Guo Kunzhong, Zhang Minjie, Cai Junyi, Ma Zunwei, Fang Zhou, Zhou Haiyan, Chen Junjian, Gao Meng, Wang Lin
National Engineering Research Center for Tissue Restoration and Reconstruction, South China University of Technology, Guangzhou, 510006, China.
School of Materials Science and Engineering, South China University of Technology, Guangzhou, 510641, China.
Small. 2022 Apr;18(17):e2108030. doi: 10.1002/smll.202108030. Epub 2022 Mar 20.
Photosensitizers with aggregation-induced emission properties (AIEgens) can produce reactive oxygen species (ROS) under irradiation, showing great potential in the antibacterial field. However, due to the limited molecular skeletons, the development of AIEgens with precisely adjustable antibacterial activity is still a daunting challenge. Herein, a series of AIE nanofibers (AIE-NFs) based on the AIEgen of DTPM as the inner core and rationally designed peptides as bacterial recognition ligands (e.g., antimicrobial peptide (AMP) HHC36, ditryptophan, polyarginine, and polylysine) is developed. These AIE-NFs show precisely adjustable antibacterial behaviors simply by changing the decorated peptides, which can regulate the aggregation and inhibition of different bacteria. By mechanistic analysis, it is demonstrated that this effect can be attributed to the synergistic antibacterial activities of the ROS and the peptides. It is noteworthy that the optimized AIE-NFs, NFs-K18, can efficiently aggregate bacteria to cluster and kill four types of clinical bacteria under irradiation in vitro, inhibit the infection of methicillin-resistant Staphylococcus aureus (MRSA) and promote wound healing in vivo. To the authors' knowledge, this is the first report of AIE-NFs with precisely adjustable antibacterial activity, providing new opportunities for photodynamic therapy (PDT) treatment of infection.
具有聚集诱导发光特性的光敏剂（AIEgens）在光照下可产生活性氧（ROS），在抗菌领域显示出巨大潜力。然而，由于分子骨架有限，开发具有精确可调抗菌活性的AIEgens仍然是一项艰巨的挑战。在此，开发了一系列基于DTPM的AIEgen作为内核，并将合理设计的肽作为细菌识别配体（如抗菌肽（AMP）HHC36、双色氨酸、聚精氨酸和聚赖氨酸）的AIE纳米纤维（AIE-NFs）。这些AIE-NFs只需改变修饰的肽就能显示出精确可调的抗菌行为，从而可以调节对不同细菌的聚集和抑制作用。通过机理分析表明，这种效应可归因于ROS和肽的协同抗菌活性。值得注意的是，优化后的AIE-NFs，即NFs-K1十八，在体外光照下可有效聚集细菌使其成簇并杀死四种临床细菌，在体内可抑制耐甲氧西林金黄色葡萄球菌（MRSA）的感染并促进伤口愈合。据作者所知，这是首次报道具有精确可调抗菌活性的AIE-NFs，为光动力疗法（PDT）治疗感染提供了新的机会。
