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Issue 23, 2017
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Rapid screening of pancreatic lipase inhibitors from Monascus-fermented rice by ultrafiltration liquid chromatography-mass spectrometry

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Abstract

Ultrafiltration liquid chromatography-mass spectrometry (UF-LC-MS), affinity-guided isolation, and molecular docking were integrated into one strategy for screening of enzyme inhibitors from functional foods. UF-LC-MS facilitated the rapid characterization of ligands that could bind to an enzyme; affinity-guided isolation was helpful for the efficient preparation of ligands for further bioactivity validation; and molecular docking contributed to studying ligand–protein interactions. The strategy was employed to screen pancreatic lipase inhibitors from Monascus-fermented rice (MFR). Finally, three active compounds, namely monascin, monasfluore B, and ankaflavin were discovered by UF-LC-MS and then purified by semipreparative HPLC. Their lipase-inhibitory activities were verified using an enzymatic functional assay. The Lineweaver–Burk plots showed that they inhibited lipase in a non-competitive manner, and the potential mechanisms were preliminarily explored by molecular docking. The results suggest that the strategy is effective in discovering bioactive compounds from complex systems.

Graphical abstract: Rapid screening of pancreatic lipase inhibitors from Monascus-fermented rice by ultrafiltration liquid chromatography-mass spectrometry

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Supplementary files

Article information


Submitted
23 Mar 2017
Accepted
06 Apr 2017
First published
10 Apr 2017

Anal. Methods, 2017,9, 3422-3429
Article type
Paper

Rapid screening of pancreatic lipase inhibitors from Monascus-fermented rice by ultrafiltration liquid chromatography-mass spectrometry

Y. Fang, H. Song, J. Liang, P. Li and H. Yang, Anal. Methods, 2017, 9, 3422
DOI: 10.1039/C7AY00777A

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