FOOD SCIENCE ›› 2019, Vol. 40 ›› Issue (11): 70-74.doi: 10.7506/spkx1002-6630-20180503-031

• Basic Research • Previous Articles     Next Articles

Inhibition Kinetics and Mechanisms of Resveratrol on α-Glucosidase

JIANG Lili, ZHANG Zhongmin, CHEN Daoyu, WANG Zhen, XUE Hongyu, LIU Yong*   

  1. School of Life Science and Medicine, Dalian University of Technology, Panjin 124221, China
  • Online:2019-06-15 Published:2019-06-28

Abstract: Due to its extensive biological activities such as hypoglycemic effects, resveratrol has gained much attention. Besides, α-glucosidase inhibitors can decrease hyperglycemia, which is closely related to the treatment of type-2 diabetes. In the present study, enzyme-inhibitory kinetics and computer simulation were applied to investigate the effect of resveratrol on the activity of α-glucosidase. The activity of α-glucosidase was measured by spectrophotometry, the inhibition kinetics was investigated using Lineweaver-Burk method, and the binding mechanisms between resveratrol and α-glucosidase were explored using molecular docking simulation. The results indicated that resveratrol was a stronger inhibitor (half maximal inhibitory concentration (IC50) = 5.047 μmol/L) than acarbose (IC50 = 632.6 μmol/L). The inhibition type was noncompetitive, and the value of Ki was 5.743 μmol/L. Molecular docking results demonstrated that the existence of multiple binding modes between resveratrol and α-glucosidase did not affect the binding interaction between acarbose and α-glucosidase. Therefore, resveratrol had potent inhibitory activity against α-glucosidase, and thus had the potential to be developed as an antidiabetic drug or as a dietary supplement in a synergetic manner with acarbose for the treatment of diabetes.

Key words: resveratrol, α-glucosidase, inhibition kinetics, molecular docking, homology modeling

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