Anne E Mattingly, Haoting Li, Roberta J Melander, Christian Melander
{"title":"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。","authors":"Anne E Mattingly, Haoting Li, Roberta J Melander, Christian Melander","doi":"10.1021/acsinfecdis.5c00226","DOIUrl":null,"url":null,"abstract":"<p><p>Infections in the lungs of cystic fibrosis (CF) patients are often polymicrobial in nature, typically comprising <i>Pseudomonas aeruginosa</i> and <i>Staphylococcus aureus</i><i>.</i> 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 <i>S. aureus</i>/<i>P. aeruginosa</i> coculture screening model in synthetic sputum, and identified compounds from our in-house library that simultaneously have potent anti-<i>S. aureus</i> activity, and potentiate colistin against colistin-resistant <i>P. aeruginosa</i>. 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.</p>","PeriodicalId":17,"journal":{"name":"ACS Infectious Diseases","volume":" ","pages":"1686-1696"},"PeriodicalIF":3.8000,"publicationDate":"2025-06-13","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Validation of a Cystic Fibrosis Co-Culture Model for the Identification of Dual Acting Compounds with Antibiotic and Antibiotic Adjuvant Properties.\",\"authors\":\"Anne E Mattingly, Haoting Li, Roberta J Melander, Christian Melander\",\"doi\":\"10.1021/acsinfecdis.5c00226\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<p><p>Infections in the lungs of cystic fibrosis (CF) patients are often polymicrobial in nature, typically comprising <i>Pseudomonas aeruginosa</i> and <i>Staphylococcus aureus</i><i>.</i> 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 <i>S. aureus</i>/<i>P. aeruginosa</i> coculture screening model in synthetic sputum, and identified compounds from our in-house library that simultaneously have potent anti-<i>S. aureus</i> activity, and potentiate colistin against colistin-resistant <i>P. aeruginosa</i>. 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.</p>\",\"PeriodicalId\":17,\"journal\":{\"name\":\"ACS Infectious Diseases\",\"volume\":\" \",\"pages\":\"1686-1696\"},\"PeriodicalIF\":3.8000,\"publicationDate\":\"2025-06-13\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"ACS Infectious Diseases\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://doi.org/10.1021/acsinfecdis.5c00226\",\"RegionNum\":2,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"2025/5/11 0:00:00\",\"PubModel\":\"Epub\",\"JCR\":\"Q2\",\"JCRName\":\"CHEMISTRY, MEDICINAL\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"ACS Infectious Diseases","FirstCategoryId":"3","ListUrlMain":"https://doi.org/10.1021/acsinfecdis.5c00226","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2025/5/11 0:00:00","PubModel":"Epub","JCR":"Q2","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
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.
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.