Design, synthesis and anti-influenza virus activities of terminal modified antisense oligonucleotides
摘要:
Four novel terminal modified antisense oligonucleotides (ODNs) were designed, synthesized and tested for their anti-influenza virus activity. Initial biological studies indicated that lipophilic and rimantadin emodificated Flutide exhibited more potent anti-H1N1 activity than Flutide. Among them, lipophilic modificated ODN (Flutide-I) showed the most antiviral activity. The EC50 value of Flutide-I for inhibiting H1N1 induced cytopathic effect (CPE) and H1N1 RNA were respectively (0.26 +/- 0.16) mu M and (0.11 +/- 0.03) mu M. The cytotoxicity of these compounds has also been assessed. No significant cytotoxicities were found for any of these compounds with the concentrations up to 20 mu M. (C) 2013 Elsevier Ltd. All rights reserved.
Design, synthesis and anti-influenza virus activities of terminal modified antisense oligonucleotides
摘要:
Four novel terminal modified antisense oligonucleotides (ODNs) were designed, synthesized and tested for their anti-influenza virus activity. Initial biological studies indicated that lipophilic and rimantadin emodificated Flutide exhibited more potent anti-H1N1 activity than Flutide. Among them, lipophilic modificated ODN (Flutide-I) showed the most antiviral activity. The EC50 value of Flutide-I for inhibiting H1N1 induced cytopathic effect (CPE) and H1N1 RNA were respectively (0.26 +/- 0.16) mu M and (0.11 +/- 0.03) mu M. The cytotoxicity of these compounds has also been assessed. No significant cytotoxicities were found for any of these compounds with the concentrations up to 20 mu M. (C) 2013 Elsevier Ltd. All rights reserved.
Design, synthesis and anti-influenza virus activities of terminal modified antisense oligonucleotides
作者:Jingyu Zhang、Dandan Lu、Aixing Li、Jing Yang、Shengqi Wang
DOI:10.1016/j.tetlet.2013.10.129
日期:2014.1
Four novel terminal modified antisense oligonucleotides (ODNs) were designed, synthesized and tested for their anti-influenza virus activity. Initial biological studies indicated that lipophilic and rimantadin emodificated Flutide exhibited more potent anti-H1N1 activity than Flutide. Among them, lipophilic modificated ODN (Flutide-I) showed the most antiviral activity. The EC50 value of Flutide-I for inhibiting H1N1 induced cytopathic effect (CPE) and H1N1 RNA were respectively (0.26 +/- 0.16) mu M and (0.11 +/- 0.03) mu M. The cytotoxicity of these compounds has also been assessed. No significant cytotoxicities were found for any of these compounds with the concentrations up to 20 mu M. (C) 2013 Elsevier Ltd. All rights reserved.