Rapid screening of xanthine oxidase inhibitors from Ligusticum wallichii by using xanthine oxidase functionalized magnetic metal-organic framework

Anal Bioanal Chem. 2024 Nov;416(28):6651-6662. doi: 10.1007/s00216-024-05570-9. Epub 2024 Sep 30.

Abstract

In this study, xanthine oxidase was immobilized for the first time using a novel magnetic metal-organic framework material (Fe3O4-SiO2-NH2@MnO2@ZIF-8-NH2). A ligand fishing method was established to rapidly screen XOD inhibitors from Ligusticum wallichii based on the immobilized XOD. Characterization and properties of the immobilized enzyme revealed its excellent stability and reusability. A ligand was screened from Ligusticum wallichii and identified as ligustilide by ultra-high performance liquid chromatography tandem mass spectrometry. The IC50 value of ligustilide was determined to be 27.70 ± 0.13 μM through in vitro inhibition testing. Furthermore, molecular docking verified that ligustilide could bind to amino acid residues at the active site of XOD. This study provides a rapid and effective method for the preliminary screening of XOD inhibitors from complex natural products and has great potential for further discovery of anti-hyperuricemic compounds.

Keywords: Ligusticum wallichii; Inhibitor screening; Magnetic metal–organic framework; Molecular docking; Xanthine oxidase.

MeSH terms

  • Enzyme Inhibitors* / chemistry
  • Enzyme Inhibitors* / pharmacology
  • Enzymes, Immobilized / antagonists & inhibitors
  • Enzymes, Immobilized / chemistry
  • Enzymes, Immobilized / metabolism
  • Metal-Organic Frameworks* / chemistry
  • Molecular Docking Simulation*
  • Xanthine Oxidase* / antagonists & inhibitors
  • Xanthine Oxidase* / metabolism

Substances

  • Xanthine Oxidase
  • Enzyme Inhibitors
  • Metal-Organic Frameworks
  • Enzymes, Immobilized