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Identification of a new natural gastric lipase inhibitor from star anise

Abstract

Bioactive compounds identification and isolation from natural complex samples, even though being a difficult task, is of great interest in the drug discovery field. We describe here an innovative strategy for the identification of a new gastric lipase inhibitor from star anise for the treatment of obesity. After plant screening assays for gastric lipase inhibition, star anise was selected and investigated by bioactivity guided fractionation. MALDI-TOF mass spectrometry and peptide mass fingerprinting allowed the detection of an inhibitor covalently bound to the catalytic serine of gastric lipase. Mass-directed screening approach using UPLC-HRMS and accurate mass determination searching identified the flavonoid myricitrin-5-methyl ether (M5ME) as a lipase inhibitor. The inhibitory activity was rationalized based on molecular docking, showing that M5ME is susceptible to a nucleophilic attack by gastric lipase. Overall, our data suggest that M5ME may be considered as a potential candidate for future application as a lipase inhibitor for the treatment of obesity.

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Publication details

The article was received on 14 Oct 2018, accepted on 23 Nov 2018 and first published on 24 Nov 2018


Article type: Paper
DOI: 10.1039/C8FO02009D
Citation: Food Funct., 2018, Accepted Manuscript
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    Identification of a new natural gastric lipase inhibitor from star anise

    J. Kamoun, R. Rahier, S. I. Mohamed, I. Koubaa, P. Mansuelle, R. Lebrun, A. Berlioz-barbier, K. Alvarez, A. Abousalham, F. Carrière and A. Aloulou, Food Funct., 2018, Accepted Manuscript , DOI: 10.1039/C8FO02009D

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