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Fluorescence-based Neuraminidase Inhibition Assay to Assess the Susceptibility of Influenza Viruses to The Neuraminidase Inhibitor Class of Antivirals
09:31

Fluorescence-based Neuraminidase Inhibition Assay to Assess the Susceptibility of Influenza Viruses to The Neuraminidase Inhibitor Class of Antivirals

Published on: April 15, 2017

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Antipneumococcal activity of neuraminidase inhibiting artocarpin

E Walther1, M Richter1, Z Xu1

  • 1Jena University Hospital, Department of Virology and Antiviral Therapy, Hans-Knöll-Straße 2, 07745 Jena, Germany.

International Journal of Medical Microbiology : IJMM
|January 17, 2015
PubMed

Insights

Artocarpin, a natural compound, effectively inhibits pneumococcal neuraminidase (NA) and bacterial growth. This promising NA inhibitor shows potential against secondary bacterial pneumonia caused by Streptococcus pneumoniae.

Area of Science:

  • Microbiology
  • Biochemistry
  • Pharmacology

Background:

  • Streptococcus pneumoniae causes secondary bacterial pneumonia during influenza epidemics.
  • Neuraminidase (NA) is a key virulence factor for both influenza viruses and S. pneumoniae.
  • Bacterial NAs are structurally similar to viral NAs and can be inhibited by oseltamivir.

Purpose of the Study:

  • To evaluate the antipneumococcal potential of natural neuraminidase inhibitors (NAIs): katsumadain A and artocarpin.
  • To determine the inhibitory efficiency and mechanism of action of these compounds against pneumococcal NAs.

Main Methods:

  • Enzyme assays (chemiluminescence, fluorescence, hemagglutination) to determine IC50 values.
  • Enzyme kinetics using recombinant NanA NA to elucidate the inhibition mechanism.
  • Minimum Inhibitory Concentration (MIC) and Minimum Biofilm Inhibitory Concentration (MBIC) assays for growth and biofilm inhibition.

Main Results:

  • Artocarpin demonstrated mixed-type inhibition of pneumococcal NA with a Ki of 9.70 microM.
  • Artocarpin inhibited S. pneumoniae growth (MIC: 0.99-5.75 microM) and biofilm formation (MBIC: 1.15-2.97 microM).
  • Artocarpin exhibited significant bactericidal activity (>1000-fold reduction in viability) without harming lung epithelial cells.

Conclusions:

  • Artocarpin is a potent inhibitor of pneumococcal NA and bacterial growth.
  • Artocarpin's ability to inhibit growth and biofilm formation makes it a promising candidate for treating S. pneumoniae infections.
  • Further investigation of artocarpin as a therapeutic agent against secondary bacterial pneumonia is warranted.
Keywords:
AntipneumococcalArtocarpinBiofilmDANAKatsumadain ANanANeuraminidaseNeuraminidase inhibitorsOseltamivirPneumococciZanamivir

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