Brazilian Biosciences National Laboratory (LNBio), Brazilian Center for Research in Energy and Materials (CNPEM), Campinas 13083-100, Brazil.
Department of Genetics, Microbiology and Immunology, Institute of Biology, State University of Campinas (UNICAMP), Campinas 13083-100, Brazil.
Viruses. 2023 Dec 13;15(12):2416. doi: 10.3390/v15122416.
St. Louis encephalitis virus (SLEV) is a neglected mosquito-borne Flavivirus that may cause severe neurological disease in humans and other animals. There are no specific treatments against SLEV infection or disease approved for human use, and drug repurposing may represent an opportunity to accelerate the development of treatments against SLEV. Here we present a scalable, medium-throughput phenotypic cell culture-based screening assay on Vero CCL81 cells to identify bioactive compounds that could be repurposed against SLEV infection. We screened eighty compounds from the Medicines for Malaria Venture (MMV) COVID Box library to identify nine (11%) compounds that protected cell cultures from SLEV-induced cytopathic effects, with low- to mid-micromolar potencies. We validated six hit compounds using viral plaque-forming assays to find that the compounds ABT-239, Amiodarone, Fluphenazine, Posaconazole, Triparanol, and Vidofludimus presented varied levels of antiviral activity and selectivity depending on the mammalian cell type used for testing. Importantly, we identified and validated the antiviral activity of the anti-flavivirus nucleoside analog 7DMA against SLEV. Triparanol and Fluphenazine reduced infectious viral loads in both Vero CCL81 and HBEC-5i cell cultures and, similar to the other validated compounds, are likely to exert antiviral activity through a molecular target in the host.
圣路易斯脑炎病毒(SLEV)是一种被忽视的蚊媒黄病毒,它可能导致人类和其他动物严重的神经疾病。目前尚无针对 SLEV 感染或疾病的特异性治疗方法获得批准用于人类,药物再利用可能是加速开发针对 SLEV 的治疗方法的机会。在这里,我们在 Vero CCL81 细胞上建立了一种可扩展的、基于细胞培养的高通量表型筛选测定法,以鉴定可用于治疗 SLEV 感染的生物活性化合物。我们从抗疟疾药物 Venture(MMV)COVID 盒库中筛选了 80 种化合物,以鉴定出 9 种(11%)化合物可保护细胞培养免受 SLEV 诱导的细胞病变效应,其效力为低至中微摩尔。我们使用病毒噬斑形成测定法验证了 6 种命中化合物,发现化合物 ABT-239、胺碘酮、氟奋乃静、泊沙康唑、曲普拉醇和 Vidofludimus 根据用于测试的哺乳动物细胞类型,具有不同程度的抗病毒活性和选择性。重要的是,我们鉴定并验证了抗病毒药物核苷类似物 7DMA 对 SLEV 的抗病毒活性。曲普拉醇和氟奋乃静降低了 Vero CCL81 和 HBEC-5i 细胞培养物中的感染性病毒载量,并且与其他验证的化合物类似,可能通过宿主中的分子靶标发挥抗病毒活性。