Synthesis and Evaluation of Coumarin-Chalcone Derivatives as α-Glucosidase Inhibitors
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 (KI = 18.82 μM, KIS = 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..
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2022 |
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| Erschienen: |
2022 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:10 |
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| Enthalten in: |
Frontiers in Chemistry - 10(2022) |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Chun-Mei Hu [VerfasserIn] |
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| Links: |
doi.org [kostenfrei] |
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| Themen: |
α-glucosidase |
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| doi: |
10.3389/fchem.2022.926543 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
DOAJ042404770 |
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| 520 | |a 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 (KI = 18.82 μM, KIS = 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. | ||
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| 700 | 0 | |a Jian-Ping Li |e verfasserin |4 aut | |
| 700 | 0 | |a Meng-Yue Li |e verfasserin |4 aut | |
| 700 | 0 | |a Yu-Fei Zhang |e verfasserin |4 aut | |
| 700 | 0 | |a Di Xiao |e verfasserin |4 aut | |
| 700 | 0 | |a Li Lu |e verfasserin |4 aut | |
| 700 | 0 | |a Zhuang Xiong |e verfasserin |4 aut | |
| 700 | 0 | |a Na Feng |e verfasserin |4 aut | |
| 700 | 0 | |a Chen Li |e verfasserin |4 aut | |
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