Eropkin M Yu, Solovskii M V, Smirnova M Yu, Bryazzhikova T S, Gudkova T M, Konovalova N I
1Research Institute of Influenza, Russian Academy of Medical Sciences, ul. Prof. Popova 15/17, St. Petersburg, 197376 Russia.
2Institute of High-Molecular-Weight Compounds, Russian Academy of Sciences, Bol shoi pr. 31, St. Petersburg, 199004 Russia.
Pharm Chem J. 2009;43(10):563-567. doi: 10.1007/s11094-010-0351-7. Epub 2010 Feb 4.
We have synthesized water-soluble complexes between the antiviral drug arbidol and polymer compounds with molecular masses of 19-31 kDa representing copolymers of acrylamide (AA) and 2-acrylamido-2-methylpropanesulfonic acid (AAMPS). The complexes are less toxic than arbidol and retain the high level of antiviral activity of this drug. The content of arbidol in the obtained complexes is within 26.4-32.1 mass%. The antiviral activity of the synthesized polymeric complexes against all studied viruses, including human epidemic influenza virus A (H3N2), bird highly pathogenic influenza virus A (H5N1), herpes type 1 virus (HSV-1), and adenovirus type III (AV-III) is comparable to the antiviral effect of nonmodified arbidol. The toxicity of the obtained complexes is about one order of magnitude lower than that of nonmodified arbidol; the pharmacological index, four times that of the initial low-molecular-weight drug. The synthesized water-soluble polymer complexes of arbidol can be useful in pharmacology since they can serve as the basis for new effective and safe parent antiviral substances and related formulations.
我们合成了抗病毒药物阿比朵尔与分子量为19 - 31 kDa的聚合物化合物之间的水溶性复合物，该聚合物化合物为丙烯酰胺（AA）和2 - 丙烯酰胺基 - 2 - 甲基丙烷磺酸（AAMPS）的共聚物。这些复合物的毒性低于阿比朵尔，并且保留了该药物的高抗病毒活性水平。所得复合物中阿比朵尔的含量在26.4 - 32.1质量%范围内。合成的聚合物复合物对所有研究的病毒，包括人类甲型流行性感冒病毒（H3N2）、高致病性甲型禽流感病毒（H5N1）、1型疱疹病毒（HSV - 1）和III型腺病毒（AV - III）的抗病毒活性与未修饰的阿比朵尔的抗病毒效果相当。所得复合物的毒性比未修饰的阿比朵尔低约一个数量级；药理指数是初始低分子量药物的四倍。合成的阿比朵尔水溶性聚合物复合物在药理学中可能有用，因为它们可作为新型有效且安全的母体抗病毒物质及相关制剂的基础。
