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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MDPI AG
2023-03-01
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| Series: | Microorganisms |
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| Online Access: | https://www.mdpi.com/2076-2607/11/3/681 |
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| author | Ekaterina O. Sinegubova Olga A. Kraevaya Aleksandrina S. Volobueva Alexander V. Zhilenkov Alexander F. Shestakov Sergey V. Baykov Pavel A. Troshin Vladimir V. Zarubaev |
| author_facet | Ekaterina O. Sinegubova Olga A. Kraevaya Aleksandrina S. Volobueva Alexander V. Zhilenkov Alexander F. Shestakov Sergey V. Baykov Pavel A. Troshin Vladimir V. Zarubaev |
| author_sort | Ekaterina O. Sinegubova |
| collection | DOAJ |
| description | 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. |
| first_indexed | 2024-03-09T10:58:50Z |
| format | Article |
| id | doaj.art-0b2aabd3349540ca8136b342c8e38e30 |
| institution | Directory Open Access Journal |
| issn | 2076-2607 |
| language | English |
| last_indexed | 2024-03-09T10:58:50Z |
| publishDate | 2023-03-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Microorganisms |
| spelling | doaj.art-0b2aabd3349540ca8136b342c8e38e302023-12-01T01:22:36ZengMDPI AGMicroorganisms2076-26072023-03-0111368110.3390/microorganisms11030681Water-Soluble Fullerene C<sub>60</sub> Derivatives Are Effective Inhibitors of Influenza Virus ReplicationEkaterina O. Sinegubova0Olga A. Kraevaya1Aleksandrina S. Volobueva2Alexander V. Zhilenkov3Alexander F. Shestakov4Sergey V. Baykov5Pavel A. Troshin6Vladimir V. Zarubaev7Saint Petersburg Pasteur Institute, 14 Ulitsa Mira, 197101 St. Petersburg, RussiaFederal Research Center for Problems of Chemical Physics and Medicinal Chemistry RAS, 1 Prospekt Akademika Semenova, 142432 Chernogolovka, RussiaSaint Petersburg Pasteur Institute, 14 Ulitsa Mira, 197101 St. Petersburg, RussiaFederal Research Center for Problems of Chemical Physics and Medicinal Chemistry RAS, 1 Prospekt Akademika Semenova, 142432 Chernogolovka, RussiaFederal Research Center for Problems of Chemical Physics and Medicinal Chemistry RAS, 1 Prospekt Akademika Semenova, 142432 Chernogolovka, RussiaInstitute of Chemistry, Saint Petersburg State University, 7/9 Universitetskaya Nab., 199034 St. Petersburg, RussiaFederal Research Center for Problems of Chemical Physics and Medicinal Chemistry RAS, 1 Prospekt Akademika Semenova, 142432 Chernogolovka, RussiaSaint Petersburg Pasteur Institute, 14 Ulitsa Mira, 197101 St. Petersburg, RussiaThe 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.https://www.mdpi.com/2076-2607/11/3/681influenza virushemagglutininantiviral agentfullerene |
| spellingShingle | Ekaterina O. Sinegubova Olga A. Kraevaya Aleksandrina S. Volobueva Alexander V. Zhilenkov Alexander F. Shestakov Sergey V. Baykov Pavel A. Troshin Vladimir V. Zarubaev Water-Soluble Fullerene C<sub>60</sub> Derivatives Are Effective Inhibitors of Influenza Virus Replication Microorganisms influenza virus hemagglutinin antiviral agent fullerene |
| title | Water-Soluble Fullerene C<sub>60</sub> Derivatives Are Effective Inhibitors of Influenza Virus Replication |
| title_full | Water-Soluble Fullerene C<sub>60</sub> Derivatives Are Effective Inhibitors of Influenza Virus Replication |
| title_fullStr | Water-Soluble Fullerene C<sub>60</sub> Derivatives Are Effective Inhibitors of Influenza Virus Replication |
| title_full_unstemmed | Water-Soluble Fullerene C<sub>60</sub> Derivatives Are Effective Inhibitors of Influenza Virus Replication |
| title_short | Water-Soluble Fullerene C<sub>60</sub> Derivatives Are Effective Inhibitors of Influenza Virus Replication |
| title_sort | water soluble fullerene c sub 60 sub derivatives are effective inhibitors of influenza virus replication |
| topic | influenza virus hemagglutinin antiviral agent fullerene |
| url | https://www.mdpi.com/2076-2607/11/3/681 |
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