Coumarins with α-glucosidase and α-amylase inhibitory activities from the flower of Edgeworthia gardneri
| Autor: | Kun Zhang, Zhiyun Du, Ai-Yu Zhou, Yu Zhang, Deng-Gao Zhao, Yan-Yan Ma |
|---|---|
| Rok vydání: | 2015 |
| Předmět: |
Pharmacology
biology Molecular Structure Stereochemistry Chemistry Plant Extracts Dimer Trimer alpha-Glucosidases General Medicine Flowers Edgeworthia gardneri biology.organism_classification Binding constant chemistry.chemical_compound Coumarins Thymelaeaceae Drug Discovery biology.protein Glycoside Hydrolase Inhibitors Amylase alpha-Amylases Alpha-amylase IC50 |
| Zdroj: | Fitoterapia. 107 |
| ISSN: | 1873-6971 |
| Popis: | The flower of Edgeworthia gardneri is consumed in beverages in Tibet and has potential health benefits for diabetes. As a part of our continuous studies on dietary supplements for diabetes, two monomers, five dimers and one trimer of coumarins were isolated from the flowers of E. gardneri. One dimer was a new compound (1) and its structure was determined by spectroscopic methods, including multiple NMR techniques and mass spectrometry. The inhibitory activities of all coumarins against α-amylase and α-glucosidase were evaluated. Compound 4 displayed potent inhibitory effect on both α-amylase and α-glucosidase, with an IC50 of 90 and 86μg/mL, respectively. The IC50 of compound 3 against α-glucosidase was 18.7μg/mL, and its inhibition mode was noncompetitive. Based on the fluorescence analysis, the binding constant and the number of binding sites of compound 3 were calculated as 2.05×10(5) and 1.24, respectively. Furthermore, the interaction between compound 3 and α-glucosidase was a spontaneous process that was driven mainly by hydrophobic force. This study could facilitate the utilization of E gardneri as functional food ingredient. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
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