| 张洋,李文淼,王伟.海洋来源的吲哚生物碱衍生物抗流感病毒作用研究[J].中国海洋药物,2020,39(1):19-25. |
| 海洋来源的吲哚生物碱衍生物抗流感病毒作用研究 |
| Studies on the Anti-Influenza Virus Activity of indole alkaloid from Marine |
| 投稿时间：2019-08-21 修订日期：2019-08-30 |
| DOI： |
| 中文关键词: 抗流感病毒，海洋来源化合物，吲哚生物碱，神经氨酸酶，病毒释放 |
| English Keywords:Anti-influenza virus, Marine derived compound, indole alkaloid, Neuraminidase, Virus release |
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| 中文摘要: |
| 目的 对海洋来源的吲哚生物碱类化合物HDYL-GQQ-1932进行体外抗流感病毒活性研究。方法 CPE抑制实验测定HDYL-GQQ-1932对多种病毒株的增殖抑制作用。CPE实验结合血凝抑制和神经氨酸酶活性实验探究HDYL-GQQ-1932 作用病毒入侵细胞的方式以及细胞毒性,并且初步探究HDYL-GQQ-1932的作用靶点。 结果 HDYL-GQQ-1932体外对多种流感病毒株均有增殖抑制作用,其中对H1N1的抑制作用最强,IC50为26.1μM ,且无明显的细胞毒性,CC50为3313.2μM。通过不同作用方式以及不同作用时间的实验显示,感染后加入 HDYL-GQQ-1932能够很好的抑制病毒增值,且用HDYL-GQQ-1932预处理细胞后可明显降低病毒增殖。此外结果显示HDYL-GQQ-1932在病毒吸附后6-9 h有很好的抑制作用,且剂量依赖性地抑制神经氨酸酶(NA)的活力。故 HDYL-GQQ-1932可能是通过结合病毒神经氨酸酶并抑制其活性来阻断IAV的释放过程。结论 HDYL-GQQ-1932体外对甲型流感具有较好的抑制效果。本研究为海洋来源的该类小分子化合物的药物开发与理性改造提供了思路与方向。 |
| English Summary: |
| Objective To study the anti-influenza virus activity of compound HDYL-GQQ-1932 derived from marine indole alkaloid in vitro. Methods Cytopathic effect (CPE) inhibition assay was used to determine the inhibitory effect of HDYL-GQQ-1932 on the proliferation of various viral strains. CPE experiments combined with hemagglutinin inhibition and neuraminidase activity assay were used to explore the action mechanisms and cytotoxicity, and reveal the antiviral taget of HDYL-GQQ-1932.Results HDYL-GQQ-1932 inhibited the proliferation of different influenza virus strains in vitro, especially H1N1. The IC50 value for H1N1 inhibition was 26.1 uM and The CC50 value was 3313.2 uM, suggesting that HDYL-GQQ-1932 had no obvious cytotoxicity. The results showed that the addition of HDYL-GQQ-1932 after adsorption could effectively inhibit the growth of viruses, and pretreatment of cells could also reduce the viral titers. In addition, HDYL-GQQ-1932 showed a good inhibition effect during 6-9 hours post virus infection, and dose-dependently inhibited the activity of neuraminidase. Therefore, HDYL-GQQ-1932 may block the release of IAV by binding to viral neuraminidase (NA) and inhibiting the activity of NA. Conclusion HDYL-GQQ-1932 has a good inhibitory effect on influenza A virus in vitro. This study provides ideas and directions for the future drug development and rational modification of this small molecule compound. |
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