alpha-Glucosidase inhibition by flavonoids: an in vitro and in silico structure-activity relationship study
authors Proenca, C; Freitas, M; Ribeiro, D; Oliveira, EFT; Sousa, JLC; Tome, SM; Ramos, MJ; Silva, AMS; Fernandes, PA; Fernandes, E
nationality International
journal JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
author keywords Diabetes; flavonoids; alpha-glucosidase inhibition; in vitro; in silico
keywords TYPE-2 DIABETES-MELLITUS; POSTPRANDIAL HYPERGLYCEMIA; ENZYME-INHIBITION; HUMAN NEUTROPHILS; SCORING FUNCTION; DOCKING; AMYLASE; MECHANISM; KINETICS; APIGENIN
abstract alpha-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 alpha-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 alpha-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.
publisher TAYLOR & FRANCIS LTD
issn 1475-6366
year published 2017
volume 32
issue 1
beginning page 1216
ending page 1228
digital object identifier (doi) 10.1080/14756366.2017.1368503
web of science category Biochemistry & Molecular Biology; Chemistry, Medicinal
subject category Biochemistry & Molecular Biology; Pharmacology & Pharmacy
unique article identifier WOS:000434685400008
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journal analysis (jcr 2017):
journal impact factor 3.638
5 year journal impact factor 3.000
category normalized journal impact factor percentile 73.622
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