Santus Pierachille, Strizzi Sergio, Danzo Fiammetta, Biasin Mara, Saulle Irma, Vanetti Claudia, Saad Marina, Radovanovic Dejan, Trabattoni Daria
Division of Respiratory Diseases, Ospedale L. Sacco, ASST Fatebenefratelli-Sacco, 20147 Milan, Italy.
Department of Biomedical and Clinical Sciences (DIBIC), Università degli Studi di Milano, 20122 Milan, Italy.
Pathogens. 2025 Apr 15;14(4):388. doi: 10.3390/pathogens14040388.
Respiratory viral infections trigger immune and inflammatory responses that can be associated with excessive oxidative stress, glutathione (GSH) depletion, and a cytokine storm that drives virus-induced cell/tissue damage and severe disease. Erdosteine is a thiol-based drug with proven mucolytic, anti-inflammatory, antioxidant, and antibacterial properties, but less is known about its antiviral effects. We performed in vitro studies to investigate the antiviral and anti-inflammatory activity of erdosteine in A549-hACE2 human lung epithelial cells infected with severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) or respiratory syncytial virus (RSV) and in Caco-2 human colon carcinoma cells infected with influenza A virus (H1N1). The cells were treated with different concentrations of erdosteine or its active metabolite 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MET-1) before and after viral infection. The viral replication/load in the cell culture supernatants was measured by real-time quantitative polymerase chain reaction (RT-qPCR) assay and digital droplet PCR. The gene expression of innate immune response signaling pathways and oxidative stress was analyzed by reverse transcription PCR custom-array. The results showed that erdosteine and its active metabolite, at concentrations consistent with an approved therapeutic human dosage, were not directly cytotoxic and had significant antiviral effects in cells pre-infected with SARS-CoV-2, RSV, and H1N1. The transcriptome analysis showed that erdosteine activated innate immune responses by stimulating overexpression of type I interferon and inflammasome pathways and modulated oxidative stress by inducing the modulation of oxidative stress and GSH pathways. These findings suggest that erdosteine may be a useful treatment for respiratory viral infections.
呼吸道病毒感染会引发免疫和炎症反应,这些反应可能与过度氧化应激、谷胱甘肽(GSH)耗竭以及驱动病毒诱导的细胞/组织损伤和严重疾病的细胞因子风暴有关。厄多司坦是一种基于硫醇的药物,具有已证实的黏液溶解、抗炎、抗氧化和抗菌特性,但对其抗病毒作用了解较少。我们进行了体外研究,以调查厄多司坦在感染严重急性呼吸综合征冠状病毒2(SARS-CoV-2)或呼吸道合胞病毒(RSV)的A549-hACE2人肺上皮细胞以及感染甲型流感病毒(H1N1)的Caco-2人结肠癌细胞中的抗病毒和抗炎活性。在病毒感染前后,用不同浓度的厄多司坦或其活性代谢物3-(4,5-二甲基噻唑-2-基)-2,5-二苯基-2H-四唑溴盐(MET-1)处理细胞。通过实时定量聚合酶链反应(RT-qPCR)测定法和数字液滴PCR测量细胞培养上清液中的病毒复制/载量。通过逆转录PCR定制阵列分析先天免疫反应信号通路和氧化应激的基因表达。结果表明,厄多司坦及其活性代谢物在与批准的治疗性人体剂量一致的浓度下,没有直接细胞毒性,并且在预先感染SARS-CoV-2、RSV和H1N1的细胞中具有显著的抗病毒作用。转录组分析表明,厄多司坦通过刺激I型干扰素和炎性小体途径的过表达激活先天免疫反应,并通过诱导氧化应激和GSH途径的调节来调节氧化应激。这些发现表明,厄多司坦可能是治疗呼吸道病毒感染的有效药物。