SONGKLANAKARIN JOURNAL OF SCIENCE & TECHNOLOGY

Volume 42, No. 02, Month MARCH, Year 2020, Pages 359 - 364

Highly potent a glucosidase inhibitors from pterocarpus indicus and molecular docking studies

Jirapast Sichaem, Santi Tip-pyang, Kiattisak Lugsanangarm, Rumpa Jutakanoke

Abstract Download PDF

The phytochemical investigation of Pterocarpus indicus barks led to isolation of twelve compounds (1-12), including two major triterpenoids (1 and 2), one quinone derivative (3), three phenolic compounds (4-6) and six flavonoids (7-12). A major active compound (1) was derivatized to one new analogue (1d) and five known derivatives (1a-1c and 1e-1f). All isolated compounds (1-12) and modified analogues (1a-1f) were evaluated for their α-glucosidase activity. In this regard, compounds 1 and 11 exhibited potent inhibitory activity towards yeast -glucosidase when compared to the positive control (acarbose). In addition, the -glucosidase (maltase and sucrase) inhibitory activity of all compounds (1-12 and 1a-1f) was also evaluated. Only compound 11 showed moderate inhibitory activity towards rat intestinal -glucosidase. Further study on mechanism underlying yeast α-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 as promising molecules for diabetic therapy.

Keywords

Pterocarpus indicus, lupeol, clycosin, glucosidase inhibitory activity, molecular docking calculation

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