Magnetic beads-based neuraminidase enzyme microreactor as a drug discovery tool for screening inhibitors from compound libraries and fishing ligands from natural products

Journal of Chromatography. a
Yumei ZhaoZhengjin Jiang

Abstract

Neuraminidase (NA) is a glycoside hydrolase that has been proposed as a potential therapeutic target for influenza. Thus, the identification of compounds that modulate NA activity could be of great therapeutic importance. The aim of this study is to develop a drug discovery tool for the identification of novel modulators of NA from both compound libraries and natural plant extracts. NA was immobilized onto the surface of magnetic beads and the inherent catalytic activity of NA-functionalized magnetic beads was characterized. Based on the enzymatic activity (hydrolysis ratio), the inhibitory activities of 12 compounds from plant secondary metabolites were screened, and the desired anti-NA activities of flavonoids were certified. Ligand fishing with the immobilized enzyme was optimized using an artificial test mixture consisting of oseltamivir, lycorine and matrine prior to carrying out the proof-of-concept experiment with the crude extract of Flos Lonicerae. The combination of ligand fishing and HPLC-MS/MS identified luteolin-7-O-β-D-glucoside, luteolin, 3,5-di-O-caffeoylquinic acid and 3,4-di-O-caffeoylquinic acid as neuraminidase inhibitory ligands in Flos Lonicerae. This is the first report on the use of neuraminidase functio...Continue Reading

Citations

Dec 6, 2019·Frontiers in Chemistry·Marcela Cristina de MoraesQuezia Bezerra Cass
Nov 23, 2020·Journal of Pharmaceutical and Biomedical Analysis·Cong-Peng ZhaoFeng-Qing Yang
Mar 29, 2021·Journal of Pharmaceutical and Biomedical Analysis·Daniella Romano de CarvalhoCarmen Lúcia Cardoso
Aug 7, 2021·Journal of Pharmaceutical and Biomedical Analysis·Isabela Abreu Trindade XimenesMarcela Cristina de Moraes

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