Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling, Shaanxi, 712100, China; College of Medicine, Pingdingshan University, Pingdingshan, Henan, 467000, China.
Shaanxi Key Laboratory of Natural Products & Chemical Biology, College of Chemistry & Pharmacy, Northwest A&F University, Yangling, Shaanxi, 712100, China.
Carbohydr Polym. 2019 Apr 15;210:364-371. doi: 10.1016/j.carbpol.2019.01.068. Epub 2019 Jan 23.
Many pathogenic bacteria can invade phagocytic and non-phagocytic cells and colonize inside, which protects them from the attack by host immune system and antibiotics. A novel amphiphilic molecule was synthesized through conjugation of streptomycin and decylamine to hyaluronan. Rapamycin was encapsulted by the spontaneous self-assembly of hyaluronan-based amphiphilic molecules. The newly formed micelles not only facilitated the entry of drugs into host cells in part via CD44 phagocytic receptor, released streptomycin in the acidic compartment, but also could activate autophagy. The micelles elicited an efficient killing capacity against intracellular bacteria through the promotion of streptomycin uptake and rapamycin-initiated activation of autophagy. This strategy might highlight an acid-sensitive hyaluronan-based drug delivery system for effective treatment of intracellular infections.
许多病原菌可以入侵吞噬细胞和非吞噬细胞并在内部定植,从而使它们免受宿主免疫系统和抗生素的攻击。通过将链霉素和癸胺与透明质酸偶联,合成了一种新型两亲分子。雷帕霉素通过基于透明质酸的两亲分子的自发自组装被包封。新形成的胶束不仅通过 CD44 吞噬受体部分促进药物进入宿主细胞,在酸性隔室中释放链霉素,还可以激活自噬。胶束通过促进链霉素摄取和雷帕霉素引发的自噬激活,对细胞内细菌产生了有效的杀伤能力。该策略可能突出了一种基于透明质酸的酸敏感药物递送系统,用于有效治疗细胞内感染。