Rapid screening natural-origin lipase inhibitors from hypolipidemic decoctions by ultrafiltration combined with liquid chromatography-mass spectrometry

Shun Xiao, Runru Yu, Ni Ai, Xiaohui Fan

Research output: Contribution to journalArticlepeer-review

40 Scopus citations

Abstract

Lipase inhibitors generate hypolipidemic effect that is helpful to control or treat some obesity diseases by inactivating catalytic activity of human pancreatic lipase, a key enzyme involved in triglyceride hydrolysis in vivo. Many traditional Chinese medicine (TCM) formulae have been effectively used to treat obesity and other fat related diseases for centuries and modern biological experiments demonstrate therapeutic effect of these formulae can be linked to their lipid-lowering capability in blood. These observations suggest that these hypolipidemic decoctions (HDs) could be a promising resource of natural-origin lipase inhibitors. This work described a rapid approach for screening lipase inhibitors from four widely used HDs, including Wu-Ling-San (WLS), Ze-Xie decoction (ZX), Xiao-Xian-Xiong decoction (XXX) and Xiao-Chai-Hu decoction (XCH), by ultrafiltration combing with high performance liquid chromatography-mass spectrometry (HPLC-MS). Our results showed sixteen natural-origin lipase inhibitors were discovered and identified by high resolution and multistage mass spectrometry. Inhibitory activities of two compounds were confirmed by a functional assay of lipase, which validated the reliability of our approach. Molecular docking simulation was then performed to investigate potential mechanism of action for these compounds. Together we present an efficient method for rapid screening lipase inhibitors from complex natural products, which can be easily accommodated to other important enzymatic system with therapeutic values.

Original languageEnglish (US)
Pages (from-to)67-74
Number of pages8
JournalJournal of Pharmaceutical and Biomedical Analysis
Volume104
DOIs
StatePublished - Feb 1 2015

Bibliographical note

Funding Information:
This work was financially supported by the National Basic Research Program of China (No. 2012CB518405 ), program for New Century Excellent Talents in University (NCET-12-0488) and the Science and Technology Foundation of Zhejiang Province (No. 2014C33180 ).

Publisher Copyright:
© 2014 Elsevier B.V.

Copyright:
Copyright 2014 Elsevier B.V., All rights reserved.

Keywords

  • HPLC-MS
  • Hypolipidemic decoctions
  • Lipase inhibitors
  • TCM formulae
  • Ultrafiltration

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