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水溶性富勒烯C衍生物是流感病毒复制的有效抑制剂。

Water-Soluble Fullerene C Derivatives Are Effective Inhibitors of Influenza Virus Replication.

作者信息

Sinegubova Ekaterina O, Kraevaya Olga A, Volobueva Aleksandrina S, Zhilenkov Alexander V, Shestakov Alexander F, Baykov Sergey V, Troshin Pavel A, Zarubaev Vladimir V

机构信息

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.

出版信息

Microorganisms. 2023 Mar 7;11(3):681. doi: 10.3390/microorganisms11030681.

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 , 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.

摘要

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。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/e8a5/10053623/d8314208023e/microorganisms-11-00681-g001.jpg

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