Synthesis and Biological Activity of trans-Tiliroside Derivatives as Potent Anti-Diabetic Agents

A set of novel trans-tiliroside derivatives were synthesized. The structures of the derivatives were identified by their IR, H-1-NMR, and MS spectra analysis. Their anti-diabetic activities were evaluated on the insulin resistant (IR) HepG2 cell model. As a result, compounds 7a, 7c, 7h, and trans-tiliroside exhibited significant glucose consumption-enhancing effects in IR-HepG2 cells compared with the positive control (metformin). This research provides useful clues for further design and discovery of anti-diabetic agents.