揭示基链在提高抗菌选择性和细胞生物相容性方面的作用
Ziwei Deng1, Rongyuan Zhang1,2, Junyi Gong1
1School of Science and Engineering, Clinical Translational Research Center of Aggregation-Induced Emission, School of Medicine, The Second Affiliated Hospital, Shenzhen Institute of Aggregate Science and Technology, The Chinese University of Hong Kong (CUHK-Shenzhen), Shenzhen, Guangdong 518172, China.
JACS Au
|February 28, 2025
概括
研究人员开发了具有可调节的抗菌活性的新型阴两聚合诱导排放光原体 (AIEgens). TPD-6 AIEgen 显示出强大的格拉姆阳性细菌抑制和伤口愈合,哺乳动物细胞毒性最小.
科学领域:
- 超分子化学 超分子化学
- 材料科学 材料科学 材料科学
- 抗菌研究 抗菌研究
背景情况:
- 阴离子两类表现出有前途的向抗菌剂,其活性与基链长度有关.
- 对这些药物缺乏对结构性质关系和生物安全问题的全面了解.
- 聚合诱导排放发光剂 (AIEgens) 为潜在的生物医学应用提供了独特的光学特性.
研究的目的:
- 合成和描述具有不同链长度的新型阴阳性两性AIEgens.
- 为了研究这些AIEgens对格拉姆阳性细菌的结构-活性关系.
- 评估这些AIEgens的生物安全性和体内疗效.
主要方法:
- 合成具有不同链长度的阴阳性两性AIE基因 (TPD-4,TPD-6,TPD-12).
- 抗菌活性测定对抗格拉姆阳性细菌.
- 哺乳动物细胞细胞毒性评估.
- 分子动力学模拟.分子动力学模拟.
- 在体内伤口愈合模型.
主要成果:
- 抗菌活性因酸链长度而异,TPD-6对阳性细菌的疗效最高.
- 开发的AIEgens对哺乳动物细胞具有微不足道的毒性.
- 分子动力学模拟表明,细菌膜结合和变形是作用的关键机制.
- 在体内,TPD-6显示出显著的抗菌和伤口愈合作用.
结论:
- 酸性两性AIEgens可以设计为具有选择性和强大的抗菌活性.
- TPD-6是治疗格拉姆阳性细菌感染和促进伤口愈合的有希望的候选人.
- 艾伊基因具有有利的生物安全概况,可用于潜在的临床转化.
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