离子通道抑制剂金刚烷胺、美金刚和金刚乙胺治疗 SARS-CoV-2 的体外疗效。
Efficacy of Ion-Channel Inhibitors Amantadine, Memantine and Rimantadine for the Treatment of SARS-CoV-2 In Vitro.
机构信息
Copenhagen Hepatitis C Program (CO-HEP), Department of Infectious Diseases, Copenhagen University Hospital-Hvidovre, Kettegård Alle 30, 2650 Hvidovre, Denmark.
Copenhagen Hepatitis C Program (CO-HEP), Department of Immunology and Microbiology, Faculty of Health and Medical Sciences, University of Copenhagen, Blegdamsvej 3B, 2200 Copenhagen, Denmark.
出版信息
Viruses. 2021 Oct 15;13(10):2082. doi: 10.3390/v13102082.
We report the in vitro efficacy of ion-channel inhibitors amantadine, memantine and rimantadine against severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2). In VeroE6 cells, rimantadine was most potent followed by memantine and amantadine (50% effective concentrations: 36, 80 and 116 µM, respectively). Rimantadine also showed the highest selectivity index, followed by amantadine and memantine (17.3, 12.2 and 7.6, respectively). Similar results were observed in human hepatoma Huh7.5 and lung carcinoma A549-hACE2 cells. Inhibitors interacted in a similar antagonistic manner with remdesivir and had a similar barrier to viral escape. Rimantadine acted mainly at the viral post-entry level and partially at the viral entry level. Based on these results, rimantadine showed the most promise for treatment of SARS-CoV-2.
我们报告了离子通道抑制剂金刚烷胺、美金刚和金刚乙胺对严重急性呼吸综合征冠状病毒 2（SARS-CoV-2）的体外疗效。在 VeroE6 细胞中，金刚烷胺的活性最强，其次是美金刚和金刚烷胺（50%有效浓度分别为 36、80 和 116µM）。金刚烷胺还显示出最高的选择性指数，其次是金刚烷胺和美金刚（分别为 17.3、12.2 和 7.6）。在人肝癌 Huh7.5 和肺腺癌 A549-hACE2 细胞中也观察到了类似的结果。抑制剂以类似的拮抗方式与瑞德西韦相互作用，对病毒逃逸具有相似的屏障。金刚烷胺主要作用于病毒进入后阶段，部分作用于病毒进入阶段。基于这些结果，金刚烷胺显示出治疗 SARS-CoV-2 的最大潜力。
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