Department of Chemistry, School of Chemical Science and Technology, Dr. Harisingh Gour Central University, Sagar, MP, 470003, India.
Department of Chemistry, University of Copenhagen, Universitetsparken 5, 2100, Copenhagen, Denmark.
Chembiochem. 2018 Aug 6;19(15):1630-1637. doi: 10.1002/cbic.201800220. Epub 2018 Jun 21.
We report the design and synthesis of a biocompatible small-peptide-based compound for the controlled and targeted delivery of encapsulated bioactive metal ions through transformation of the internal nanostructures of its complexes. A tyrosine-based short-peptide amphiphile (sPA) was synthesized and observed to self-assemble into β-sheet-like secondary structures. The self-assembly of the designed sPA was modulated by application of different bioactive transition-metal ions, as was confirmed by spectroscopic and microscopic techniques. These bioactive metal-ion-conjugated sPA hybrid structures were further used to develop antibacterial materials. As a result of the excellent antibacterial activity of zinc ions the growth of clinically relevant bacteria such as Escherichia coli was inhibited in the presence of zinc⋅sPA conjugate. Bacterial testing demonstrated that, due to high biocompatibility with bacterial cells, the designed sPA acted as a metal ion delivery agent and might therefore show great potential in locally addressing bacterial infections.
我们报告了一种基于生物相容性小肽的化合物的设计和合成,该化合物可通过其配合物的内部纳米结构的转变来控制和靶向递封装的生物活性金属离子。合成了一种基于酪氨酸的短肽两亲物(sPA),并观察到其自组装成β-折叠状二级结构。通过应用不同的生物活性过渡金属离子来调节设计的 sPA 的自组装,这通过光谱和显微镜技术得到了证实。这些生物活性金属离子共轭的 sPA 杂化结构进一步用于开发抗菌材料。由于锌离子的出色抗菌活性,在锌-sPA 缀合物存在的情况下,抑制了诸如大肠杆菌等临床相关细菌的生长。细菌测试表明,由于与细菌细胞具有很高的生物相容性,因此设计的 sPA 可作为金属离子输送剂,因此在局部解决细菌感染方面可能具有很大的潜力。