Article

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

Carina ProençaLAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of PortoMarisa FreitasLAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of PortoDaniela RibeiroLAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of PortoSara M. ToméDepartment of Chemistry and QOPNA, University of AveiroEduardo F. OliveiraUCIBIO, REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences, University of PortoMatilde F. ViegasUCIBIO, REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences, University of PortoAlberto N. AraújoLAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of PortoMaria J. RamosUCIBIO, REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences, University of PortoArtur M. S. SilvaDepartment of Chemistry and QOPNA, University of AveiroPedro Alexandrino FernandesUCIBIO, REQUIMTE, Department of Chemistry and Biochemistry, Faculty of Sciences, University of PortoEduarda FernandesLAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy, University of Porto

2019en

ABI

Abstract

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.

Identifiers

DOI: 10.1080/14756366.2018.1558221

Citations and references

Cited by 20 references

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