Zhang Shui-Juan, Jiang Jun-Xia, Ren Qian-Qian, Xie Qiang-Min, Xiong Yao-Kang
Department of Pharmacy, Zhejiang Chinese Medical University, Hangzhou, 310053, China.
Department of Pharmacology, Zhejiang University School of Medicine, Hangzhou, China, 310058.
Drug Dev Res. 2015 May;76(3):123-31. doi: 10.1002/ddr.21248. Epub 2015 May 11.
Bencycloquidium bromide (BCQB), a novel M3 receptor antagonist, alleviates airway hyperresponsiveness, inflammation, and airway remodeling in a murine model of asthma. The aim of this study was to investigate the anti-inflammatory activity of inhaled BCQB in a cigarette smoke (CS)-induced model of acute lung inflammation. Mice exposed to CS developed chronic obstructive pulmonary disease (COPD). Inhalation of BCQB suppressed the accumulation of neutrophils and macrophages in airways and lung and also inhibited the CS-induced increases in mRNA levels of keratinocyte-derived chemokine, monocyte chemotactic protein-1, tumor necrosis factor-alpha, and interleukin-1β in lung and protein expression levels in bronchoalveolar lavage fluid. Moreover, BCQB (300 μg/ml) inhibited the CS-induced changes in superoxide dismutase and myeloperoxidase activities in the lungs. Our study suggests that BCQB might be a potential therapy for inflammation in CS-induced pulmonary diseases, including COPD.
苄环溴铵（BCQB）是一种新型M3受体拮抗剂，可减轻小鼠哮喘模型中的气道高反应性、炎症和气道重塑。本研究的目的是在香烟烟雾（CS）诱导的急性肺部炎症模型中研究吸入BCQB的抗炎活性。暴露于CS的小鼠会发展为慢性阻塞性肺疾病（COPD）。吸入BCQB可抑制气道和肺中中性粒细胞和巨噬细胞的积聚，还可抑制CS诱导的肺中角质形成细胞衍生趋化因子、单核细胞趋化蛋白-1、肿瘤坏死因子-α和白细胞介素-1β的mRNA水平升高以及支气管肺泡灌洗液中的蛋白表达水平升高。此外，BCQB（300μg/ml）可抑制CS诱导的肺中超氧化物歧化酶和髓过氧化物酶活性变化。我们的研究表明，BCQB可能是治疗包括COPD在内的CS诱导的肺部疾病炎症的潜在疗法。
