State Key Laboratory of Pathogen and Biosecurity, Beijing Institute of Microbiology and Epidemiology, Beijing 100071, China.
CAMS Key Laboratory of Antiviral Drug Research, Beijing Key Laboratory of Antimicrobial Agents, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
Molecules. 2022 Jan 21;27(3):712. doi: 10.3390/molecules27030712.
COVID-19 has spread around the world and caused serious public health and social problems. Although several vaccines have been authorized for emergency use, new effective antiviral drugs are still needed. Some repurposed drugs including Chloroquine, Hydroxychloroquine and Remdesivir were immediately used to treat COVID-19 after the pandemic. However, the therapeutic effects of these drugs have not been fully demonstrated in clinical studies. In this paper, we found an antimalarial drug, Naphthoquine, showed good broad-spectrum anti-coronavirus activity. Naphthoquineinhibited HCoV-229E, HCoV-OC43 and SARS-CoV-2 replication in vitro, with IC = 2.05 ± 1.44 μM, 5.83 ± 0.74 μM, and 2.01 ± 0.38 µM, respectively. Time-of-addition assay was also performed to explore at which stage Naphthoquine functions during SARS-CoV-2 replication. The results suggested that Naphthoquine may influence virus entry and post-entry replication. Considering the safety of Naphthoquine was even better than that of Chloroquine, we think Naphthoquine has the potential to be used as a broad-spectrum drug for coronavirus infection.
新型冠状病毒肺炎(COVID-19)在全球范围内传播,造成了严重的公共卫生和社会问题。虽然已经有几种疫苗获得了紧急使用授权,但仍需要新的有效抗病毒药物。一些已被重新用于治疗其他疾病的药物,包括氯喹、羟氯喹和瑞德西韦,在大流行后立即被用于治疗 COVID-19。然而,这些药物的治疗效果在临床研究中尚未得到充分证实。在本文中,我们发现一种抗疟药物萘喹啉对冠状病毒具有良好的广谱抗病毒活性。萘喹啉在体外抑制 HCoV-229E、HCoV-OC43 和 SARS-CoV-2 的复制,IC = 2.05 ± 1.44 μM、5.83 ± 0.74 μM 和 2.01 ± 0.38 µM。加药时间测定实验也探索了萘喹啉在 SARS-CoV-2 复制过程中的哪个阶段发挥作用。结果表明,萘喹啉可能影响病毒进入和进入后复制。考虑到萘喹啉的安全性甚至优于氯喹,我们认为萘喹啉有可能成为一种广谱抗冠状病毒感染药物。