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乙烯基膦酸(共)聚物的合成及其抗流感活性

Synthesis and Anti-influenza Activity of Vinylphosphonic Acid (Co)polymers.

作者信息

Zarubaev V V, Buchkov E V, Nazarova O V, Zolotova Yu I, Panarin E F

机构信息

St. Petersburg Pasteur Institute, St. Petersburg, Russia.

Peter the Great St. Petersburg Polytechnic University, St. Petersburg, Russia.

出版信息

Dokl Biochem Biophys. 2022 Oct;506(1):227-230. doi: 10.1134/S1607672922050155. Epub 2022 Oct 27.

Abstract

New copolymers of vinylphosphonic acid (VPA) with 2-deoxy-2-methacrylamido-D-glucose, 4-acryloylmorpholine (4-AM), and acrylamide have been synthesized, and their antiviral activity against influenza virus has been studied in in vitro and in vivo experiments. Optimal antiviral characteristics and low cytotoxicity were exhibited by the copolymer of VPA with 4-AM, composition 56 : 44 mol %, molecular weight 33 000. The polymer exhibited virus-inhibiting properties with an IC = 1 µg/mL and a selectivity index of 302. Prophylactic intranasal administration of the polymer in a murine model of influenza pneumonia completely prevented the virus-induced death of animals, whereas the level of mortality in the placebo group was 90%. The results of this study indicate a high antiviral potential of polymeric compounds based on VPA.

摘要

已合成了乙烯基膦酸(VPA)与2-脱氧-2-甲基丙烯酰胺基-D-葡萄糖、4-丙烯酰基吗啉(4-AM)和丙烯酰胺的新型共聚物,并在体外和体内实验中研究了它们对流感病毒的抗病毒活性。VPA与4-AM的共聚物(组成56∶44摩尔%,分子量33 000)表现出最佳的抗病毒特性和低细胞毒性。该聚合物表现出病毒抑制特性,IC = 1 µg/mL,选择性指数为302。在流感肺炎小鼠模型中预防性鼻内给药该聚合物可完全防止病毒诱导的动物死亡,而安慰剂组的死亡率为90%。本研究结果表明基于VPA的聚合物化合物具有很高的抗病毒潜力。

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