Key Laboratory of Medical Molecular Virology (MOE/NHC/CAMS), School of Basic Medical Sciences, Shanghai Institute of Infectious Disease and Biosecurity, Biosafety Level 3 Laboratory, Shanghai Medical College, Shanghai Frontiers Science Center of Pathogenic Microbes and Infection, Fudan University, Shanghai 200438, China.
Beijing Institute of Radiation Medicine, Beijing 200032, China.
Viruses. 2022 Feb 27;14(3):489. doi: 10.3390/v14030489.
In recent years, infectious diseases caused by viral infections have seriously endangered human health, especially COVID-19, caused by SARS-CoV-2, which continues to spread worldwide. The development of broad-spectrum antiviral inhibitors is urgently needed. Here, we report a series of small-molecule compounds that proved effective against human coronaviruses (HCoV), such as SARS-CoV-2 and its variants of concern (VOCs), including Alpha (B.1.1.7), Beta (B.1.351), Gamma (P.1), Delta (B.1.617.2), and Omicron (B.1.1.529), SARS-CoV, MERS-CoV, HCoV-OC43, and other viruses with class I viral fusion proteins, such as influenza virus, Ebola virus (EBOV), Nipah virus (NiV), and Lassa fever virus (LASV). They are also effective against class II enveloped viruses represented by ZIKV and class III enveloped viruses represented by vesicular stomatitis virus (VSV). Further studies have shown that these compounds may exert antiviral effects through a variety of mechanisms, including inhibiting the formation of the six-helix bundle, which is a typical feature of enveloped virus fusion with cell membranes, and/or targeting viral membrane to inactivate cell-free virions. These compounds are expected to become drug candidates against SARS-CoV-2 and other enveloped viruses.
近年来,由病毒感染引起的传染病严重威胁着人类健康,尤其是由 SARS-CoV-2 引起的持续在全球范围内传播的 COVID-19。因此,迫切需要开发广谱抗病毒抑制剂。在这里,我们报告了一系列小分子化合物,它们对人类冠状病毒(HCoV),如 SARS-CoV-2 及其关注的变异株(VOCs),包括 Alpha(B.1.1.7)、Beta(B.1.351)、Gamma(P.1)、Delta(B.1.617.2)和 Omicron(B.1.1.529)、SARS-CoV、MERS-CoV、HCoV-OC43 以及具有 I 类病毒融合蛋白的其他病毒,如流感病毒、埃博拉病毒(EBOV)、尼帕病毒(NiV)和拉萨热病毒(LASV),均具有有效的抑制作用。它们对以 ZIKV 为代表的 II 类包膜病毒和以 VSV 为代表的 III 类包膜病毒也具有抑制作用。进一步的研究表明,这些化合物可能通过多种机制发挥抗病毒作用,包括抑制六螺旋束的形成,这是包膜病毒与细胞膜融合的典型特征,和/或靶向病毒膜使无细胞病毒失活。这些化合物有望成为针对 SARS-CoV-2 和其他包膜病毒的候选药物。