Water-Soluble Fullerene C<sub>60</sub> Derivatives Are Effective Inhibitors of Influenza Virus Replication

The influenza virus genome features a very high mutation rate leading to the rapid selection of drug-resistant strains. Due to the emergence of drug-resistant strains, there is a need for the further development of new potent antivirals against influenza with a broad activity spectrum. Thus, the sea...

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Bibliographic Details
Main Authors: Ekaterina O. Sinegubova, Olga A. Kraevaya, Aleksandrina S. Volobueva, Alexander V. Zhilenkov, Alexander F. Shestakov, Sergey V. Baykov, Pavel A. Troshin, Vladimir V. Zarubaev
Format: Article
Language:English
Published: MDPI AG 2023-03-01
Series:Microorganisms
Subjects:
Online Access:https://www.mdpi.com/2076-2607/11/3/681
Description
Summary:The influenza virus genome features a very high mutation rate leading to the rapid selection of drug-resistant strains. Due to the emergence of drug-resistant strains, there is a need for the further development of new potent antivirals against influenza with a broad activity spectrum. Thus, the search for a novel, effective broad-spectrum antiviral agent is a top priority of medical science and healthcare systems. In this paper, derivatives based on fullerenes with broad virus inhibiting activities in vitro against a panel of influenza viruses were described. The antiviral properties of water-soluble fullerene derivatives were studied. It was demonstrated that the library of compounds based on fullerenes has cytoprotective activity. Maximum virus-inhibiting activity and minimum toxicity were found with compound <b>2</b>, containing residues of salts of 2-amino-3-cyclopropylpropanoic acid (CC<sub>50</sub> > 300 µg/mL, IC<sub>50</sub> = 4.73 µg/mL, SI = 64). This study represents the initial stage in a study of fullerenes as anti-influenza drugs. The results of the study lead us conclude that five leading compounds (<b>1</b>–<b>5</b>) have pharmacological prospects.
ISSN:2076-2607