Inhibitory effect of fisetin on α-glucosidase activity. - GreenMedInfo Summary
Inhibitory Effect of Fisetin onα-Glucosidase Activity: Kinetic and Molecular Docking Studies.
Molecules. 2021 Aug 31 ;26(17). Epub 2021 Aug 31. PMID: 34500738
The inhibition ofα-glucosidase is a clinical strategy for the treatment of type 2 diabetes mellitus (T2DM), and many natural plant ingredients have been reported to be effective in alleviating hyperglycemia by inhibiting α-glucosidase. In this study, the α-glucosidase inhibitory activity of fisetin extracted fromScop. was evaluated in vitro. The results showed that fisetin exhibited strong inhibitory activity with an ICvalue of 4.099× 10mM. Enzyme kinetic analysis revealed that fisetin is a non-competitive inhibitor ofα-glucosidase, with an inhibition constant value of 0.01065 ± 0.003255 mM. Moreover, fluorescence spectrometric measurements indicated the presence of only one binding site between fisetin and α-glucosidase, with a binding constant (lgKa) of 5.896 L·mol. Further molecular docking studies were performed to evaluate the interaction of fisetin with several residues close to the inactive site ofα-glucosidase. These studies showed that the structure of the complex was maintained by Pi-Sigma and Pi-Pi stacked interactions. These findings illustrate that fisetin extracted fromScop. is a promising therapeutic agent for the treatment of T2DM.