Yamamoto Keisuke, Yamamoto Soh, Ogasawara Noriko, Takano Kenichi, Shiraishi Tsukasa, Sato Toyotaka, Miyata Ryo, Kakuki Takuya, Kamekura Ryuta, Kojima Takashi, Tsutsumi Hiroyuki, Himi Tetsuo, Yokota Shin-Ichi
Department of Otorhinolaryngology, Sapporo Medical University School of Medicine, Sapporo, Japan.
Department of Microbiology, Sapporo Medical University School of Medicine, Sapporo, Japan.
Pharmacol Res. 2016 Sep;111:804-814. doi: 10.1016/j.phrs.2016.07.033. Epub 2016 Jul 26.
Macrolide antibiotics exert immunomodulatory activity by reducing pro-inflammatory cytokine production by airway epithelial cells, fibroblasts, vascular endothelial cells, and immune cells. However, the underlying mechanism of action remains unclear. Here, we examined the effect of clarithromycin (CAM) on pro-inflammatory cytokine production, including interferons (IFNs), by primary human nasal epithelial cells and lung epithelial cell lines (A549 and BEAS-2B cells) after stimulation by Toll-like receptor (TLR) and RIG-I-like receptor (RLR) agonists and after infection by human respiratory syncytial virus (RSV). CAM treatment led to a significant reduction in poly I:C- and RSV-mediated IL-8, CCL5, IFN-β and -λ production. Furthermore, IFN-β promoter activity (activated by poly I:C and RSV infection) was significantly reduced after treatment with CAM. CAM also inhibited IRF-3 dimerization and subsequent translocation to the nucleus. We conclude that CAM acts a crucial modulator of the innate immune response, particularly IFN production, by modulating IRF-3 dimerization and subsequent translocation to the nucleus of airway epithelial cells. This newly identified immunomodulatory action of CAM will facilitate the discovery of new macrolides with an anti-inflammatory role.
大环内酯类抗生素通过减少气道上皮细胞、成纤维细胞、血管内皮细胞和免疫细胞产生促炎细胞因子来发挥免疫调节活性。然而,其潜在的作用机制仍不清楚。在此,我们检测了克拉霉素(CAM)对原代人鼻上皮细胞和肺上皮细胞系(A549和BEAS-2B细胞)在受到Toll样受体(TLR)和RIG-I样受体(RLR)激动剂刺激后以及感染人呼吸道合胞病毒(RSV)后促炎细胞因子产生的影响,这些促炎细胞因子包括干扰素(IFN)。CAM处理导致多聚肌苷酸胞苷酸(poly I:C)和RSV介导的白细胞介素-8(IL-8)、趋化因子配体5(CCL5)、IFN-β和IFN-λ产生显著减少。此外,用CAM处理后,(由poly I:C和RSV感染激活的)IFN-β启动子活性显著降低。CAM还抑制干扰素调节因子3(IRF-3)二聚化及其随后向细胞核易位。我们得出结论,CAM通过调节IRF-3二聚化及其随后向气道上皮细胞核易位,从而作为先天性免疫反应尤其是IFN产生的关键调节因子。CAM这种新发现的免疫调节作用将有助于发现具有抗炎作用的新型大环内酯类药物。