a LAQV, REQUIMTE, Laboratory of Applied Chemistry, Department of Chemical Sciences, Faculty of Pharmacy , University of Porto , Porto , Portugal.
b Department of Chemistry and QOPNA , University of Aveiro , Aveiro , Portugal.
J Enzyme Inhib Med Chem. 2019 Dec;34(1):577-588. doi: 10.1080/14756366.2018.1558221.
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.
α-淀粉酶一直被认为是治疗 2 型糖尿病（T2DM）、降低餐后高血糖（PPHG）的重要治疗靶点。在本工作中，使用微分析筛选系统、抑制动力学分析和分子对接计算，测试了一组 40 种结构相关的黄酮类化合物，以研究它们抑制 α-淀粉酶活性的能力。从获得的结果中，可以观察到 C 环 3 位带有 -Cl 离子、B 环 3'和 4'位带有 -OH 基团以及 A 环 5 位和 7 位带有 -OH 基团和 C2=C3 双键的黄酮类化合物，通过竞争性抑制作用，是测试的最活跃的黄酮类化合物。总之，一些测试的黄酮类化合物对 α-淀粉酶显示出有希望的抑制作用，可被视为调节 T2DM 的可能替代物。
