The application of nanotechnology for antimicrobial delivery has capacity to improve antibacterial efficacy. Currently, the usage of various inorganic and organic carriers, such as metal ions, nano-silicon and surfactants, might increase the potential toxicity of nanoparticles and make their clinical transformation more difficult. Herein, a nano-delivery system was constructed by direct self-assembly of antibacterial phytochemicals (berberine and rhein) originated from traditional Chinese medicine Coptis chinensis Franch. and Rheum palmatum L., respectively. Combining X-ray single crystal diffraction, nuclear magnetic resonance and other spectra characterizations, the stacked structure of nanoparticles was profoundly demonstrated. Briefly, rhein acted as the layered backbone and berberine embedded in it. In vitro bacteriostasis experiment showed the minimum bactericidal concentration of nanoparticles was 0.1 μmol/mL, which was lower than that of berberine and rhein. The results of confocal laser scanning microscope, biofilm quantitive assay and scanning electron microscopy indicated that nanoparticles had strong inhibitory effects on Staphylococcus aureus biofilm. More importantly, transmission electron microscopy and mass spectra indicated the further bacteriostatic mechanism of nanoparticles. Meanwhile, the nanoparticles had well biocompatibility and safety. Current study will open up new prospect that the design of self-assemblies between active phytochemicals can be originated from traditional Chinese medicine combination.

纳米技术在抗菌药物输送中的应用具有提高抗菌功效的能力。目前，各种无机和有机载体的使用，如金属离子、纳米硅和表面活性剂，可能会增加纳米粒子的潜在毒性，使其临床转化更加困难。在此，通过直接自组装源自中药黄连的抗菌植物化学物质（小檗碱和大黄酸）构建了纳米递送系统。和大黄L.，分别。结合X射线单晶衍射、核磁共振等光谱表征，深入论证了纳米颗粒的堆叠结构。简而言之，大黄酸充当分层骨架，小檗碱嵌入其中。体外抑菌实验表明，纳米粒的最低杀菌浓度为0.1 μmol/mL，低于小檗碱和大黄酸。共聚焦激光扫描显微镜、生物膜定量测定和扫描电镜结果表明，纳米粒子对金黄色葡萄球菌有较强的抑制作用。生物膜。更重要的是，透射电子显微镜和质谱表明纳米粒子的进一步抑菌机制。同时，纳米粒子具有良好的生物相容性和安全性。目前的研究将开辟新的前景，即活性植物化学物质之间的自组装设计可以起源于中药组合。