Institute for Virology and Immunobiology, University of Würzburg, Würzburg, Germany.
Fraunhofer Institute for Toxicology and Experimental Medicine ITEM, Member of Fraunhofer International Consortium for Anti-Infective Research (iCAIR), Member of the German Center for Lung Research (DZL), Biomedical Research in Endstage and Obstructive Lung Disease (BREATH), Hannover, Germany.
Front Cell Infect Microbiol. 2023 Aug 11;13:1100028. doi: 10.3389/fcimb.2023.1100028. eCollection 2023.
Recently, Tummino et al. reported that 34 compounds, including Chloroquine and Fluoxetine, inhibit SARS-CoV-2 replication by inducing phospholipidosis, although Chloroquine failed to suppress viral replication in Calu-3 cells and patients. In contrast, Fluoxetine represses viral replication in human precision-cut lung slices (PCLS) and Calu-3 cells. Thus, it is unlikely that these compounds have similar mechanisms of action. Here, we analysed a subset of these compounds in the viral replication and phospholipidosis assays using the Calu-3 cells and PCLS as the patient-near system. Trimipramine and Chloroquine induced phospholipidosis but failed to inhibit SARS-CoV-2 replication in Calu-3 cells, which contradicts the reported findings and the proposed mechanism. Fluoxetine, only slightly induced phospholipidosis in Calu-3 cells but reduced viral replication by 2.7 orders of magnitude. Tilorone suppressed viral replication by 1.9 orders of magnitude in Calu-3 cells without causing phospholipidosis. Thus, induction of phospholipidosis is not correlated with the inhibition of SARS-CoV-2, and the compounds act via other mechanisms. However, we show that compounds, such as Amiodarone, Tamoxifen and Tilorone, with antiviral activity on Calu-3 cells, also inhibited viral replication in human PCLS. Our results indicate that antiviral assays against SARS-CoV-2 are cell-line specific. Data from Vero E6 can lead to non-transferable results, underlining the importance of an appropriate cell system for analysing antiviral compounds against SARS-CoV-2. We observed a correlation between the active compounds in Calu-3 cells and PCLS.
最近,Tummino 等人报告说,包括氯喹和氟西汀在内的 34 种化合物通过诱导磷脂病来抑制 SARS-CoV-2 复制,尽管氯喹未能抑制 Calu-3 细胞和患者中的病毒复制。相比之下,氟西汀抑制人精密切割肺切片(PCLS)和 Calu-3 细胞中的病毒复制。因此,这些化合物不太可能具有相似的作用机制。在这里,我们使用 Calu-3 细胞和 PCLS 作为接近患者的系统,在病毒复制和磷脂病测定中分析了这些化合物中的一部分。曲米帕明和氯喹诱导了磷脂病,但未能抑制 Calu-3 细胞中的 SARS-CoV-2 复制,这与报道的发现和提出的机制相矛盾。氟西汀仅在 Calu-3 细胞中轻度诱导磷脂病,但将病毒复制减少了 2.7 个数量级。替洛隆在 Calu-3 细胞中抑制病毒复制达 1.9 个数量级,而不会引起磷脂病。因此,诱导磷脂病与抑制 SARS-CoV-2 无关,这些化合物通过其他机制起作用。然而,我们表明,阿莫多林、他莫昔芬和替洛隆等在 Calu-3 细胞中具有抗病毒活性的化合物,也抑制了人 PCLS 中的病毒复制。我们的结果表明,针对 SARS-CoV-2 的抗病毒测定是细胞系特异性的。来自 Vero E6 的数据可能导致不可转移的结果,这凸显了针对 SARS-CoV-2 分析抗病毒化合物时使用适当细胞系统的重要性。我们观察到 Calu-3 细胞和 PCLS 中活性化合物之间存在相关性。