Biophysical Immunology Laboratory, Dept. of Biomedicine, Aarhus University, Aarhus, Denmark.
CF and Chronic Lung Infection, National Heart and Lung Institute, Imperial College London, London, United Kingdom.
Sci Rep. 2017 Nov 15;7(1):15653. doi: 10.1038/s41598-017-15969-3.
Classic drug development strategies have failed to meet the urgent clinical needs in treating infections with Gram-negative bacteria. Repurposing drugs can lead to timely availability of new antibiotics, accelerated by existing safety profiles. Glatiramer acetate (GA) is a widely used and safe formulation for treatment of multiple sclerosis. It contains a large diversity of essentially isomeric polypeptides with the cationic and amphiphilic character of many antimicrobial peptides (AMP). Here, we report that GA is antibacterial, targeting Gram-negative organisms with higher activity towards Pseudomonas aeruginosa than the naturally-occurring AMP LL-37 in human plasma. As judged from flow cytometric assays, bacterial killing by GA occurred within minutes. Laboratory strains of Escherichia coli and P. aeruginosa were killed by a process of condensing intracellular contents. Efficient killing by GA was also demonstrated in Acinetobacter baumannii clinical isolates and approximately 50% of clinical isolates of P. aeruginosa from chronic airway infection in CF patients. By contrast, the Gram-positive Staphylococcus aureus cells appeared to be protected from GA by an increased formation of nm-scale particulates. Our data identify GA as an attractive drug repurposing candidate to treat infections with Gram-negative bacteria.
经典的药物开发策略未能满足治疗革兰氏阴性菌感染的迫切临床需求。重新利用药物可以加速新抗生素的及时供应,利用现有的安全概况。醋酸格拉替雷(GA)是一种广泛使用且安全的多发性硬化症治疗制剂。它包含大量本质上是异构的多肽,具有许多抗菌肽(AMP)的阳离子和两亲性特征。在这里,我们报告 GA 具有抗菌作用,针对革兰氏阴性菌,对铜绿假单胞菌的活性高于人血浆中天然存在的 AMP LL-37。从流式细胞术测定来看,GA 导致细菌在数分钟内被杀灭。实验室培养的大肠杆菌和铜绿假单胞菌通过浓缩细胞内内容物而被杀死。GA 在鲍曼不动杆菌临床分离株和大约 50%的 CF 患者慢性气道感染的铜绿假单胞菌临床分离株中也表现出有效的杀菌作用。相比之下,革兰氏阳性金黄色葡萄球菌细胞似乎通过形成纳米级颗粒而受到 GA 的保护。我们的数据将 GA 鉴定为一种有吸引力的药物再利用候选物,可用于治疗革兰氏阴性菌感染。