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Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors.

ABSTRACT: Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (a∼v) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC50: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better α-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC50: 1.5 × 105 μM) and the positive control acarbose (IC50: 259.90 ± 1.06 μM). Among them, compound 3t displayed the highest α-glucosidase inhibitory activity (IC50: 24.09 ± 2.36 μM), which was approximately 10 times stronger than that of acarbose. The kinetic assay of 3t (K I = 18.82 μM, K IS = 59.99 μM) revealed that these compounds inhibited α-glucosidase in a mixed-type manner. Molecular docking was used to simulate the interaction between α-glucosidase and compound 3t.

SUBMITTER: Hu CM 

PROVIDER: S-EPMC9271751 | biostudies-literature | 2022

REPOSITORIES: biostudies-literature

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Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors.

Hu Chun-Mei CM   Luo Yong-Xin YX   Wang Wen-Jing WJ   Li Jian-Ping JP   Li Meng-Yue MY   Zhang Yu-Fei YF   Xiao Di D   Lu Li L   Xiong Zhuang Z   Feng Na N   Li Chen C  

Frontiers in chemistry 20220627

Coumarin and chalcone, two important kinds of natural product skeletons, both exhibit α-glucosidase inhibitory activity. In this work, coumarin-chalcone derivatives 3 (<b>a∼v</b>) were synthesized, and their α-glucosidase inhibitory activity was screened. The results showed that all synthetic derivatives (IC<sub>50</sub>: 24.09 ± 2.36 to 125.26 ± 1.18 μM) presented better <i>α</i>-glucosidase inhibitory activity than the parent compounds 3-acetylcoumarin (IC<sub>50</sub>: 1.5 × 10<sup>5</sup> μM  ...[more]

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