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Molecular Structural Evolution of Near-Infrared Cationic Aggregation-Induced Emission Luminogens: Preclinical Antimicrobial Pathogens Activities and Tissues Regeneration
CCS Chemistry ( IF 9.4 ) Pub Date : 2021-08-23 , DOI: 10.31635/ccschem.021.202101206
Haidong Li 1 , Liuwei Zhang 2, 3 , Jingjing Han 1 , Dayeh Kim 1 , Heejeong Kim 1 , Jeongsun Ha 1 , Jingyun Wang 2, 3 , Juyoung Yoon 1
Affiliation  

Increasingly infectious diseases from microbial pathogens (including bacteria and fungi) threaten human health: a situation that has aroused public health concern around the world. Unfortunately, broad-spectrum antimicrobial agents for treatment resistance pathogens and molecular research on their antimicrobial mechanisms are still scarce. Thus, the development of smart agents against microbial infection for surmounting the above dilemmas is an urgent task. In this contribution, we have tactfully designed a family of flexible aggregation-induced emission luminogens (AIEgens) with various alkyl chain lengths and successfully optimized a cationic AIEgen TPA-S-C6-NMe3 + based on the molecular relay strategy for killing both bacteria and fungi in vitro with desired results under white light irradiation, superior to traditional commercial photosensitizers including methylene blue, chlorin e6, and protoporphyrin IX. The cationic AIEgen TPA-S-C6-NMe3 + was bound to microbial pathogens via electrostatic and hydrophobic forces and exerted antimicrobial efficacy due to the synergistic effect of alkyl chain length, reactive oxygen species (ROS) generation capability, and two positive charges. Remarkably, AIEgen TPA-S-C6-NMe3 + also exhibited a striking antimicrobial activity in vivo, and promoted the generation of new blood vessels and fibroblasts in bacteria-infected tissues, which was beneficial for wound healing in mice. Overall, we expect that our work could provide a powerful tool against microbial pathogens to avoid infections and to promote tissues regeneration in clinical practice.



中文翻译:

近红外阳离子聚集诱导发光发光原的分子结构进化:临床前抗菌病原体活性和组织再生

来自微生物病原体(包括细菌和真菌)的传染病越来越多地威胁着人类健康:这种情况已经引起了全世界的公共卫生关注。不幸的是,用于治疗耐药病原体的广谱抗菌剂及其抗菌机制的分子研究仍然很少。因此,开发针对微生物感染的智能药剂以克服上述困境是一项紧迫的任务。在这一贡献中,我们巧妙地设计了一系列具有各种烷基链长度的灵活聚集诱导发光发光体 (AIEgens),并成功优化了阳离子 AIEgen TPA-S-C6-NMe 3 +基于分子中继策略,在体外杀死细菌和真菌,在白光照射下达到预期效果,优于传统的商业光敏剂,包括亚甲蓝、二氢卟酚 e6 和原卟啉 IX。阳离子 AIEgen TPA-S-C6-NMe 3 +由于烷基链长度、活性氧 (ROS) 生成能力和两个正电荷的协同作用,通过静电和疏水力与微生物病原体结合并发挥抗菌功效。值得注意的是,AIEgen TPA-S-C6-NMe 3 +在体内也表现出惊人的抗菌活性,并促进细菌感染组织中新血管和成纤维细胞的生成,这有利于小鼠的伤口愈合。总的来说,我们希望我们的工作可以提供一种强大的工具来对抗微生物病原体,以避免感染并促进临床实践中的组织再生。

更新日期:2021-08-23
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