Design, synthesis and anti-influenza virus activities of terminal modified antisense oligonucleotides

被引：0
|
作者：
Zhang, Jingyu [1 ,2 ]
Lu, Dandan [1 ]
Li, Aixing [3 ]
Yang, Jing [1 ]
Wang, Shengqi [1 ,2 ]
机构：
[1] Beijing Inst Radiat Med, Beijing 100850, Peoples R China
[2] Henan Univ Tradit Chinese Med, Zhengzhou 450008, Peoples R China
[3] Zhengzhou Univ, Sch Pharmaceut Sci, Zhengzhou 450001, Peoples R China
来源：
TETRAHEDRON LETTERS | 2014年 / 55卷 / 01期
基金：
中国国家自然科学基金;
关键词：
Antisense oligonucleotides; Influenza virus; H1N1; Terminal modification; EXPRESSION; DELIVERY; CELLS;
D O I：
10.1016/j.tetlet.2013.10.129
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
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.
引用
收藏
页码：94 / 97
页数：4
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