磷脂酰甘油
两亲性
树枝状大分子
抗菌活性
化学
鲍曼不动杆菌
细菌细胞结构
背景(考古学)
多重耐药
微生物学
生物化学
生物
磷脂
细菌
抗生素
膜
铜绿假单胞菌
有机化学
磷脂酰胆碱
共聚物
聚合物
古生物学
遗传学
作者
N Zhang,Dinesh Dhumal,Shanny Hsuan Kuo,Shi Qian Lew,Pankaj D. Patil,Raléb Taher,Sanika Vaidya,Christina Galanakou,Abdechakour Elkihel,Myung Whan Oh,Sook Yin Chong,Domenico Marson,Jun Zheng,Oleg Rouvinski,Williams O. Abolarin,Sabrina Pricl,Gee W. Lau,Leo Tsz On Lee,Ling Peng
出处
期刊:Science Advances
[American Association for the Advancement of Science (AAAS)]
日期:2024-09-25
卷期号:10 (39)
标识
DOI:10.1126/sciadv.adn8117
摘要
The rapid emergence and spread of multidrug-resistant bacterial pathogens require the development of antibacterial agents that are robustly effective while inducing no toxicity or resistance development. In this context, we designed and synthesized amphiphilic dendrimers as antibacterial candidates. We report the promising potent antibacterial activity shown by the amphiphilic dendrimer AD1b , composed of a long hydrophobic alkyl chain and a tertiary amine-terminated poly(amidoamine) dendron, against a panel of Gram-negative bacteria, including multidrug-resistant Escherichia coli and Acinetobacter baumannii. AD1b exhibited effective activity against drug-resistant bacterial infections in vivo. Mechanistic studies revealed that AD1b targeted the membrane phospholipids phosphatidylglycerol (PG) and cardiolipin (CL), leading to the disruption of the bacterial membrane and proton motive force, metabolic disturbance, leakage of cellular components, and, ultimately, cell death. Together, AD1b that specifically interacts with PG/CL in bacterial membranes supports the use of small amphiphilic dendrimers as a promising strategy to target drug-resistant bacterial pathogens and addresses the global antibiotic crisis.
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