α-Glucosidase inhibition by flavonoids: an in vitro and in silico structure-activity relationship study.
Carina Proença,Marisa Freitas,Daniela Ribeiro,Eduardo F. Oliveira,Joana L. C. Sousa,Sara M. Tomé,Maria J. Ramos,Artur M. S. Silva,Pedro A. Fernandes,Eduarda Fernandes +9 more
TLDR
The present work suggests that several of the studied flavonoids have the potential to be used as alternatives for the regulation of PPHG, with a flavonoid with two catechol groups in A- and B-rings being the most active.Abstract:
α-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 α-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 α-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.read more
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A comprehensive review on xanthone derivatives as α-glucosidase inhibitors.
TL;DR: A comprehensive review of the literature on xanthones as inhibitors of α-glucosidase activity, their mechanism of action, experimental procedures and structure-activity relationships have been reviewed for more than 280 analogs.
Journal ArticleDOI
Mediterranean Diet Nutrients to Turn the Tide against Insulin Resistance and Related Diseases.
Maria Mirabelli,Eusebio Chiefari,Biagio Arcidiacono,Domenica Maria Corigliano,Francesco Saverio Brunetti,Valentina Maggisano,Diego Russo,Daniela Foti,Antonio Brunetti +8 more
TL;DR: The Mediterranean diet, characterized by high consumption of extra-virgin olive oil (EVOO), nuts, red wine, vegetables and other polyphenol-rich elements, has proved to be associated with greater improvement of IR in obese individuals, when compared to other nutritional interventions.
Journal ArticleDOI
Evaluation of a flavonoids library for inhibition of pancreatic α-amylase towards a structure–activity relationship
Carina Proença,Marisa Freitas,Daniela Ribeiro,Sara M. Tomé,Eduardo F. Oliveira,Matilde F. Viegas,Alberto N. Araújo,Maria J. Ramos,Artur M. S. Silva,Pedro A. Fernandes,Eduarda Fernandes +10 more
TL;DR: Some of the tested flavonoids have shown promising inhibition of α-amylase and may be considered as possible alternatives to the modulation of T2DM.
Journal ArticleDOI
Interactions between phenolic compounds, amylolytic enzymes and starch: an updated overview
TL;DR: A short review on the complex interactions occurring between phenolic compounds and amylolytic enzymes within the food-matrix and during food digestion, together with the postulated effects provided by polyphenols-starch interactions on starch digestibility is provided in this paper.
Journal ArticleDOI
Alpha glucosidase inhibitory activities of plants with focus on common vegetables
Samuel Tilahun Assefa,Eun-Young Yang,Soo-Young Chae,Mihye Song,Jundae Lee,Myeong-Cheoul Cho,Seonghoe Jang +6 more
TL;DR: This review focuses on the alpha-glucosidases inhibitors found in common vegetable crops and the major classes of phytochemicals responsible for the inhibitory activity, and also as potential/natural drug candidates for the treatment of type-2 diabetes mellitus.
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