Division of Pharmacology, Utrecht Institute for Pharmaceutical Sciences, Faculty of Science, Utrecht University, 3584 CG Utrecht, The Netherlands.
Sulfateq B.V., Admiraal de Ruyterlaan 5, 9726 GN Groningen, The Netherlands.
Int J Mol Sci. 2021 May 8;22(9):4991. doi: 10.3390/ijms22094991.
Chronic obstructive pulmonary disease (COPD) caused by cigarette smoke (CS) is featured by oxidative stress and chronic inflammation. Due to the poor efficacy of standard glucocorticoid therapy, new treatments are required. Here, we investigated whether the novel compound SUL-151 with mitoprotective properties can be used as a prophylactic and therapeutic treatment in a murine CS-induced inflammation model. SUL-151 (4 mg/kg), budesonide (500 μg/kg), or vehicle were administered via oropharyngeal instillation in this prophylactic and therapeutic treatment setting. The number of immune cells was determined in the bronchoalveolar lavage fluid (BALF). Oxidative stress response, mitochondrial adenosine triphosphate (ATP) production, and mitophagy-related proteins were measured in lung homogenates. SUL-151 significantly decreased more than 70% and 50% of CS-induced neutrophils in BALF after prophylactic and therapeutic administration, while budesonide showed no significant reduction in neutrophils. Moreover, SUL-151 prevented the CS-induced decrease in ATP and mitochondrial mtDNA and an increase in putative protein kinase 1 expression in the lung homogenates. The concentration of SUL-151 was significantly correlated with malondialdehyde level and radical scavenging activity in the lungs. SUL-151 inhibited the increased pulmonary inflammation and mitochondrial dysfunction in this CS-induced inflammation model, which implied that SUL-151 might be a promising candidate for COPD treatment.
慢性阻塞性肺疾病(COPD)由香烟烟雾(CS)引起,其特征为氧化应激和慢性炎症。由于标准糖皮质激素治疗的疗效不佳,需要新的治疗方法。在这里,我们研究了具有线粒体保护特性的新型化合物 SUL-151 是否可用于 CS 诱导的炎症模型的预防和治疗。通过口咽滴注在该预防和治疗设置中给予 SUL-151(4mg/kg)、布地奈德(500μg/kg)或载体。在支气管肺泡灌洗液(BALF)中测定免疫细胞的数量。在肺匀浆中测量氧化应激反应、三磷酸腺苷(ATP)的产生和与线粒体自噬相关的蛋白质。SUL-151 在预防和治疗给药后可显著降低 BALF 中超过 70%和 50%的 CS 诱导的中性粒细胞,而布地奈德对中性粒细胞没有显著降低作用。此外,SUL-151 可防止 CS 诱导的肺匀浆中 ATP 和线粒体 mtDNA 减少以及假定蛋白激酶 1 表达增加。SUL-151 的浓度与肺中的丙二醛水平和自由基清除活性呈显著相关。SUL-151 抑制了 CS 诱导的炎症模型中肺部炎症和线粒体功能障碍的增加,这意味着 SUL-151 可能是 COPD 治疗的有前途的候选药物。