Jun Shu , Hui Jiang , Minwei Lin , Jinzhe Liang , Yukun Zhao , Diqing Luo , Jinquan Wang , Hui Chao
{"title":"D-Alanine functionalized Iridium(III) complexes as two-photon photo-antibiotics for bacteria-specific ablation in infected macrophages","authors":"Jun Shu , Hui Jiang , Minwei Lin , Jinzhe Liang , Yukun Zhao , Diqing Luo , Jinquan Wang , Hui Chao","doi":"10.1016/j.ejmech.2025.117758","DOIUrl":null,"url":null,"abstract":"<div><div>The prevalence of bacterial resistance, driven by extensive antibiotic overuse, significantly threatens patient safety. Consequently, it is urgent and helpful for the clinician to develop new antibacterial therapy techniques. In this study, we designed a novel photodynamic antibacterial therapeutic strategy by functionalizing D-alanine on Iridium(III) complexes. The synergistic D-alanine metabolic labeling function and two-photon photodynamic eradication capacity of Ir(III) complexes enable bacterial imaging and elimination of bacterial pathogens within host cells. These two-photon photoantibiotics effectively inhibit bacterial biofilm formation and efficiently eliminate intracellular bacterial infections in macrophages, enabling real-time dynamic monitoring of antimicrobial efficacy. Furthermore, both in vitro and <em>in vivo</em> experiments demonstrated superior antibacterial performance compared to conventional antibiotics alone.</div></div>","PeriodicalId":314,"journal":{"name":"European Journal of Medicinal Chemistry","volume":"294 ","pages":"Article 117758"},"PeriodicalIF":6.0000,"publicationDate":"2025-05-15","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"European Journal of Medicinal Chemistry","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0223523425005239","RegionNum":2,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CHEMISTRY, MEDICINAL","Score":null,"Total":0}
引用次数: 0
Abstract
The prevalence of bacterial resistance, driven by extensive antibiotic overuse, significantly threatens patient safety. Consequently, it is urgent and helpful for the clinician to develop new antibacterial therapy techniques. In this study, we designed a novel photodynamic antibacterial therapeutic strategy by functionalizing D-alanine on Iridium(III) complexes. The synergistic D-alanine metabolic labeling function and two-photon photodynamic eradication capacity of Ir(III) complexes enable bacterial imaging and elimination of bacterial pathogens within host cells. These two-photon photoantibiotics effectively inhibit bacterial biofilm formation and efficiently eliminate intracellular bacterial infections in macrophages, enabling real-time dynamic monitoring of antimicrobial efficacy. Furthermore, both in vitro and in vivo experiments demonstrated superior antibacterial performance compared to conventional antibiotics alone.
期刊介绍:
The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers.
A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.