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

• Tipo: Artigo em Revista Científica Internacional
• Data: 2019

Autores

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

Revista

Título: Journal of Enzyme Inhibition and Medicinal Chemistry

Vol. 34

Páginas: 577-588

ISSN: 1475-6366

Editora: Taylor & Francis

Indexação

ISI Web of Knowledge - 89 Citações

Scopus - 97 Citações

Outras Informações

ID Authenticus: 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] .

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 12