囊性纤维化共培养模型的验证,用于鉴定具有抗生素和抗生素佐剂特性的双重作用化合物。

IF 3.8 2区 医学 Q2 CHEMISTRY, MEDICINAL
ACS Infectious Diseases Pub Date : 2025-06-13 Epub Date: 2025-05-11 DOI:10.1021/acsinfecdis.5c00226
Anne E Mattingly, Haoting Li, Roberta J Melander, Christian Melander
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引用次数: 0

摘要

囊性纤维化(CF)患者的肺部感染通常是多微生物性的,通常包括铜绿假单胞菌和金黄色葡萄球菌。作为抗其中一种病原体的抗菌剂和作为抗另一种病原体的抗生素佐剂的化合物可以为治疗此类感染提供有价值的方法,然而,需要一个模拟CF肺中发现的独特环境的模型来鉴定和表征这些分子。为了解决这个问题,我们采用了金黄色葡萄球菌/P。合成痰中铜绿假单胞菌共培养筛选模型,并从我们的内部文库中鉴定出同时具有强效抗s的化合物。并增强粘菌素对抗耐粘菌素铜绿假单胞菌。当与亚抑制浓度的粘菌素一起给药时,两种先导化合物12F1和12G9可以控制这两种细菌的生长,这突出了在多微生物感染中使用单分子作为抗生素和抗生素佐剂来靶向多种细菌的潜力,以及在临床相关介质中进行活性筛选的重要性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Validation of a Cystic Fibrosis Co-Culture Model for the Identification of Dual Acting Compounds with Antibiotic and Antibiotic Adjuvant Properties.

Infections in the lungs of cystic fibrosis (CF) patients are often polymicrobial in nature, typically comprising Pseudomonas aeruginosa and Staphylococcus aureus. Compounds that act as an antimicrobial agent against one of these pathogens, and as an antibiotic adjuvant against the other, could provide a valuable approach to treating such infections, however a model that mimics the unique environment found with the CF lung is required for the identification and characterization of such molecules. To address this, we employed a S. aureus/P. aeruginosa coculture screening model in synthetic sputum, and identified compounds from our in-house library that simultaneously have potent anti-S. aureus activity, and potentiate colistin against colistin-resistant P. aeruginosa. The two lead compounds, 12F1 and 12G9, control growth of both species when dosed alongside sub-inhibitory concentrations of colistin, highlighting the potential of using a single molecule as both an antibiotic and antibiotic adjuvant to target multiple species in polymicrobial infections, as well as the importance of conducting activity screens in clinically relevant media.

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来源期刊
ACS Infectious Diseases
ACS Infectious Diseases CHEMISTRY, MEDICINALINFECTIOUS DISEASES&nb-INFECTIOUS DISEASES
CiteScore
9.70
自引率
3.80%
发文量
213
期刊介绍: ACS Infectious Diseases will be the first journal to highlight chemistry and its role in this multidisciplinary and collaborative research area. The journal will cover a diverse array of topics including, but not limited to: * Discovery and development of new antimicrobial agents — identified through target- or phenotypic-based approaches as well as compounds that induce synergy with antimicrobials. * Characterization and validation of drug target or pathways — use of single target and genome-wide knockdown and knockouts, biochemical studies, structural biology, new technologies to facilitate characterization and prioritization of potential drug targets. * Mechanism of drug resistance — fundamental research that advances our understanding of resistance; strategies to prevent resistance. * Mechanisms of action — use of genetic, metabolomic, and activity- and affinity-based protein profiling to elucidate the mechanism of action of clinical and experimental antimicrobial agents. * Host-pathogen interactions — tools for studying host-pathogen interactions, cellular biochemistry of hosts and pathogens, and molecular interactions of pathogens with host microbiota. * Small molecule vaccine adjuvants for infectious disease. * Viral and bacterial biochemistry and molecular biology.
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