Effects of novel chalcone derivatives on α-glucosidase, dipeptidyl peptidase-4, and adipocyte differentiation in vitro

Chana series are new chalcone derivatives. To evaluate the possibility of Chana series as therapeutic agents of type 2 diabetes, the inhibitory effects of Chana series on the activities of alpha-glucosidase and DPP-4 were investigated using in vitro enzyme assays, and their effects on adipocyte differentiation were investigated in C3H10T1/2 cells. Chana 1 and Chana 7 among the Chana series showed significant inhibition of alpha-glucosidase activity. In DPP-4 enzyme assay, Chana 1 exhibited the highest inhibitory activity while Chana 7 did not. In MU assay, Chana 1 did not show significant cytotoxicity up to a concentration of 250 mu M, whereas cytotoxicity was observed with Chana 7 at a concentration of 300 mu M. In addition, Chana 1 induced adipocyte differentiation. Therefore, Chana 1 showed inhibitory effects on alpha-glucosidase and DPP-4 as well as a stimulatory effect on adipocyte differentiation, suggesting that Chana 1 may be a potential beneficial agent for the treatment of type 2 diabetes. [BMB reports 2011; 44(6): 410-414]