Laboratory of Medicinal Plant Biotechnology, College of Pharmacy, Zhejiang Chinese Medical University, Hangzhou, Zhejiang, 310053, PR China.
Department of Bio-resources and Food Science, Konkuk University, Seoul, 143701, South Korea.
Food Chem Toxicol. 2020 Jan;135:110985. doi: 10.1016/j.fct.2019.110985. Epub 2019 Nov 22.
Investigation of antiviral and cytotoxic effect of quercetin 3-glucoside (Q3G) from Dianthus superbus L over influenza virus infection and replication were studied. Moreover, anti-influenza mechanism was screened by time-dependent antiviral assay, virus-induced symptoms and related gene expressions. The blockade of cap-binding domain of polymerase basic protein subunit were analysed by molecular docking study. The Q3G demonstrated potent antiviral activity showing 4.93, 6.43, 9.94, 8.3, and 7.1 μg/mL of IC for A/PR/8/34, A/Victoria/3/75, A/WS/33, B/Maryland/1/59, and B/Lee/40, respectively. The cellular toxicity of Q3G and oseltamivir (control) were tested and >100 μg/mL of CC value considered as nontoxic. Influenza A virus infection induced a higher ROS production, however potentially reduced by Q3G treatment and significantly blocked virus infection induced acidic vesicular organelles (AVO). Moreover, Q3G has no inhibitory effect for neuraminidase activity but blocked virus replication through time dependent assay and showed more competitive binding affinity (-8.0 kcal/mal) than GTP (-7.0 kcal/mol) to block polymerase basic protein-2 subunit of influenza virus. Q3G from D. superbus showed potent antiviral activity against influenza A and B viruses with suppressive effect on virus-induced cellular ROS generation and AVO formation. Thus, this study provided a new line of research for Q3G to develop possible natural anti-influenza drug.
研究了来自瞿麦（ Dianthus superbus L ）的槲皮素 3-葡萄糖苷（Q3G）对流感病毒感染和复制的抗病毒和细胞毒性作用。此外，通过时间依赖性抗病毒测定、病毒诱导的症状和相关基因表达筛选了抗流感机制。通过分子对接研究分析了聚合酶碱性蛋白亚基的帽结合域的阻断。Q3G 表现出很强的抗病毒活性，对 A/PR/8/34、A/Victoria/3/75、A/WS/33、B/Maryland/1/59 和 B/Lee/40 的 IC 分别为 4.93、6.43、9.94、8.3 和 7.1μg/mL。测试了 Q3G 和奥司他韦（对照）的细胞毒性，CC 值>100μg/mL 被认为是非毒性的。流感 A 病毒感染诱导更高的 ROS 产生，但 Q3G 处理可潜在降低，并且可显著阻断病毒感染诱导的酸性囊泡细胞器（AVO）。此外，Q3G 对神经氨酸酶活性没有抑制作用，但通过时间依赖性测定可阻断病毒复制，并显示出比 GTP（-7.0 kcal/mol）更强的竞争结合亲和力（-8.0 kcal/mol）来阻断流感病毒聚合酶碱性蛋白 2 亚基。瞿麦中的 Q3G 对甲型和乙型流感病毒表现出很强的抗病毒活性，并对病毒诱导的细胞 ROS 产生和 AVO 形成具有抑制作用。因此，这项研究为 Q3G 开发可能的天然抗流感药物提供了新的研究方向。
