Beijing National Laboratory of Molecular Science, Institute of Chemistry, Chinese Academy of Sciences , Beijing 100910, P. R. China.
University of Chinese Academy of Sciences , Beijing 100049, P. R. China.
ACS Appl Mater Interfaces. 2017 Aug 23;9(33):27427-27432. doi: 10.1021/acsami.7b10105. Epub 2017 Aug 14.
Polymers are mostly trapped in lysosomes when they enter cells and are then expelled, otherwise they were designed to be degradable to small molecules or to sabotage lysosomes. Therefore, they have reached the limit of the unique functionalities as a whole. Different from other escaping strategies, we introduced the polarity exchanging approach to rigid-backboned conjugated polymer for controlled penetrating through endosome or lysosome membranes. With the aid of pH-sensitive cleavage of water-soluble side chain, the rigid conjugated polymer turns highly hydrophobic after it is internalized into lysosomes and then accomplishes escaping. Thus, polarity exchange of CPs could become a new strategy for their application on chemotherapeutics.
聚合物进入细胞时大多被困在溶酶体中,然后被排出,否则它们被设计成可降解为小分子或破坏溶酶体。因此,它们已经达到了整体独特功能的极限。与其他逃避策略不同,我们引入了极性交换方法来刚性主链共轭聚合物,以控制穿透内体或溶酶体膜。在水溶性侧链的 pH 敏感裂解的帮助下,刚性共轭聚合物在被内化到溶酶体后变得高度疏水,然后完成逃逸。因此,CP 的极性交换可以成为其在化学疗法中的应用的新策略。