Beijing Area Major Laboratory of Peptide and Small Molecular Drugs, Engineering Research Center of Ministry of Education of China, Beijing Laboratory of Biomedical Materials, School of Pharmaceutical Science, Capital Medical University, Beijing, 100069, China.
Discipline of Oral and Maxillofacial Surgery, Faculty of Dentistry, The University of Hong Kong, Hong Kong SAR, 999077, China.
Adv Healthc Mater. 2023 Nov;12(29):e2301688. doi: 10.1002/adhm.202301688. Epub 2023 Aug 13.
Antimicrobial peptides (AMPs) are a developing class of natural and synthetic oligopeptides with host defense mechanisms against a broad spectrum of microorganisms. With in-depth research on the structural conformations of AMPs, synthesis or modification of peptides has shown great potential in effectively obtaining new therapeutic agents with improved physicochemical and biological properties. Notably, AMPs with self-assembled properties have gradually become a hot research topic for various biomedical applications. Compared to monomeric peptides, these peptides can exist in diverse forms (e.g., nanoparticles, nanorods, and nanofibers) and possess several advantages, such as high stability, good biocompatibility, and potent biological functions, after forming aggregates under specific conditions. In particular, the stability and antibacterial property of these AMPs can be modulated by rationally regulating the peptide sequences to promote self-assembly, leading to the reconstruction of molecular structure and spatial orientation while introducing some peptide fragments into the scaffolds. In this work, four self-assembled AMPs are developed, and the relationship between their chemical structures and antibacterial activity is explored extensively through different experiments. Importantly, the evaluation of antibacterial performance in both in vitro and in vivo studies has provided a general guide for using self-assembled AMPs in subsequent treatments for combating bacterial infections.
抗菌肽（AMPs）是一类新兴的天然和合成寡肽，具有针对广谱微生物的宿主防御机制。随着对 AMPs 结构构象的深入研究，肽的合成或修饰显示出在有效获得具有改善的物理化学和生物学特性的新型治疗剂方面的巨大潜力。值得注意的是，具有自组装特性的 AMPs 逐渐成为各种生物医学应用的热门研究课题。与单体肽相比，这些肽在特定条件下形成聚集体后，可以以多种形式（例如纳米颗粒、纳米棒和纳米纤维）存在，并具有高稳定性、良好的生物相容性和强大的生物学功能等优势。特别是，通过合理调节肽序列来促进自组装，可以调节这些 AMPs 的稳定性和抗菌性能，从而在引入一些肽片段到支架中时，重建分子结构和空间取向。在这项工作中，开发了四种自组装 AMP，并通过不同的实验广泛探索了它们的化学结构与抗菌活性之间的关系。重要的是，在体外和体内研究中对抗菌性能的评估为随后使用自组装 AMP 治疗细菌感染提供了一般性指导。
