Antiviral activity of novel oseltamivir derivatives against some influenza virus strains

作者：Kocik Janusz; Kolodziej Marcin^*; Joniec Justyna; Kwiatek Magdalena; Bartoszcze Michal

来源：ACTA BIOCHIMICA POLONICA, 2014, 61(3): 509-513.

DOI：10.18388/abp.2014_1872

• influenza virus
• neuraminidase inhibitors
• oseltamivir
• antiviral activity
• cytotoxicity

The aim of this study was to investigate the in vitro cytotoxicity of oseltamivir derivatives and determine their activity against A/H1N1/PR/8/34 and A/H3N2/Hong Kong/8/68 strains of influenza virus. Antiviral activity of these compounds was determined by using two methods. MTT staining was used to assess the viability of MDCK cells infected with influenza viruses and treated with various concentrations of drugs. In parallel, the effect of drugs on viral replication was assessed using the hemagglutination test. The most toxic compounds were: OS-64, OS-35, OS-29, OS-27 and OS-25, whereas OS-11, OS-20 and OS-23 were the least toxic ones. Statistically significant antiviral effect at a higher virus dose was shown by compounds: OS-11, OS-20, OS-27, OS-35, and OS-64. H3N2 virus was sensitive to 10-times lower concentrations of OS-11 and OS-35 than H1N1. At a lower infection dose, the antiviral activity was observed for OS-11, OS 27, OS-35 and OS-20. OS-64 turned out to be effective only at a high concentration. OS-23 showed no antiviral effect.

• 出版日期2014