Interactions of Flavone and Steroid from A. subintegra as Potential Inhibitors for Porcine Pancreatic Lipase
| Autor: | Yuhanis Mhd Bakri, Saripah Salbiah Syed Abdul Azziz, Chee Fah Wong, Fauziah Abdullah, Mastura Ibrahim |
|---|---|
| Rok vydání: | 2019 |
| Předmět: |
Swine
medicine.medical_treatment Ether 01 natural sciences Steroid Enzyme catalysis Aquilaria subintegra chemistry.chemical_compound Column chromatography Drug Discovery medicine Pancreatic lipase Animals Enzyme Inhibitors chemistry.chemical_classification biology Molecular Structure 010405 organic chemistry Chemistry Plant Extracts Health condition General Medicine Lipase Flavones 0104 chemical sciences Molecular Docking Simulation 010404 medicinal & biomolecular chemistry Enzyme Biochemistry Thymelaeaceae biology.protein Molecular Medicine Steroids |
| Zdroj: | Current computer-aided drug design. 16(6) |
| ISSN: | 1875-6697 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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