Tao Guoqing, Ji Tan, Wang Ning, Yang Guang, Lei Xiaolai, Zheng Wei, Liu Rongying, Xu Xuyang, Yang Ling, Yin Guang-Qiang, Liao Xiaojuan, Li Xiaopeng, Ding Hong-Ming, Ding Xiaoming, Xu Jinfu, Yang Hai-Bo, Chen Guosong
The State Key Laboratory of Molecular Engineering of Polymers and Department of Macromolecular Science, Fudan University, Shanghai 200433, China.
Shanghai Key Laboratory of Green Chemistry and Chemical Processes and School of Chemistry and Molecular Engineering, East China Normal University, Shanghai 200062, China.
ACS Macro Lett. 2020 Jan 21;9(1):61-69. doi: 10.1021/acsmacrolett.9b00914. Epub 2019 Dec 27.
Bacterial biofilms are troublesome in the treatment of bacterial infectious diseases due to their inherent resistance to antibiotic therapy. Exploration of alternative antibiofilm reagents provides opportunities to achieve highly effective treatments. Herein, we propose a strategy to employ self-assembled saccharide-functionalized amphiphilic metallacycles (, , and ) with multiple positive charges as a different type of antibacterial reagent, marrying saccharide functionalization that interact with bacteria via "sweet talking". These self-assembled glyco-metallacycles gave various nanostructures (nanoparticles, vesicles or micron-sized vesicles) with different biofilms inhibition effect on (). Especially, the peculiar self-assembly mechanism, superior antibacterial effect and biofilms inhibition distinguished the from other metallacycles. Meanwhile, in vivo pneumonia animal model experiments suggested that could relieve mice pneumonia aroused by effectively. In addition, the control study of metallacycle confirmed the significant role of galactoside both in the self-assembly process and the antibacterial efficacy. In view of the superior effect against bacteria, the saccharide-functionalized metallacycle could be a promising candidate as biofilms inhibitor or treatment agent for pneumonia.
细菌生物膜在细菌感染性疾病的治疗中是个棘手的问题，因为它们对抗生素治疗具有固有的抗性。探索替代的抗生物膜试剂为实现高效治疗提供了机会。在此，我们提出一种策略，即使用具有多个正电荷的自组装糖功能化两亲金属环化物（、和）作为一种不同类型的抗菌试剂，将通过“甜言蜜语”与细菌相互作用的糖功能化结合起来。这些自组装糖金属环化物产生了各种纳米结构（纳米颗粒、囊泡或微米级囊泡），对（）具有不同的生物膜抑制作用。特别是，独特的自组装机制、优异的抗菌效果和生物膜抑制作用使与其他金属环化物区分开来。同时，体内肺炎动物模型实验表明，能够有效缓解由引起的小鼠肺炎。此外，金属环化物的对照研究证实了半乳糖苷在自组装过程和抗菌效果中的重要作用。鉴于其对细菌的优异效果，糖功能化金属环化物有望成为生物膜抑制剂或肺炎治疗剂的候选物。
