穆雷帕瓦定通过抑制药物外排增强环丙沙星对……的杀菌效力。（原文中“against”后缺少具体对象）

Murepavadin Enhances the Killing Efficacy of Ciprofloxacin against by Inhibiting Drug Efflux.

作者信息

Wei Xiaoya, Zhou Dandan, Xu Congjuan, Chen Ping, Chen Shuiping, Cheng Zhihui, Jin Yongxin, Jin Shouguang, Wu Weihui

机构信息

State Key Laboratory of Medicinal Chemical Biology, Key Laboratory of Molecular Microbiology and Technology of the Ministry of Education, Department of Microbiology, College of Life Sciences, Nankai University, Tianjin 300071, China.

Department of Laboratory Medicine, 5th Medical Center of PLA General Hospital, Beijing 100071, China.

出版信息

Antibiotics (Basel). 2024 Aug 26;13(9):810. doi: 10.3390/antibiotics13090810.

DOI:10.3390/antibiotics13090810

PMID:39334985

原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC11429200/

Abstract

is a multidrug-resistant Gram-negative pathogen and one of the leading causes of ventilator-associated pneumonia and infections in patients with chronic obstructive pulmonary disease and cystic fibrosis. Murepavadin is a peptidomimetic that specifically targets outer-membrane lipopolysaccharide transport protein LptD of . In this study, we find that murepavadin enhances the bactericidal efficacy of ciprofloxacin. We further demonstrate that murepavadin increases intracellular accumulation of ciprofloxacin by suppressing drug efflux. In addition, the murepavadin-ciprofloxacin combination exhibits a synergistic bactericidal effect in an acute murine pneumonia model. In conclusion, our results identify an effective drug combination for the treatment of infections.

摘要

是一种多重耐药革兰氏阴性病原体，是呼吸机相关性肺炎以及慢性阻塞性肺疾病和囊性纤维化患者感染的主要原因之一。穆雷帕瓦定是一种拟肽，专门靶向……的外膜脂多糖转运蛋白LptD。在本研究中，我们发现穆雷帕瓦定增强了环丙沙星的杀菌效力。我们进一步证明，穆雷帕瓦定通过抑制药物外排增加了环丙沙星在细胞内的积累。此外，穆雷帕瓦定-环丙沙星组合在急性小鼠肺炎模型中表现出协同杀菌作用。总之，我们的结果确定了一种治疗……感染的有效药物组合。