Synthesis and biological activity of novel tiliroside derivants
- Eur J Med Chem. 2011 Oct;46(10):5189-95. doi: 10.1016/j.ejmech.2011.07.059.
Affiliations
- 1. 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.
PMID: 21856048
DOI: 10.1016/j.ejmech.2011.07.059
Abstract
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.