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

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, u...

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Detalles Bibliográficos
Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2019
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6366418/
https://www.ncbi.nlm.nih.gov/pubmed/30724629
http://dx.doi.org/10.1080/14756366.2018.1558221
Descripción
Sumario: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.