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Identification of a new natural gastric lipase inhibitor from star anise

Jannet Kamoun 1, 2, 3 Renaud Rahier 3 Imed Koubaa 4 Pascal Mansuelle 5, 6 Régine Lebrun 5, 7 Alexandra Berlioz-Barbier 3 Michele Fiore 8 Karine Alvarez 9 Abdelkarim Abousalham 3 Frederic Carriere 10, 2 Ahmed Aloulou 1
1 ENIS - École Nationale d'Ingénieurs de Sfax | National School of Engineers of Sfax
2 BIP - Bioénergétique et Ingénierie des Protéines
3 MEM² - Métabolisme, Enzymes et Mécanismes Moléculaires
ICBMS - Institut de Chimie et Biochimie Moléculaires et Supramoléculaires
4 Faculté des Sciences de Sfax
5 IMM - Institut de Microbiologie de la Méditerranée
6 Plateforme Protéomique [Marseille]
IMM - Institut de Microbiologie de la Méditerranée
7 MSPP - Plateforme de Spectrométrie de Masse Protéomique - Mass Spectrometry Proteomics Platform
8 CO2GLYCO - Chimie Organique 2-Glycochimie
ICBMS - Institut de Chimie et Biochimie Moléculaires et Supramoléculaires
9 AFMB - Architecture et fonction des macromolécules biologiques
10 EIPL - Enzymologie interfaciale et de physiologie de la lipolyse
Abstract : The identification and isolation of bioactive compounds are of great interest in the drug delivery field, despite being a difficult task. 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. A 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 nucleophilic attack by gastric lipase. Overall, our data suggest that M5ME may be considered as a potential candidate for future application as a gastric lipase inhibitor for the treatment of obesity
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Journal articles
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https://hal-amu.archives-ouvertes.fr/hal-02094625
Contributor : Yves Bourne <>
Submitted on : Tuesday, April 9, 2019 - 5:40:33 PM
Last modification on : Wednesday, July 8, 2020 - 12:43:59 PM

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UNIV-AMU | CNRS | INRA | UNIV-LYON1 | INC-CNRS | INSA-LYON | INSA-GROUPE | UNIV-MONTPELLIER | MONTPELLIER-SUPAGRO | UDL | ICBMS | INRAE

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Jannet Kamoun, Renaud Rahier, Imed Koubaa, Pascal Mansuelle, Régine Lebrun, et al.. Identification of a new natural gastric lipase inhibitor from star anise. Food and Function, Cambridge : Royal Society of Chemistry, 2019, 10 (1), pp.469-478. ⟨10.1039/c8fo02009d⟩. ⟨hal-02094625⟩

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