High-Resolution Bioassay Profiling with Complemented Sensitivity and Resolution for Pancreatic Lipase Inhibitor Screening

Jingyi Jian, Jiaming Yuan, Yu Fan, Jincai Wang, Tingting Zhang, Jeroen Kool, Zhengjin Jiang*

*Corresponding author for this work

Research output: Contribution to JournalArticleAcademicpeer-review

Abstract

How to rapidly and accurately screen bioactive components from complex natural products remains a major challenge. In this study, a screening platform for pancreatic lipase (PL) inhibitors was established by combining magnetic beads-based ligand fishing and high-resolution bioassay profiling. This platform was well validated using a mixture of standard compounds, i.e., (-)- epigallocatechin gallate (EGCG), luteolin and schisandrin. The dose–effect relationship of high-resolution bioassay profiling was demonstrated by the standard mixture with different concentrations for each compound. The screening of PL inhibitors from green tea extract at the concentrations of 0.2, 0.5 and 1.0 mg/mL by independent high-resolution bioassay profiling was performed. After sample pre-treatment by ligand fishing, green tea extract at the concentration of 0.2 mg/mL was specifically enriched and simplified, and consequently screened through the high-resolution bioassay profiling. As a result, three PL inhibitors, i.e., EGCG, (-)-Gallocatechin gallate (GCG) and (-)-Epicatechin gallate (ECG), were rapidly identified from the complex matrix. The established platform proved to be capable of enriching affinity binders and eliminating nonbinders in sample pre-treatment by ligand fishing, which overcame the technical challenges of high-resolution bioassay profiling in the aspects of sensitivity and resolution. Meanwhile, the high-resolution bioassay profiling possesses the ability of direct bioactive assessment, parallel structural analysis and identification after separation. The established platform allowed more accurate and rapid screening of PL inhibitors, which greatly facilitated natural product-based drug screening.

Original languageEnglish
Article number6923
Pages (from-to)1-12
Number of pages12
JournalMolecules
Volume27
Issue number20
DOIs
Publication statusPublished - 2 Oct 2022

Bibliographical note

Special Issue: Advanced Analytical Methodologies in Detecting Bioactive Food and Plant Constituents.

Funding Information:
This research was funded by the National Natural Science Foundation of China (82073806), the Natural Science Foundation of Guangdong Province (2021A0505020014), the Guangdong Basic and Applied Basic Research Foundation (2020A1515110867) and the High-End Foreign Experts Project (G2021199005L).

Publisher Copyright:
© 2022 by the authors.

Keywords

  • high-performance liquid chromatography
  • high-resolution bioassay profiling
  • inhibitor screening
  • magnetic beads-based ligand fishing
  • pancreatic lipase

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