Abstract A set of novel trans-tiliroside derivatives were synthesized. The structures of the derivatives were identified by their IR, 1 H-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 ...