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

• Type: Article in International Scientific Journal
• Date: 2019

Authors

Proenca, C (Author) Other; Freitas, M (Author) Other; Ribeiro, D (Author) Other; Tome, SM (Author) Other; Oliveira, EFT (Author) Other; Viegas, MF (Author) Other; Araujo, AN (Author) FFUP; Ramos, MJ (Author) FCUP; Silva, AMS (Author) Other; Pedro A Fernandes (Author) FCUP; Eduarda Fernandes (Author) FFUP

Journal

Title: Journal of Enzyme Inhibition and Medicinal Chemistry

Vol. 34

Pages: 577-588

ISSN: 1475-6366

Publisher: Taylor & Francis

Indexing

ISI Web of Knowledge - 89 Citations

Scopus - 97 Citations

Other information

Authenticus ID: P-00Q-595

DOI: 10.1080/14756366.2018.1558221

Abstract (EN): alpha-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 alpha-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 alpha-amylase and may be considered as possible alternatives to the modulation of T2DM. [GRAPHICS] .

Language: English

Type (Professor's evaluation): Scientific

No. of pages: 12