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Current Computer-Aided Drug Design

Editor-in-Chief

ISSN (Print): 1573-4099
ISSN (Online): 1875-6697

Research Article

Interactions of Flavone and Steroid from A. subintegra as Potential Inhibitors for Porcine Pancreatic Lipase

Author(s): Mastura Ibrahim, Saripah Salbiah Syed Abdul Azziz*, Chee Fah Wong*, Yuhanis Mhd Bakri and Fauziah Abdullah

Volume 16, Issue 6, 2020

Page: [698 - 706] Pages: 9

DOI: 10.2174/1573409915666191015112320

Price: $65

Abstract

Background: Obesity is one serious health condition that contributes to various chronic diseases. The inhibition of pancreatic lipase is a promising treatment for obesity.

Objective: The present study was designed to investigate anti-porcine pancreatic lipase effect of isolated compounds from Aquilaria subintegra and its mechanism.

Methods: Compounds were isolated with serial column chromatography and their structure were identified using spectroscopic methods. Isolated compounds were tested for anti-lipase potential activity using colorimetric assay. The prediction of energy binding between isolated compounds and enzyme was described using YASARA software.

Results: Four compounds were successfully isolated from the bark of A. subintegra, namely, 5- hydroxy-7,4’-dimethoxyflavone, luteolin-7,3’,4’-trimethyl ether, 5,3’-dihydroxy-7,4’-dimethoxyflavone and β-sitosterol. The results indicated that all compounds displayed promising pancreatic lipase inhibitory activity ranging between of 6% to 53% inhibition. Compound 5-hydroxy-7,4’- dimethoxyflavone was a competitive inhibitor and decreases the enzyme catalysis. Meanwhile, β- sitosterol was a non- competitive inhibitor since the latter was bind allosterically toward enzyme.

Conclusion: This finding is significant for further investigation of bioactive compounds from A. subintegra on animal study.

Keywords: Aquilaria subintegra, lipase, flavonoid, docking, competitive, YASARA.

Graphical Abstract


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