Abstract：
Currently, specific cancer-responsive fluorogenic probes with activatable imaging and therapeutic functionalities are in great demand in the accurate diagnostics and efficient therapy of malignancies. Herein, an all-in-one strategy is presented to realize fluorescence (FL) imaging-guided and synergetic chemodynamic-photodynamic cancer therapy by using a multifunctional alkaline phosphatase (ALP)-response aggregation-induced emission (AIE) probe, TPE-APP. By responding to the abnormal expression levels of an ALP biomarker in cancer cells, the phosphate groups on the AIE probe are selectively hydrolyzed, accompanied by in situ formation of strong emissive AIE aggregates for discriminative cancer cell imaging over normal cells and highly active quinone methide species with robust chemodynamic-photodynamic activities. Consequently, the activated AIE probes can efficiently destroy cancer cell membranes and lead to the death of cancer cells within 30 min. A superior efficacy in cancer cell ablation is demonstrated in vitro and in vivo. The cancer-associated biomarker response-derived discriminative FL imaging and synergistic chemodynamic-photodynamic therapy are expected to provide a promising avenue for precise image-guided cancer therapy.
摘要：
目前,具有可激活的成像和治疗功能的特异性癌症反应性荧光探针在恶性肿瘤的准确诊断和有效治疗中非常需要。在这里，提出了一种多合一策略，通过使用多功能碱性磷酸酶（ALP）-反应聚集诱导发射（AIE）探针来实现荧光（FL）成像引导和协同化学动力学-光动力学癌症治疗，TPE-APP。通过响应癌细胞中ALP生物标志物的异常表达水平，AIE探针上的磷酸基团被选择性地水解，伴随着原位形成强发射性AIE聚集体，用于对正常细胞和具有强大化学动力学-光动力学活性的高活性醌甲基化物进行区分性癌细胞成像。因此,激活的AIE探针可以有效破坏癌细胞膜，并在30分钟内导致癌细胞死亡。在体外和体内证明了癌细胞消融的优异功效。癌症相关的生物标志物反应来源的判别FL成像和协同化学动力学-光动力学疗法有望为精确的图像引导癌症治疗提供有希望的途径。
