Abstract

Small molecules isolated from herbal medicines (HMs) were identified as the potential neuraminidase inhibitors which are effective in influenza prevention and treatment. Unfortunately, current available screen methods of small molecules isolated from HMs are inefficient and insensitive. Here a novel Ultra Performance Liquid Chromatography coupled with diode-array detectors and auto-fraction collector / time-of-flight mass spectrometry (UPLC-DAD-FC/Q-TOF-MS) screening method with high efficiency was developed and validated to separate, collect, enrich, identify and quantify potential neuraminidase inhibitors from Radix Scutellariae. The results showed that 26 components with neuraminidase inhibitory activity were identified from Radix Scutellariae extracts. It was also found that the influence of origins on the quality of RS was more than that of cultivated time on the basis of the concentration of the effective components. These results brought novel insights into quality evaluation of Radix Scutellariae. It was demonstrated that new activity-integrated strategy was a suitable technique for the identification, screening and determination of potential neuraminidase inhibitors in herbal medicine and will provide novel potential strategies in other drug screening from herbal medicine.

Highlights

  • Influenza is a burgeoning infectious disease which causes severe respiratory illnesses [1]

  • The accuracy ranging ±15% of the primitive concentration and relative standard deviation (RSD) less than 5% were considered to be acceptable

  • By comparing the shapes of the peaks and the resolutions of the target compounds, the best results were obtained in the conditions with acetonitrile 0.1% formic acid as a mobile phase

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Summary

Introduction

Influenza is a burgeoning infectious disease which causes severe respiratory illnesses [1]. The viral surface protein neuraminidase (NA) is widely used as a direct target to inhibit viral replication and block human body infection [2], which promotes the hydrolysis of terminal sialic acid residues of newly generated virus and host cell receptors [3]. Identification, screening and determination of potential neuraminidase inhibitors

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