Chinese Academy of Sciences (CAS) Key Laboratory for Biological Effects of Nanomaterials and Nanosafety, CAS Center for Excellence in Nanoscience, National Center for Nanoscience and Technology , Chinese Academy of Sciences , Beijing 100190 , P.R. China.
ACS Nano. 2019 Jun 25;13(6):6770-6781. doi: 10.1021/acsnano.9b01346. Epub 2019 May 28.
The abuse of traditional antibiotics has caused a series of health problems including antimicrobial resistance, which threatens human health. Therefore, searching for broad sources of antimicrobial agents and developing multidimensional strategies to combat bacterial infections are urgent. Here, we reported two natural self-assembling modes between berberine (BBR) and flavonoid glycosides: nanoparticles (NPs) and nanofibers (NFs), which were both mainly governed by electrostatic and hydrophobic interactions. These two nanostructures exhibited different antibacterial properties from BBR. NPs showed significantly enhanced bacteriostatic activity, whereas NFs displayed a much weaker effect than BBR. The distinguishing properties can be attributed to the different spatial configurations and self-assembly processes of NPs and NFs. Flavonoid glycosides and BBR first formed a one-dimensional complex unit and subsequently self-assembled into three-dimensional nanostructures. With the hydrophilic glucuronic acid toward the outside, NPs exhibited stronger affinity to bacteria, thereby inducing the collapse of the bacteria population and the decrease in biofilm. In addition, in vitro hemolysis tests, cytotoxicity tests, and in vivo zebrafish toxicity evaluation showed that the obtained self-assemblies had good biocompatibility. This supramolecular self-assembly strategy can be applied to construct other nanoscale antibacterial drugs and thus provides weapons for the development of self-delivering drugs in bacterial infection treatment.
传统抗生素的滥用导致了一系列健康问题，包括抗菌药物耐药性，这威胁着人类健康。因此，迫切需要寻找抗菌药物的广泛来源并制定多维策略来对抗细菌感染。在这里，我们报道了小檗碱（BBR）和类黄酮糖苷之间的两种天然自组装模式：纳米颗粒（NPs）和纳米纤维（NFs），它们主要由静电和疏水相互作用控制。这两种纳米结构表现出与 BBR 不同的抗菌特性。 NPs 表现出明显增强的抑菌活性，而 NFs 的效果比 BBR 弱得多。这种区别特性可归因于 NPs 和 NFs 的不同空间构型和自组装过程。类黄酮糖苷和 BBR 首先形成一维复合单元，然后自组装成三维纳米结构。带亲水的葡萄糖醛酸朝外，NPs 对细菌表现出更强的亲和力，从而导致细菌种群的崩溃和生物膜的减少。此外，体外溶血试验、细胞毒性试验和体内斑马鱼毒性评价表明，所得自组装具有良好的生物相容性。这种超分子自组装策略可应用于构建其他纳米级抗菌药物，从而为细菌感染治疗中自递药的发展提供武器。
