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Highly potent ?-glucosidase inhibitors from Pterocarpus indicusand molecular docking studies |
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| รหัสดีโอไอ | |
| Creator | 1. Jirapast Sichaem 2. Santi Tip-pyang 3. Kiattisak Lugsanangarm 4. Rumpa Jutakanoke |
| Title | Highly potent ?-glucosidase inhibitors from Pterocarpus indicusand molecular docking studies |
| Publisher | Research and Development Office, Prince of Songkla University |
| Publication Year | 2563 |
| Journal Title | Songklanakarin Journal of Science and Technology |
| Journal Vol. | 42 |
| Journal No. | 2 |
| Page no. | 359-364 |
| Keyword | Pterocarpus indicus, lupeol, clycosin, ?-glucosidase inhibitory activity, molecular docking calculation |
| URL Website | https://rdo.psu.ac.th/sjstweb/index.php |
| ISSN | 0125-3395 |
| Abstract | The phytochemical investigation of Pterocarpus indicus barks led to isolation of twelve compounds (1-12), includingtwo major triterpenoids (1 and 2), one quinone derivative (3), three phenolic compounds (4-6) and six flavonoids (7-12). A majoractive compound (1) was derivatized to one new analogue (1d) and five known derivatives (1a-1c and 1e-1f). All isolatedcompounds (1-12) and modified analogues (1a-1f) were evaluated for their ?-glucosidase activity. In this regard, compounds 1and 11 exhibited potent inhibitory activity towards yeast ?-glucosidase when compared to the positive control (acarbose). Inaddition, the ?-glucosidase (maltase and sucrase) inhibitory activity of all compounds (1-12 and 1a-1f) was also evaluated. Onlycompound 11 showed moderate inhibitory activity towards rat intestinal ?-glucosidase. Further study on mechanism underlyingyeast ?-glucosidase inhibition indicated that 1 and 11 could retard the enzyme function by noncompetitive and mixed manners,respectively. The experimental results were also confirmed by docking analysis. Therefore, these compounds have emerged aspromising molecules for diabetic therapy. |
