Li Meng, Li Shengliang, Chen Hui, Hu Rong, Liu Libing, Lv Fengting, Wang Shu
Beijing National Laboratory for Molecular Science, Key Laboratory of Organic Solids, Institute of Chemistry, Chinese Academy of Sciences , Beijing 100190, P. R. China.
ACS Appl Mater Interfaces. 2016 Jan 13;8(1):42-6. doi: 10.1021/acsami.5b11846. Epub 2016 Jan 4.
In this work, a new conjugated polymer poly(fluorene-co-phenylene) derivative containing pendent quaternized chlormethine (PFP-Chl) was synthesized by covalent linking small molecular prodrug groups onto conjugated polymer side chains. H2O2-sensitive prodrug with an eight-member-cyclic boronate ester structure could suffer from H2O2-triggered nitrogen mustard release and further DNA cross-linking and alkylation. PFP-Chl combines therapeutic characteristic with excellent optical property of conjugated polymers. It is found that PFP-Chl could enter into cells by endocytosis to simultaneously exhibit abilities of fluorescent imaging and tumor cell inhibition.
在本研究中，通过将小分子前药基团共价连接到共轭聚合物侧链上，合成了一种含有侧链季铵化氯甲基的新型共轭聚合物聚（芴-共-亚苯基）衍生物（PFP-Chl）。具有八元环硼酸酯结构的对过氧化氢敏感的前药可在过氧化氢触发下释放氮芥，并进一步导致DNA交联和烷基化。PFP-Chl将治疗特性与共轭聚合物优异的光学性质相结合。研究发现，PFP-Chl可通过内吞作用进入细胞，同时展现出荧光成像和抑制肿瘤细胞的能力。
