Murepavadin 通过增强膜电位提高氨基糖苷类抗生素对 的杀伤效力。
Murepavadin promotes the killing efficacies of aminoglycoside antibiotics against by enhancing membrane potential.
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, China.
Department of Laboratory Medicine, 5th Medical Center of PLA General Hospital, Beijing, China.
出版信息
Antimicrob Agents Chemother. 2024 Apr 3;68(4):e0153923. doi: 10.1128/aac.01539-23. Epub 2024 Mar 12.
Abstract
Murepavadin is a peptidomimetic that specifically targets the lipopolysaccharide transport protein LptD of . Here, we found that murepavadin enhances the bactericidal efficacies of tobramycin and amikacin. We further demonstrated that murepavadin enhances bacterial respiration activity and subsequent membrane potential, which promotes intracellular uptake of aminoglycoside antibiotics. In addition, the murepavadin-amikacin combination displayed a synergistic bactericidal effect in a murine pneumonia model.
摘要
美罗培南是一种针对 脂多糖转运蛋白 LptD 的肽模拟物。在这里，我们发现美罗培南增强了妥布霉素和阿米卡星的杀菌效果。我们进一步证明，美罗培南增强了细菌的呼吸活性和随后的膜电位，从而促进了氨基糖苷类抗生素的细胞内摄取。此外，美罗培南-阿米卡星联合用药在肺炎小鼠模型中显示出协同杀菌作用。
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