Santos, Clementina M.M.Proença, CarinaFreitas, MarisaAraújo, Alberto N.Silva, ArturFernandes, Eduarda2024-05-092024-05-092024Santos, Clementina M. M.; Proença, Carina; Freitas, Marisa; Araújo, Alberto N.; Silva, Artur M. S.; Fernandes, Eduarda (2024). 2-Styrylchromones as inhibitors of α-amylase and α-glucosidase enzymes for the management of type 2 diabetes mellitus. Medicinal Chemistry Research. ISSN 1054-2523. 33:4, p. 600-6101054-2523http://hdl.handle.net/10198/29737alpha-amylase and alpha-glucosidase are key enzymes implicated in carbohydrate digestion and their inhibition has been suggested as a powerful approach for regulating blood glucose levels. The present work describes for the first time their inhibition by a group of twelve hydroxylated 2-styrylchromones (2-SC). Our findings revealed that 2-SC display strong systematic inhibition of alpha-glucosidase rather than alpha-amylase activity. The number and position of the hydroxy groups in the chromone moiety further modulate the inhibitory profile of the studied compounds, and the derivatives bearing one catechol unit are efficient inhibitors of both enzymes. Enzyme kinetic studies indicate that all active compounds act as competitive inhibitors of alpha-amylase while most of them behave as non-competitive inhibitors of alpha-glucosidase. The results are promising and pave the way to further deciphering the potential of this class of compounds as a suitable alternative for the management of type 2 diabetes and its complications.engAlpha-amylaseAlpha-glucosidaseDiabetesKinetics2-Styrylchromonesjournal article10.1007/s00044-024-03200-81554-8120