Evaluation of a flavonoids library for inhibition of pancreatic alpha-amylase towards a structure-activity relationship.
Article Details
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Proenca C, Freitas M, Ribeiro D, Tome SM, Oliveira EFT, Viegas MF, Araujo AN, Ramos MJ, Silva AMS, Fernandes PA, Fernandes E
Evaluation of a flavonoids library for inhibition of pancreatic alpha-amylase towards a structure-activity relationship.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):577-588. doi: 10.1080/14756366.2018.1558221.
- PubMed ID
- 30724629 [ View in PubMed]
- Abstract
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.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Acarbose Derived Hexasaccharide Pancreatic alpha-amylase Protein Humans UnknownLigandDetails - Drug Enzymes
Drug Enzyme Kind Organism Pharmacological Action Actions Acarbose Derived Hexasaccharide Pancreatic alpha-amylase Protein Humans UnknownLigandDetails