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

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

  • J Enzyme Inhib Med Chem. 2017 Dec;32(1):1216-1228. doi: 10.1080/14756366.2017.1368503.
Carina Proença 1,  Marisa Freitas 1,  Daniela Ribeiro 1,  Eduardo F T Oliveira 2,  Joana L C Sousa 3,  Sara M Tomé 3,  Maria J Ramos 2,  Artur M S Silva 3,  Pedro A Fernandes 2,  Eduarda Fernandes 1
Affiliations

Affiliations

  • 1 a UCIBIO, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy , University of Porto , Porto , Portugal.
  • 2 b UCIBIO, REQUIMTE, Faculty of Sciences, Department of Chemistry and Biochemistry , University of Porto , Porto , Portugal.
  • 3 c Department of Chemistry & QOPNA , University of Aveiro , Aveiro , Portugal.
PMID: 28933564 DOI: 10.1080/14756366.2017.1368503
Abstract

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.

Keywords

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

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