Xue Jia
1*
Yongjian Li
2*The final, formatted version of the article will be published soon.
ORIGINAL RESEARCH article
Front. Chem.
Sec. Medicinal and Pharmaceutical Chemistry
Volume 12 - 2024 |
doi: 10.3389/fchem.2024.1479308
This article is part of the Research Topic Preparation, Bioactivity Evaluation, and Quality Control of Natural Products and Their Derivatives View all 14 articles
Inhibition effects and mechanism of daphnetin against α-glucosidase
Provisionally accepted- 1 Nankai University, Tianjin, China
- 2 tianjin nankai hospital, Nankai, Tianjin, China
- 3 zhejiang jinxing pharmaceutical Co, Ltd, shaoxing, China
Daphnetin, one important coumarin derivative obtained from Daphne koreanum Nakai, exhibits a spectrum of pharmacological properties. But the inhibition effects and mechanism of daphnetin against α-glucosidase were still ambiguous. Hence, we investigated above topic issue by multispectroscopic method and molecular docking. Enzyme activity evaluation results showed that daphnetin reversibly inhibited α-glucosidase in mixed-type manner with an IC 50 value of 0.22 ± 0.01 mM. Fluorescence quenching results showed daphnetin could bind to α-glucosidase and quench its fluorescence in the static quenching mechanism. Synchronous fluorescence, 3D fluorescence, and ANS-binding fluorescence results revealed that the binding of daphnetin to α-glucosidase could change the microenvironment and conformation of α-glucosidase. CD spectra described the changes in α-glucosidase secondary structure by daphnetin. Besides, molecular docking simulated the detailed hydrogen bonds and hydrophobic interactions between daphnetin and α-glucosidase. All findings provided insights into the inhibition effects and mechanism of daphnetin against α-glucosidase.
Keywords: α-glucosidase, inhibitor, Daphnetin, Inhibition mechanism, nature product
Received: 12 Aug 2024; Accepted: 10 Sep 2024.
Copyright: © 2024 Jia, Li and Zhao. This is an open-access article distributed under the terms of the Creative Commons Attribution License (CC BY). The use, distribution or reproduction in other forums is permitted, provided the original author(s) or licensor are credited and that the original publication in this journal is cited, in accordance with accepted academic practice. No use, distribution or reproduction is permitted which does not comply with these terms.
* Correspondence:
Xue Jia, Nankai University, Tianjin, 300071, China
Yongjian Li, tianjin nankai hospital, Nankai, Tianjin, China
Xiaowei Zhao, zhejiang jinxing pharmaceutical Co, Ltd, shaoxing, China
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