alpha-Glucosidase inhibition by flavonoids: an in vitro and in silico structure-activity relationship study

• Tipo: Artigo em Revista Científica Internacional
• Data: 2017

Autores

Proenca, C (Autor) Outra; Freitas, M (Autor) Outra; Ribeiro, D (Autor) Outra; Oliveira, EFT (Autor) Outra; Sousa, JLC (Autor) Outra; Tome, SM (Autor) Outra; 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. 32

Páginas: 1216-1228

ISSN: 1475-6366

Editora: Taylor & Francis

Indexação

ISI Web of Knowledge - 246 Citações

Scopus - 282 Citações

Outras Informações

ID Authenticus: P-00N-1YY

DOI: 10.1080/14756366.2017.1368503

Abstract (EN): alpha-Glucosidase inhibitors are described as the most effective in reducing post-prandial hyperglycaemia ( PPHG) from all available anti-diabetic drugs used in the management of type 2 diabetes mellitus. As flavonoids are promising modulators of this enzyme's activity, a panel of 44 flavonoids, organised in five groups, was screened for their inhibitory activity of alpha-glucosidase, based on in vitro structure-activity relationship studies. Inhibitory kinetic analysis and molecular docking calculations were also applied for selected compounds. A flavonoid with two catechol groups in A-and B-rings, together with a 3-OH group at C-ring, was the most active, presenting an IC50 much lower than the one found for the most widely prescribed alpha-glucosidase inhibitor, acarbose. The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG.

Idioma: Inglês

Tipo (Avaliação Docente): Científica

Nº de páginas: 13