淀粉酶
化学
类黄酮
结构-活动关系
生物化学
药理学
酶
医学
体外
抗氧化剂
作者
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 Alexandrino Fernandes,Eduarda Fernandes
标识
DOI:10.1080/14756366.2018.1558221
摘要
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.
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