Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure-activity relationship

• Published in: Journal of enzyme inhibition and medicinal chemistry Vol. 34; no. 1; pp. 577 - 588
• Main Authors: Proença, Carina, Freitas, Marisa, Ribeiro, Daniela, Tomé, Sara M., Oliveira, Eduardo F. T., Viegas, Matilde F., Araújo, Alberto N., Ramos, Maria J., Silva, Artur M. S., Fernandes, Pedro A., Fernandes, Eduarda
• Format: Journal Article
• Language: English
• Published: England Taylor & Francis 01.01.2019; Taylor & Francis Group
• Subjects: diabetes; docking; flavonoids; in vitro; α-Amylase inhibition; docking; flavonoids; diabetes; α-Amylase inhibition
• ISSN: 1475-6366; 1475-6374
• DOI: 10.1080/14756366.2018.1558221

α-Amylase has been considered an important therapeutic target for the management of type 2 diabetes mellitus (T2DM), decreasing postprandial hyperglycaemia (PPHG). In the present work, a panel of 40 structurally related flavonoids was tested, concerning their ability to inhibit α-amylase activity, using a microanalysis screening system, an inhibitory kinetic analysis and molecular docking calculations. From the obtained results, it was possible to observe that the flavone with a -Cl ion at 3-position of C-ring, an -OH group at 3′- and 4′- positions of B-ring and at 5- and 7- positions of A-ring and the C2 = C3 double bond, was the most active tested flavonoid, through competitive inhibition. In conclusion, some of the tested flavonoids have shown promising inhibition of α-amylase and may be considered as possible alternatives to the modulation of T2DM.