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首页> 外文期刊>Chemistry: A European journal >Cell Penetrating Synthetic Antimicrobial Peptides (SAMPs) Exhibiting Potent and Selective Killing of Mycobacterium by Targeting Its DNA
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Cell Penetrating Synthetic Antimicrobial Peptides (SAMPs) Exhibiting Potent and Selective Killing of Mycobacterium by Targeting Its DNA

机译：细胞穿透合成抗菌肽（SAMPs）通过靶向其DNA表现出强力和选择性杀灭分枝杆菌的能力

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摘要

Naturally occurring antimicrobial peptides (AMPs) are powerful defence tools to tackle pathogenic microbes. However, limited natural production and high synthetic costs in addition to poor selectivity limit large-scale use of AMPs in clinical settings. Here, we present a series of synthetic AMPs (SAMPs) that exhibit highly selective and potent killing of Mycobacterium (minimum inhibitory concentration <20gmL(-1)) over E.coli or mammalian cells. These SAMPs are active against rapidly multiplying as well as growth saturated Mycobacterium cultures. These SAMPs are not membrane-lytic in nature, and are readily internalized by Mycobacterium and mammalian cells; whereas in E.coli, the lipopolysaccharide layer inhibits their cellular uptake, and hence, their antibacterial action. Upon internalization, these SAMPs interact with the unprotected genomic DNA of mycobacteria, and impede DNA-dependent processes, leading to bacterial cell death.
机译：天然存在的抗菌肽（AMP）是解决病原微生物的强大防御工具。然而，除了选择性差之外，有限的天然生产和高合成成本限制了AMP在临床环境中的大规模使用。在这里，我们介绍了一系列合成的AMP（SAMP），它们对大肠杆菌或哺乳动物细胞表现出高度选择性和有效的杀灭分枝杆菌的作用（最低抑制浓度<20gmL（-1））。这些SAMP对快速繁殖以及饱和分枝杆菌培养物具有活性。这些SAMP本质上不是膜溶解性的，很容易被分枝杆菌和哺乳动物细胞内化。而在大肠杆菌中，脂多糖层抑制其细胞摄取，从而抑制其抗菌作用。内化后，这些SAMP与分枝杆菌的未保护基因组DNA相互作用，并阻止DNA依赖性过程，从而导致细菌细胞死亡。

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