Synthesis and inhibitory activity of euparin derivatives as potential dual inhibitors against α-glucosidase and protein tyrosine phosphatase 1B (PTP1B)

Diabetes mellitus is a serious threat to human life and health. The α-glucosidase and protein tyrosine phosphatase 1B (PTP1B) were important targets for the treatment of type 2 diabetes mellitus . In this paper, euparin, a natural product from Eupatorium chinense possessed extensive pharmacological activities , was selected as the lead compound. It was derived into chalcone compounds with high efficiency, and the inhibitory activities of these 30 products on α-glucosidase and PTP1B were tested. The results showed that compounds 12 and 15 had good inhibitory activities against both enzymes. The IC 50 value of 12 to inhibit α-glucosidase and PTP1B was 39.77 and 39.31 μM, and the IC 50 value of 15 to inhibit α-glucosidase and PTP1B was 9.02 and 3.47 μ M , respectively. In addition, molecular docking results showed that compounds 12 and 15 exhibited good binding affinities toward both α -glucosidase and PTP1B with negative binding energies. The results of the present study demonstrate that compounds 12 and 15 might be beneficial in the treatment of type 2 diabetes.