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Targeted and Intracellular Antibacterial Activity against S. agalactiae of the Chimeric Peptides Based on Pheromone and Cell-penetrating Peptides.
ACS Applied Materials & Interfaces ( IF 8.3 ) Pub Date : 2020-09-14 , DOI: 10.1021/acsami.0c12226 Jiawei Li 1 , Lu Shang 1 , Jing Lan 1 , Shuli Chou 1 , Xingjun Feng 1 , Baoming Shi 1 , Jiajun Wang 1 , Yinfeng Lyu 1 , Anshan Shan 1
ACS Applied Materials & Interfaces ( IF 8.3 ) Pub Date : 2020-09-14 , DOI: 10.1021/acsami.0c12226 Jiawei Li 1 , Lu Shang 1 , Jing Lan 1 , Shuli Chou 1 , Xingjun Feng 1 , Baoming Shi 1 , Jiajun Wang 1 , Yinfeng Lyu 1 , Anshan Shan 1
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The significance of the complex bacterial ecosystem in the human body and the impediment of the mammalian membrane against many antibiotics together emphasize the necessity to develop antimicrobial agents with precise antimicrobial and cell-penetrating activities. A simple and feasible method for generating dual-function antimicrobial peptides inspired by highly hydrophobic peptide pheromone and cationic cell-penetrating peptides is presented. Furthermore, the extension of the peptide candidate library is achieved by modifying the charged domain. The bacteria-selective peptides L1, L2, L10, and L11 kill Streptococcus agalactiae by disrupting the membrane structure, and the targeted mechanism is suggested where the peptides offset the entrapment of S. agalactiae rather than of other bacteria. Moreover, L2 and L10 possess intracellular antibacterial activity and carrier property, which is mainly dependent on endocytosis. Given their suitable biocompatibility, high tolerance, no drug resistance, and effective antimicrobial capacity in a mouse mastitis model, L2 and L10 can be powerful weapons against S. agalactiae pathogen infection.
中文翻译：
针对信息素和细胞穿透肽的嵌合肽对无乳链球菌的靶向和细胞内抗菌活性。
复杂的细菌生态系统在人体中的重要性以及哺乳动物膜对许多抗生素的阻碍共同强调了开发具有精确抗菌和穿透细胞活性的抗菌剂的必要性。提出了一种简单可行的方法，以产生由高疏水性肽信息素和阳离子细胞穿透肽启发的双功能抗菌肽。此外，通过修饰带电域实现了肽候选库的扩展。细菌选择性肽L1，L2，L10和L11通过破坏膜结构杀死无乳链球菌，并提出了靶向机制，其中该肽抵消了无乳链球菌的包裹。而不是其他细菌。此外，L2和L10具有细胞内抗菌活性和载体性质，这主要取决于内吞作用。由于L2和L10具有合适的生物相容性，高耐受性，无耐药性以及在小鼠乳腺炎模型中具有有效的抗菌能力，因此它们可以有效抵抗无乳链球菌病原体感染。
更新日期：2020-10-07
中文翻译：
针对信息素和细胞穿透肽的嵌合肽对无乳链球菌的靶向和细胞内抗菌活性。
复杂的细菌生态系统在人体中的重要性以及哺乳动物膜对许多抗生素的阻碍共同强调了开发具有精确抗菌和穿透细胞活性的抗菌剂的必要性。提出了一种简单可行的方法，以产生由高疏水性肽信息素和阳离子细胞穿透肽启发的双功能抗菌肽。此外，通过修饰带电域实现了肽候选库的扩展。细菌选择性肽L1，L2，L10和L11通过破坏膜结构杀死无乳链球菌，并提出了靶向机制，其中该肽抵消了无乳链球菌的包裹。而不是其他细菌。此外，L2和L10具有细胞内抗菌活性和载体性质，这主要取决于内吞作用。由于L2和L10具有合适的生物相容性，高耐受性，无耐药性以及在小鼠乳腺炎模型中具有有效的抗菌能力，因此它们可以有效抵抗无乳链球菌病原体感染。
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