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α-Glucosidase inhibitory activities of phenolic acid amides with l-amino acid moiety

机译：α-葡萄糖苷酶抑制酚酰胺与L-氨基酸部分的抑制活性

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α-Glucosidase inhibitors can effectively control postprandial hyperglycemia. In this study, a series of phenolic acids with the L -amino acid moiety were synthesized and their inhibitory activities against α-glucosidase from Saccharomyces cerevisiae (EC 3.2.1.20) were evaluated. The results suggested that all these compounds showed strong α-glucosidase inhibitory activities. In particular, N -(4-hydroxyl-phenylpropenoyl)- L -alanine ( c2 ) and N -(4-hydroxyl-phenylpropenoyl)- L -methionine ( c8 ) exhibited much higher potency (IC _(50) values 0.04 mM) than the positive control, acarbose (IC _(50) values 1.70 mM). Three-dimensional quantitative structure–activity relationship (3D-QSAR) model for comparative molecular field analysis (CoMFA) was generated and the result showed that bulk groups and high electron density groups on the amino acid residues were a benefit to their activities. Moreover, the substituents with low electron density and little steric hindrance on the para position of the benzene ring were helpful in improving the activities. Kinetic analysis indicated that compound ( c2 ) acted as a mixed-type inhibitor with a K _(i) value of 0.0124 mM. Docking analysis showed that they could bind to α-glucosidase at the catalytic site via hydrogen bonds and a π–π stacking.
机译：α-葡萄糖苷酶抑制剂可以有效地控制餐后高血糖。在该研究中，合成了一系列具有L-氨基酸部分的酚醛酸，并评估了它们对来自Saccharomyces Cerevisiae（EC 3.2.1.20）的对α-葡糖苷酶的抑制活性。结果表明，所有这些化合物都显示出强烈的α-葡糖苷酶抑制活性。特别地，N - （4-羟基 - 苯基丙烯酰基） - L- alanine（C2）和N - （4-羟基 - 苯基丙烯酰基） - L-methionine（C8）表现出更高的效力（IC _（50）值0.04 mm）比阳性对照，炭疽（IC _（50）值1.70 mm）。产生了对比较分子场分析（COMFA）的三维定量结构 - 活性关系（3D-QSAR）模型，结果表明，氨基酸残基上的散装基团和高电子密度基团对其活性有益。此外，具有低电子密度的取代基和苯环对位置上的空间障碍物的次数很小地有助于改善活性。动力学分析表明，化合物（C2）用作混合型抑制剂，K _（I）值为0.0124mm。对接分析表明，它们可以通过氢键和π-π堆叠在催化部位的α-葡糖苷酶结合。

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