PDF(Pubmed)
Abstract：
Previous data have suggested an antiviral effect of teriflunomide, including against severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), the agent underlying the ongoing COVID-19 pandemic. We undertook an in vitro investigation to evaluate the inhibitory activity of teriflunomide against SARS-CoV-2 in a cell-based assay. Teriflunomide was added to Vero (kidney epithelial) cells that had been infected with SARS-CoV-2. A nucleocapsid immunofluorescence assay was performed to examine viral inhibition with teriflunomide and any potential cytotoxic effect. The 50% effective concentration (EC50) for teriflunomide against SARS-CoV-2 was 15.22 μM. No cytotoxicity was evident for teriflunomide in the Vero cells (i.e., the 50% cytotoxic concentration [CC50] was greater than the highest test concentration of 100 μM). The data were supported by additional experiments using other coronaviruses and human cell lines. In the SARS-CoV-2-infected Vero cells, the prodrug leflunomide had an EC50 of 16.49 μM and a CC50 of 54.80 μM. Our finding of teriflunomide-mediated inhibition of SARS-CoV-2 infection at double-digit micromolar potency adds to a growing body of evidence for a broad-ranging antiviral effect of teriflunomide.
摘要：
以前的数据表明特立氟胺具有抗病毒作用，包括针对严重急性呼吸道综合症冠状病毒-2（SARS-CoV-2），正在进行的COVID-19大流行的潜在因素。我们进行了体外研究，以评估特立氟胺对SARS-CoV-2的抑制活性。将特立氟胺加入已经感染SARS-CoV-2的Vero(肾上皮)细胞中。进行核衣壳免疫荧光测定以检查特立氟胺对病毒的抑制作用和任何潜在的细胞毒性作用。特立氟胺对SARS-CoV-2的50%有效浓度(EC50)为15.22μM。特立氟胺在Vero细胞中没有明显的细胞毒性(即，50%细胞毒性浓度[CC50]大于100μM的最高测试浓度)。使用其他冠状病毒和人细胞系的其他实验支持了数据。在SARS-CoV-2感染的Vero细胞中,前药来氟米特的EC50为16.49μM,CC50为54.80μM.我们发现特立氟胺介导的以两位数微摩尔效力抑制SARS-CoV-2感染的发现增加了越来越多的证据表明特立氟胺具有广泛的抗病毒作用。
