LAUSR

The acidic tumor microenvironment is triggered by glycolysis in hypoxic condition, which can motivate the pH-responsive system to build certain triggers for efficiently tumor-targeted phototherapy. Additionally, the metalated porphyrin structures are widely studied in biomedical applications due to the favorable properties of high singlet oxygen quantum yield as well as strong fluorescence imaging ability. Herein, a pH-responsive zinc (II) metalated porphyrin (P-4) was designed and synthesized for amplifying cancer photodynamic/photothermal therapy with excellent fluorescence quantum yield (67.4%), superb singlet oxygen quantum yield (84.3%) and desired photothermal conversion efficiency (30.0%). In vitro, the self-assembled P-4 nanoparticles can specifically target to lysosome subcellular site and realize protonated process of dibutaneaminophenyl (DBAP) groups with high photo toxicity. Under single 660 nm laser illumination, the tumor can be ablated completely with no side effects in vivo. This work demonstrates that the pH-responsive P-4 nanoparticles provide a new avenue for highly efficient cancer combination therapy.摘要肿瘤酸性微环境是低氧条件下糖酵解引发的, 它能激发体系的酸性响应系统, 为肿瘤靶向光治疗建立一定的触发机制. 金属化卟啉结构具有单态氧产率高、 荧光成像能力强等优点, 在生物医学领域得到广泛研究. 本文设计合成了一种具有优异荧光量子产率(67.4%)、 高单态氧量子产率(84.3%)和理想光热转换效率(30.0%)的酸性响应锌(II)金属卟啉(P-4), 研究了其酸性肿瘤微环境刺激响应光动力/光热治疗性能. 自组装的P-4纳米粒子可以特异性地靶向溶酶体亚细胞器位点, 实现二丁胺苯基(DBAP)的质子化过程且伴随高光毒性; 在660 nm单激光照射下, 肿瘤被完全消除且无副作用, 表明酸刺激响应的P-4纳米粒子可以为肿瘤协同治疗提供一种新途径.