Synthesis of Benzylidene Analogs of Oleanolic Acid as Potential α-Glucosidase and α-Amylase Inhibitors
A series of benzylidene analogs of oleanolic acid 4a∼4s were synthesized and assessed for their α-glucosidase and α-amylase inhibitory activities. The results presented that all synthesized analogs exhibited excellent-to-moderate inhibitory effects on α-glucosidase and α-amylase. Analog 4i showed the highest α-glucosidase inhibition (IC50: 0.40 μM), and analog 4o presented the strongest α-amylase inhibition (IC50: 9.59 μM). Inhibition kinetics results showed that analogs 4i and 4o were reversible and mixed-type inhibitors against α-glucosidase and α-amylase, respectively. Simulation docking results demonstrated the interaction between analogs and two enzymes. Moreover, analogs 4i and 4o showed a high level of safety against 3T3-L1 and HepG2 cells..
| 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: |
Jun-Jie Ke [VerfasserIn] |
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| Links: |
doi.org [kostenfrei] |
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| Themen: |
α-amylase |
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| doi: |
10.3389/fchem.2022.911232 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
DOAJ043207847 |
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| 520 | |a A series of benzylidene analogs of oleanolic acid 4a∼4s were synthesized and assessed for their α-glucosidase and α-amylase inhibitory activities. The results presented that all synthesized analogs exhibited excellent-to-moderate inhibitory effects on α-glucosidase and α-amylase. Analog 4i showed the highest α-glucosidase inhibition (IC50: 0.40 μM), and analog 4o presented the strongest α-amylase inhibition (IC50: 9.59 μM). Inhibition kinetics results showed that analogs 4i and 4o were reversible and mixed-type inhibitors against α-glucosidase and α-amylase, respectively. Simulation docking results demonstrated the interaction between analogs and two enzymes. Moreover, analogs 4i and 4o showed a high level of safety against 3T3-L1 and HepG2 cells. | ||
| 650 | 4 | |a oleanolic acid | |
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| 650 | 4 | |a α-glucosidase | |
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| 700 | 0 | |a Xiao-Zheng Wu |e verfasserin |4 aut | |
| 700 | 0 | |a Ying-Ying Zheng |e verfasserin |4 aut | |
| 700 | 0 | |a Chun-Mei Hu |e verfasserin |4 aut | |
| 700 | 0 | |a Yu Kang |e verfasserin |4 aut | |
| 700 | 0 | |a Kun Zhang |e verfasserin |4 aut | |
| 700 | 0 | |a Zhuang Xiong |e verfasserin |4 aut | |
| 700 | 0 | |a Zhi-Qiang Ma |e verfasserin |4 aut | |
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