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KRN7000类似物作为针对化脓性链球菌和奇异变形杆菌的生物膜破坏剂。

KRN7000 analogues as biofilm disrupting agents against Streptococcus pyogenes and Proteus mirabilis.

作者信息

Krishnakumar K A, Remya Babu R, Sugathan Shiburaj, Lankalapalli Ravi S

机构信息

Chemical Sciences and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology, Thiruvananthapuram, 695019, India.

Academy of Scientific and Innovative Research (AcSIR), Ghaziabad, 201002, India.

出版信息

J Antibiot (Tokyo). 2025 Mar;78(4):246-255. doi: 10.1038/s41429-025-00810-1. Epub 2025 Feb 14.

Abstract

In this study, three KRN7000 analogues with variations in the sugar and glycosidic linkage were synthesised to assess their efficacy in disrupting the biofilms of S. pyogenes and P. mirabilis. All three analogues exhibited antibacterial activity, with the effects being more prominent at lower concentrations in S. pyogenes. The N-alkylated, 1-deoxy analogue emerged as the most effective, significantly reducing biofilm formation and extracellular polymeric substances (EPS) in both organisms. Microscopic analysis revealed notable disruption of biofilm structure by the analogue, resulting in a significant reduction in EPS for both organisms and decreasing cell surface hydrophobicity. These results position the KRN7000 analogue as a promising candidate for developing glycolipid-based antibiofilm agents.

摘要

在本研究中,合成了三种糖和糖苷键有所变化的KRN7000类似物,以评估它们破坏化脓性链球菌和奇异变形杆菌生物膜的功效。所有三种类似物均表现出抗菌活性,在较低浓度下对化脓性链球菌的作用更为显著。N-烷基化的1-脱氧类似物最为有效,能显著减少两种细菌中的生物膜形成和细胞外聚合物(EPS)。显微镜分析显示,该类似物对生物膜结构有显著破坏,导致两种细菌的EPS显著减少,并降低细胞表面疏水性。这些结果表明,KRN7000类似物是开发基于糖脂的抗生物膜药物的有前景的候选物。

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