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.

Details

Title
α-Glucosidase inhibition by flavonoids: an in vitro and in silico structure–activity relationship study
Author
Proença, Carina 1 ; Freitas, Marisa 1 ; Ribeiro, Daniela 1 ; Oliveira, Eduardo F T 2 ; Sousa, Joana L C 3 ; Tomé, Sara M 3 ; Ramos, Maria J 2 ; Silva, Artur M S 3 ; Fernandes, Pedro A 2 ; Fernandes, Eduarda 1   VIAFID ORCID Logo 

1  UCIBIO, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto, Porto, Portugal; 
2  UCIBIO, REQUIMTE, Faculty of Sciences, Department of Chemistry and Biochemistry, University of Porto, Porto, Portugal; 
3  Department of Chemistry & QOPNA, University of Aveiro, Aveiro, Portugal 
End page
1228
Publication year
2017
Publication date
Dec 2017
Publisher
Taylor & Francis Ltd.
ISSN
14756366
e-ISSN
14756374
Source type
Scholarly Journal
Language of publication
English
ProQuest document ID
2195231232
Copyright
© 2017 The Author(s). Published by Informa UK Limited, trading as Taylor & Francis Group. This work is licensed under the Creative Commons Attribution License http://creativecommons.org/licenses/by/4.0/ (the “License”). Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.