Improved Antibacterial Activity of the Marine Peptide N6 against Intracellular Salmonella Typhimurium by Conjugating with the Cell-Penetrating Peptide Tat(11) via a Cleavable Linker

文献类型： 外文期刊

第一作者： Li, Zhanzhan

作者： Li, Zhanzhan;Teng, Da;Mao, Ruoyu;Wang, Xiao;Hao, Ya;Wang, Xiumin;Wang, Jianhua;Li, Zhanzhan;Teng, Da;Mao, Ruoyu;Wang, Xiao;Hao, Ya;Wang, Xiumin;Wang, Jianhua

作者机构：

期刊名称：JOURNAL OF MEDICINAL CHEMISTRY （ 影响因子：7.446； 五年影响因子：7.319 ）

ISSN： 0022-2623

年卷期： 2018 年 61 卷 17 期

页码：

收录情况： SCI

摘要： The poor penetration ability of antimicrobial agents limits their use in the treatment of intracellular bacteria. In this study, the conjugate CNC (6) was generated by connecting the cell-penetrating peptide Tat(11) (1) and marine peptide N6 (2) via a cathepsin-cleavable linker, and the C-terminal aminated N6 (7) and CNC (8) were first designed and synthesized to eliminate intracellular Salmonellae Typhimurium. The cellular uptake of 6 and stability of 7 were higher than those of 2, and conjugates 6, 8, and 7 had almost no hemolysis and cytotoxicity. The antibacterial activities of 6, 8, and 7 against S. Typhimurium in RAW264.7 cells were increased by 67.2-76.2%, 98.6-98.9%, and 96.3-97.6%, respectively. After treatment with 1-2 mu mol/kg of 6, 8, or 7, the survival of the S. Typhimurium-infected mice was 66.7-100%, higher than that of 2 (33.4-66.7%). This result suggested that 6, 8, and 7 may be excellent candidates for novel antimicrobial agents to treat intracellular pathogens.

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