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瑞德西韦、洛匹那韦、依米丁和高三尖杉酯碱在体外抑制 SARS-CoV-2 复制。

Remdesivir, lopinavir, emetine, and homoharringtonine inhibit SARS-CoV-2 replication in vitro.

机构信息

School of Public Health, LKS Faculty of Medicine, The University of Hong Kong, Hong Kong SAR, China.

Department of Chemistry, Hong Kong University of Science and Technology, Hong Kong SAR, China.

出版信息

Antiviral Res. 2020 Jun;178:104786. doi: 10.1016/j.antiviral.2020.104786. Epub 2020 Apr 3.

Abstract

An escalating pandemic by the novel SARS-CoV-2 virus is impacting global health and effective therapeutic options are urgently needed. We evaluated the in vitro antiviral effect of compounds that were previously reported to inhibit coronavirus replication and compounds that are currently under evaluation in clinical trials for SARS-CoV-2 patients. We report the antiviral effect of remdesivir, lopinavir, homorringtonine, and emetine against SARS-CoV-2 virus in Vero E6 cells with the estimated 50% effective concentration at 23.15 μM, 26.63 μM, 2.55 μM and 0.46 μM, respectively. Ribavirin or favipiravir that are currently evaluated under clinical trials showed no inhibition at 100 μM. Synergy between remdesivir and emetine was observed, and remdesivir at 6.25 μM in combination with emetine at 0.195 μM may achieve 64.9% inhibition in viral yield. Combinational therapy may help to reduce the effective concentration of compounds below the therapeutic plasma concentrations and provide better clinical benefits.

摘要

新型 SARS-CoV-2 病毒引发的大流行正在影响全球健康,急需有效的治疗方法。我们评估了先前报道的能抑制冠状病毒复制的化合物和目前正在临床试验中评估的用于 SARS-CoV-2 患者的化合物对 Vero E6 细胞中 SARS-CoV-2 病毒的体外抗病毒作用。我们报告了瑞德西韦、洛匹那韦、高三尖杉酯碱和依米丁对 SARS-CoV-2 病毒的抗病毒作用,其估计 50%有效浓度分别为 23.15 μM、26.63 μM、2.55 μM 和 0.46 μM。目前正在临床试验中评估的利巴韦林或法匹拉韦在 100 μM 时没有抑制作用。我们观察到瑞德西韦和依米丁之间存在协同作用,瑞德西韦 6.25 μM 与依米丁 0.195 μM 联合使用可能使病毒产量达到 64.9%的抑制率。联合治疗可能有助于将化合物的有效浓度降低到治疗血浆浓度以下,并提供更好的临床获益。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/12bc/7127386/ec4a3aed5534/gr1_lrg.jpg

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