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

Curr Comput Aided Drug Des. 2020;16(6):698-706. doi: 10.2174/1573409915666191015112320.

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; YASARA; competitive; docking; flavonoid; lipase.

MeSH terms

  • Animals
  • Enzyme Inhibitors / pharmacology*
  • Flavones / pharmacology*
  • Lipase / antagonists & inhibitors*
  • Lipase / metabolism
  • Molecular Docking Simulation
  • Molecular Structure
  • Plant Extracts / pharmacology*
  • Steroids / pharmacology*
  • Swine
  • Thymelaeaceae*

Substances

  • Enzyme Inhibitors
  • Flavones
  • Plant Extracts
  • Steroids
  • Lipase