Water-Soluble Fullerene C60 Derivatives Are Effective Inhibitors of Influenza Virus Replication
Eкатерина O. Синегубова, Olga A. Kraevaya, Alexandrina S. Volobueva, Alexander V. Zhilenkov, Alexander F. Shestakov, Sergey V. Baykov, Pavel A. Troshin, Владимир В. Зарубаев
Abstract
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 2, containing residues of salts of 2-amino-3-cyclopropylpropanoic acid (CC50 > 300 µg/mL, IC50 = 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 (1–5) have pharmacological prospects.