Infection and Immunity Program, Monash Biomedicine Discovery Institute, Department of Biochemistry and Molecular Biology, Monash University, Clayton, Victoria, 3800, Australia.
ARC Centre of Excellence for Innovations in Peptide and Protein Science, Monash University, Clayton, Victoria, 3800, Australia.
Nat Commun. 2021 Oct 25;12(1):6157. doi: 10.1038/s41467-021-26244-5.
The pathogen Staphylococcus aureus can readily develop antibiotic resistance and evade the human immune system, which is associated with reduced levels of neutrophil recruitment. Here, we present a class of antibacterial peptides with potential to act both as antibiotics and as neutrophil chemoattractants. The compounds, which we term 'antibiotic-chemoattractants', consist of a formylated peptide (known to act as chemoattractant for neutrophil recruitment) that is covalently linked to the antibiotic vancomycin (known to bind to the bacterial cell wall). We use a combination of in vitro assays, cellular assays, infection-on-a-chip and in vivo mouse models to show that the compounds improve the recruitment, engulfment and killing of S. aureus by neutrophils. Furthermore, optimizing the formyl peptide sequence can enhance neutrophil activity through differential activation of formyl peptide receptors. Thus, we propose antibiotic-chemoattractants as an alternate approach for antibiotic development.
病原体金黄色葡萄球菌很容易产生抗生素耐药性并逃避人体免疫系统,这与中性粒细胞募集减少有关。在这里,我们提出了一类具有作为抗生素和中性粒细胞趋化剂双重作用的抗菌肽。这些化合物被称为“抗生素-趋化剂”,由一种甲酰化肽(已知作为中性粒细胞募集的趋化剂)与抗生素万古霉素(已知与细菌细胞壁结合)共价连接而成。我们使用体外测定、细胞测定、芯片感染和体内小鼠模型的组合来表明这些化合物可以改善中性粒细胞对金黄色葡萄球菌的募集、吞噬和杀伤作用。此外,优化甲酰化肽序列可以通过差异激活甲酰肽受体来增强中性粒细胞的活性。因此,我们提出抗生素-趋化剂作为抗生素开发的替代方法。