Department of Microbiology, Icahn School of Medicine at Mount Sinai, New York, NY, USA.
Global Health Emerging Pathogens Institute, Icahn School of Medicine at Mount Sinai, New York, NY, USA.
Science. 2021 Feb 26;371(6532):926-931. doi: 10.1126/science.abf4058. Epub 2021 Jan 25.
Severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) viral proteins interact with the eukaryotic translation machinery, and inhibitors of translation have potent antiviral effects. We found that the drug plitidepsin (aplidin), which has limited clinical approval, possesses antiviral activity (90% inhibitory concentration = 0.88 nM) that is more potent than remdesivir against SARS-CoV-2 in vitro by a factor of 27.5, with limited toxicity in cell culture. Through the use of a drug-resistant mutant, we show that the antiviral activity of plitidepsin against SARS-CoV-2 is mediated through inhibition of the known target eEF1A (eukaryotic translation elongation factor 1A). We demonstrate the in vivo efficacy of plitidepsin treatment in two mouse models of SARS-CoV-2 infection with a reduction of viral replication in the lungs by two orders of magnitude using prophylactic treatment. Our results indicate that plitidepsin is a promising therapeutic candidate for COVID-19.
严重急性呼吸综合征冠状病毒 2(SARS-CoV-2)病毒蛋白与真核翻译机制相互作用,而翻译抑制剂具有强大的抗病毒作用。我们发现,药物普乐沙福(aplidin)具有抗病毒活性(90%抑制浓度=0.88nM),比瑞德西韦在体外对 SARS-CoV-2 的抑制作用强 27.5 倍,在细胞培养中毒性有限。通过使用耐药突变体,我们表明普乐沙福抑制 SARS-CoV-2 的抗病毒活性是通过抑制已知的靶标 eEF1A(真核翻译延伸因子 1A)介导的。我们在两种 SARS-CoV-2 感染的小鼠模型中证明了普乐沙福治疗的体内疗效,通过预防性治疗,肺部病毒复制减少了两个数量级。我们的研究结果表明,普乐沙福是治疗 COVID-19 的一种很有前途的治疗候选药物。