Magnetic nanoparticles immobilized thrombin ligand fishing to screen thrombin inhibitors in natural products
Copyright © 2024 Elsevier B.V. All rights reserved..
In this study, thrombin was immobilized with magnetic particles modified by glutaraldehyde. The changes in secondary structures of immobilized enzyme revealed an increment in conformational rigidity and stability, which can be reflected in temperature and pH stability as well as the tolerance of organic reagents. The optimal reutilization times of magnetic particle immobilized thrombin were 7 times, and the half-life of enzyme activity preserved at room temperature was 5 days, which was 2.5 times higher than that of free enzyme. Ligusticum chuanxiong and Anemarrhenae Rhizoma with high enzyme inhibitory activity were selected for primary screening, and six potential inhibitors of thrombin were identified by HPLC/MS. The results showed that three compounds in Anemarrhenae Rhizoma had better predictive thrombin inhibitory activity. Through the in vitro thrombin activity inhibition experiment, it was also verified that mangiferin and neo-mangiferin had an ideal thrombin activity inhibition effect, which was consistent with the results of molecular docking.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:243 |
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| Enthalten in: |
Journal of pharmaceutical and biomedical analysis - 243(2024) vom: 15. Apr., Seite 116110 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Guo, Hui [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 08.04.2024 Date Revised 08.04.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1016/j.jpba.2024.116110 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| 500 | |a published: Print-Electronic | ||
| 500 | |a Citation Status MEDLINE | ||
| 520 | |a Copyright © 2024 Elsevier B.V. All rights reserved. | ||
| 520 | |a In this study, thrombin was immobilized with magnetic particles modified by glutaraldehyde. The changes in secondary structures of immobilized enzyme revealed an increment in conformational rigidity and stability, which can be reflected in temperature and pH stability as well as the tolerance of organic reagents. The optimal reutilization times of magnetic particle immobilized thrombin were 7 times, and the half-life of enzyme activity preserved at room temperature was 5 days, which was 2.5 times higher than that of free enzyme. Ligusticum chuanxiong and Anemarrhenae Rhizoma with high enzyme inhibitory activity were selected for primary screening, and six potential inhibitors of thrombin were identified by HPLC/MS. The results showed that three compounds in Anemarrhenae Rhizoma had better predictive thrombin inhibitory activity. Through the in vitro thrombin activity inhibition experiment, it was also verified that mangiferin and neo-mangiferin had an ideal thrombin activity inhibition effect, which was consistent with the results of molecular docking | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Immobilized enzyme | |
| 650 | 4 | |a Ligand fishing | |
| 650 | 4 | |a Magnetic nanoparticles | |
| 650 | 4 | |a Molecular docking | |
| 650 | 4 | |a Thrombin inhibitors | |
| 650 | 7 | |a Drugs, Chinese Herbal |2 NLM | |
| 650 | 7 | |a Thrombin |2 NLM | |
| 650 | 7 | |a EC 3.4.21.5 |2 NLM | |
| 650 | 7 | |a Biological Products |2 NLM | |
| 650 | 7 | |a Ligands |2 NLM | |
| 650 | 7 | |a Magnetite Nanoparticles |2 NLM | |
| 650 | 7 | |a Enzymes, Immobilized |2 NLM | |
| 650 | 7 | |a Anticoagulants |2 NLM | |
| 700 | 1 | |a Guo, Lili |e verfasserin |4 aut | |
| 700 | 1 | |a Yu, Jianwei |e verfasserin |4 aut | |
| 700 | 1 | |a Zhao, Fengju |e verfasserin |4 aut | |
| 700 | 1 | |a Yang, Wei |e verfasserin |4 aut | |
| 700 | 1 | |a Li, Jiaxin |e verfasserin |4 aut | |
| 700 | 1 | |a Chen, Hanqi |e verfasserin |4 aut | |
| 700 | 1 | |a Qian, Junqing |e verfasserin |4 aut | |
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