Abstract
Inhibition of H3N2 influenza PA endonuclease activity by a panel of anionic calix[n]arenes and β-cyclodextrin sulfate has been studied. The joint experimental and theoretical results reveal that the larger, more flexible and highly water-soluble sulfonato-calix[n]arenes have high inhibitory activity, with para-sulfonato-calix[8]arene, SC8, having an IC50 value of 6.4 μM. Molecular docking calculations show the SC8 can interact at both the polyanion binding site and also the catalytic site of H3N2 influenza PA endonuclease.
Highlights
IntroductionInfluenza A viruses are agents of infection (pathogens) that can be transmitted by skin contact or from aerosol droplets
Influenza A viruses are agents of infection that can be transmitted by skin contact or from aerosol droplets
We demonstrated that large flexible para-sulfonato-calix[n]arenes could inhibit in vitro H3N2 PA endonuclease
Summary
Influenza A viruses are agents of infection (pathogens) that can be transmitted by skin contact or from aerosol droplets. The result is a seasonal respiratory disease, characterized by fever, respiratory problems, and headaches. Influenza may be fatal in cases of highly active strains or for weakened patients, including children, the elderly, and those suffering from pre-existing chronic diseases [1]. Infection rates are generally around four million per year, influenza epidemics have reached a pandemic level in 1918, 1957, 1968, and 2009 [2]. The severity of epidemics in terms of virus type, subtype, and lineage have recently been reviewed [3]. The host reservoir for the Influenza A virus is found in waterfowl; transmission to humans is possible. Infection of swine is more common and it has been postulated that swine may be a reservoir for gene reassortment between different sub-forms of the virus [4]. As the viral genome is composed of eight negative-sense RNA segments
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