Sinegubova Ekaterina O, Kraevaya Olga A, Volobueva Aleksandrina S, Zhilenkov Alexander V, Shestakov Alexander F, Baykov Sergey V, Troshin Pavel A, Zarubaev Vladimir V
Saint Petersburg Pasteur Institute, 14 Ulitsa Mira, 197101 St. Petersburg, Russia.
Federal Research Center for Problems of Chemical Physics and Medicinal Chemistry RAS, 1 Prospekt Akademika Semenova, 142432 Chernogolovka, Russia.
Microorganisms. 2023 Mar 7;11(3):681. doi: 10.3390/microorganisms11030681.
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 , containing residues of salts of 2-amino-3-cyclopropylpropanoic acid (CC > 300 µg/mL, IC = 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 (-) have pharmacological prospects.
流感病毒基因组具有非常高的突变率，导致耐药毒株迅速出现。由于耐药毒株的出现，需要进一步开发新型强效的抗流感病毒药物，且具有广谱活性。因此，寻找一种新型、有效的广谱抗病毒药物是医学和医疗保健系统的首要任务。本文描述了基于富勒烯的衍生物，其在体外对一组流感病毒具有广泛的病毒抑制活性。研究了水溶性富勒烯衍生物的抗病毒特性。结果表明，基于富勒烯的化合物库具有细胞保护活性。化合物含有2-氨基-3-环丙基丙酸的盐残基，具有最大的病毒抑制活性和最小的毒性（CC>300μg/mL，IC=4.73μg/mL，SI=64）。本研究是富勒烯作为抗流感药物研究的初始阶段。研究结果使我们得出结论，五种主要化合物（-）具有药理学前景。
