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Fabrication of Supramolecular Antibacterial Nanofibers with Membrane-Disruptive Mechanism
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-11-16 , DOI: 10.1021/acs.jmedchem.1c00829 Tingting Chen 1 , Yinfeng Lyu 1 , Meishu Tan 1 , Chengyi Yang 1 , Ying Li 1 , Changxuan Shao 1 , Yongjie Zhu 1 , Anshan Shan 1
Journal of Medicinal Chemistry ( IF 6.8 ) Pub Date : 2021-11-16 , DOI: 10.1021/acs.jmedchem.1c00829 Tingting Chen 1 , Yinfeng Lyu 1 , Meishu Tan 1 , Chengyi Yang 1 , Ying Li 1 , Changxuan Shao 1 , Yongjie Zhu 1 , Anshan Shan 1
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By studying the principles of self-assembly and combining the structural parameters required for the asymmetric distribution of antimicrobial peptides (AMPs), we newly designed and screened the high-activity and low-toxicity AMP F2I-LL. This peptide can form a supramolecular hydrogel with a nanofiber microstructure in a simulated physiological environment (phosphate buffered saline), which exhibits broad-spectrum antibacterial activity. Compared with monomeric peptides, the introduction of a self-assembly strategy not only improved the bactericidal titer but also enhanced the serum stability of AMPs. Mechanistic studies showed that the positive charge enriched on the surface of the nanofiber was conducive to its rapid binding to the negatively charged part of the outer membrane of bacteria and further entered the inner membrane, increasing its permeability and ultimately leading to cell membrane rupture and death. This work provides insights into the design of nanopeptides with broad-spectrum antibacterial activity and provides new results for the development of biomedicine.
中文翻译：
具有破膜机制的超分子抗菌纳米纤维的制备
通过研究自组装原理，结合抗菌肽（AMPs）不对称分布所需的结构参数，我们新设计并筛选出高活性、低毒的AMP F2I-LL。该肽可在模拟生理环境（磷酸盐缓冲盐水）中形成具有纳米纤维微结构的超分子水凝胶，具有广谱抗菌活性。与单体肽相比，自组装策略的引入不仅提高了杀菌效价，而且增强了 AMPs 的血清稳定性。机理研究表明，纳米纤维表面富集的正电荷有利于其迅速与细菌外膜带负电的部分结合，进一步进入内膜，增加其通透性并最终导致细胞膜破裂和死亡。这项工作为设计具有广谱抗菌活性的纳米肽提供了见解，并为生物医学的发展提供了新的成果。
更新日期：2021-11-25
中文翻译：
具有破膜机制的超分子抗菌纳米纤维的制备
通过研究自组装原理，结合抗菌肽（AMPs）不对称分布所需的结构参数，我们新设计并筛选出高活性、低毒的AMP F2I-LL。该肽可在模拟生理环境（磷酸盐缓冲盐水）中形成具有纳米纤维微结构的超分子水凝胶，具有广谱抗菌活性。与单体肽相比，自组装策略的引入不仅提高了杀菌效价，而且增强了 AMPs 的血清稳定性。机理研究表明，纳米纤维表面富集的正电荷有利于其迅速与细菌外膜带负电的部分结合，进一步进入内膜，增加其通透性并最终导致细胞膜破裂和死亡。这项工作为设计具有广谱抗菌活性的纳米肽提供了见解，并为生物医学的发展提供了新的成果。
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