyl-CoA carboxylase activity. Thus, the tiliroside derivative 3l offers potential to be developed as a new approach for treating type II diabetes.
一系列新的獐牙菜苦苷衍生物被合成并通过分析 (1)H NMR、(13)C NMR 和质谱进行了表征。所有化合物都在体外使用 HepG2 细胞评估了抗糖尿病特性。与对照细胞和暴露于二甲双胍（一种抗糖尿病药物）的细胞相比，化合物 3c、3d 和 3i-l 显著增加了胰岛素抵抗的 HepG2 细胞的葡萄糖消耗。此外，化合物 3l 还显著激活了腺苷 5'-单磷酸激活蛋白激酶活性并降低了乙酰辅酶 A 羧化酶活性。因此，獐牙菜苦苷衍生物 3l 具有作为治疗 II 型糖尿病的新方法的潜力。
