School of Molecular and Biomedical Science, University of Adelaide, Adelaide, Australia.
Antimicrob Agents Chemother. 2013 Nov;57(11):5291-8. doi: 10.1128/AAC.01003-13. Epub 2013 Aug 12.
Nucleic acid polymers (NAPs) utilize the sequence-independent properties of phosphorothioate oligonucleotides (PS-ONs) to target protein interactions involved in viral replication. NAPs are broadly active against a diverse range of enveloped viruses that use type I entry mechanisms. The antiviral activity of NAPs against hepatitis B virus (HBV) infection was assessed in vitro in duck hepatitis B virus (DHBV)-infected primary duck hepatocytes (PDH). NAPs efficiently entered PDH in the absence of any transfection agent and displayed antiviral activity at concentrations of 0.01 to 10 μM, measured by their ability to prevent the intracellular accumulation of DHBV surface antigen, which was independent of their nucleotide sequence and was specifically dependent on phosphorothioation. Higher levels of antiviral activity were observed with NAPs 40 nucleotides in length or longer. The fully degenerate NAP (REP 2006) was active during DHBV infection or when added 12 h after infection. In contrast, an acidic-pH-sensitive NAP (REP 2031) that was broadly active against other viruses displayed antiviral activity when present during DHBV infection but no activity when added 12 h after infection, suggesting that NAPs exert their postentry effect in an acidic environment unique to DHBV infection. Both REP 2006 and REP 2031 displayed negligible cytotoxicity in PDH at concentrations of up to 10 μM, as assessed using an XTT [2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide] cytotoxicity assay. The antiviral activity of NAPs against DHBV in vitro was strictly dependent on their amphipathic character, suggesting that NAPs interact with amphipathic target(s) that are important for DHBV entry and postentry mechanisms required for infection.
核酸聚合物 (NAPs) 利用硫代磷酸酯寡核苷酸 (PS-ONs) 的序列非依赖性特性,靶向参与病毒复制的蛋白质相互作用。NAPs 对广泛使用 I 型进入机制的包膜病毒具有广泛的活性。在感染鸭乙型肝炎病毒 (DHBV) 的原代鸭肝细胞 (PDH) 中,体外评估了 NAPs 对乙型肝炎病毒 (HBV) 感染的抗病毒活性。NAPs 在没有任何转染剂的情况下有效地进入 PDH,并在 0.01 至 10 μM 的浓度下显示抗病毒活性,这是通过其阻止 DHBV 表面抗原在细胞内积累的能力来衡量的,这与它们的核苷酸序列无关,而是特异性依赖于硫代磷酸化。具有 40 个核苷酸或更长的 NAP 观察到更高水平的抗病毒活性。完全简并的 NAP(REP 2006)在 DHBV 感染期间或在感染后 12 小时添加时具有活性。相比之下,在其他病毒中广泛具有活性的酸性 pH 敏感 NAP(REP 2031)在 DHBV 感染期间存在时具有抗病毒活性,但在感染后 12 小时添加时没有活性,这表明 NAPs 在 DHBV 感染特有的酸性环境中发挥其进入后效应。在高达 10 μM 的浓度下,使用 XTT [2,3-双-(2-甲氧基-4-硝基-5-磺苯基)-2H-四唑-5-羧基苯胺]细胞毒性测定法评估,REP 2006 和 REP 2031 在 PDH 中均表现出可忽略不计的细胞毒性。NAPs 对 DHBV 的体外抗病毒活性严格依赖于它们的两亲性特征,这表明 NAPs 与两亲性靶标相互作用,这些靶标对 DHBV 进入和感染所需的进入后机制很重要。