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J Enzyme Inhib Med Chem. 2017 Dec;32(1):1216-1228. doi: 10.1080/14756366.2017.1368503.

α-Glucosidase inhibition by flavonoids: an in vitro and in silico structure-activity relationship study.

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a UCIBIO, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy , University of Porto , Porto , Portugal.
b UCIBIO, REQUIMTE, Faculty of Sciences, Department of Chemistry and Biochemistry , University of Porto , Porto , Portugal.
c Department of Chemistry & QOPNA , University of Aveiro , Aveiro , Portugal.


α-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia (PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of α-glucosidase, based on in vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds. A flavonoid with two catechol groups in A- and B-rings, together with a 3-OH group at C-ring, was the most active, presenting an IC50 much lower than the one found for the most widely prescribed α-glucosidase inhibitor, acarbose. The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG.


Diabetes; flavonoids; in silico; in vitro; α-glucosidase inhibition

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