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共价固定化抗菌肽巴亭脂质体凝胶对细菌生物膜的活性。

Covalently Immobilized Battacin Lipopeptide Gels with Activity against Bacterial Biofilms.

机构信息

School of Chemical Sciences and the Centre for Green Chemical Science, The University of Auckland, Auckland 1142, New Zealand.

School of Science, Auckland University of Technology, 34 St Paul Street, Auckland 1142, New Zealand.

出版信息

Molecules. 2020 Dec 15;25(24):5945. doi: 10.3390/molecules25245945.

Abstract

Novel antibiotic treatments are in increasing demand to tackle life-threatening infections from bacterial pathogens. In this study, we report the use of a potent battacin lipopeptide as an antimicrobial gel to inhibit planktonic and mature biofilms of and . The antimicrobial gels were made by covalently linking the -terminal cysteine containing lipopeptide (GZ3.163) onto the polyethylene glycol polymer matrix and initiating gelation using thiol-ene click chemistry. The gels were prepared both in methanol and in water and were characterised using rheology, Fourier transform infrared (FT-IR) spectroscopy and scanning electron microscopy (SEM). Antibacterial and antibiofilm analyses revealed that the gels prepared in methanol have better antibacterial and antibiofilm activity. Additionally, a minimum peptide content of 0.5 wt% (relative to polymer content) is required to successfully inhibit the planktonic bacterial growth and disperse mature biofilms of and . The antibacterial activity of these lipopeptide gels is mediated by a contact kill mechanism of action. The gels are non-haemolytic against mouse red blood cells and are non-cytotoxic against human dermal fibroblasts. Findings from this study show that battacin lipopeptide gels have the potential to be developed as novel topical antibacterial agents to combat skin infections, particularly caused by .

摘要

新型抗生素治疗方法的需求日益增长,以应对由细菌病原体引起的危及生命的感染。在这项研究中,我们报告了使用一种有效的巴塔西林脂肽作为抗菌凝胶来抑制 和 的浮游生物和成熟生物膜。抗菌凝胶是通过将含有半胱氨酸的末端脂肽(GZ3.163)共价连接到聚乙二醇聚合物基质上,并使用硫醇-烯点击化学引发凝胶化来制备的。凝胶分别在甲醇和水中制备,并通过流变学、傅里叶变换红外(FT-IR)光谱和扫描电子显微镜(SEM)进行了表征。抗菌和抗生物膜分析表明,在甲醇中制备的凝胶具有更好的抗菌和抗生物膜活性。此外,成功抑制浮游细菌生长和分散 和 成熟生物膜需要至少 0.5wt%(相对于聚合物含量)的肽含量。这些脂肽凝胶的抗菌活性是通过接触杀伤作用机制介导的。这些凝胶对小鼠红细胞无溶血作用,对人皮肤成纤维细胞无细胞毒性。这项研究的结果表明,巴塔西林脂肽凝胶有可能被开发为新型局部抗菌剂,以治疗皮肤感染,特别是由 引起的感染。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a3a0/7765475/73e15ef80eae/molecules-25-05945-sch001.jpg

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