Photocaged fluorophores with photoactivatable characteristics presented important applications in imaging the biological structures and processes. Taking advantage of their super-resolution imaging merits to manipulate and visualize anti-cancer treatment is always a goal of modern clinical medicine. Traditional photodynamic therapy (PDT) is a noninvasive treatment but limited in intracellular oxygen content. Type I PDT and photoacid therapy (PAT) are two effective supplements of traditional PDT especially in hypoxic condition. Herein, a novel white-light-driven fluorescence switch (7H-dibenzo[c,g]carbazol-7-yl)(2-iodophenyl)methanone (2IB) was designed and synthesized as an unprecedent “all in one” platform for stochastic optical reconstruction microscopy (STORM) imaging guided Type I/II PDT and PAT. The experimental and theoretical studies revealed that the working mechanism is based on two competing paths under excitation: photosensitization and photocyclization reaction. Efficient intersystem crossing (ISC) ensured the generation of reactive oxygen species (ROS) for PDT, while low energy barrier facilitated the photocyclization reaction that simultaneously yielded emissive fluorophores (2IBC) and H⁺ for super-resolution imaging and photoacid, respectively. Impressively, the fluorescent intensity of mitochondria-targeted 2IBC was positively correlated with treatment efficacy, which is beneficial to spatiotemporally visualized therapeutic process and outcome. As a result, superior anti-tumor performance was achieved in vitro and in vivo. This contribution provided a multifunctional nanodrug paradigm for multimode cancer diagnosis and treatment.

具有光活化特性的光笼荧光团在成像生物结构和过程中具有重要应用。利用它们的超分辨率成像优势来操纵和可视化抗癌治疗一直是现代临床医学的目标。传统的光动力疗法 (PDT) 是一种非侵入性治疗，但细胞内氧含量有限。I 型 PDT 和光酸疗法 (PAT) 是传统 PDT 的两种有效补充，尤其是在缺氧条件下。在此，一种新型的白光驱动荧光开关 (7 H -dibenzo [c,g]carbazol-7-yl)(2-iodophenyl) methanone ( 2IB) 被设计和合成为一个前所未有的“一体化”平台，用于随机光学重建显微镜 (STORM) 成像引导的 I/II 型 PDT 和 PAT。实验和理论研究表明，其工作机制基于激发下的两条竞争路径：光敏化和光环化反应。高效的系统间穿越 (ISC) 确保了 PDT 的活性氧 (ROS) 的产生，而低能垒促进了光环化反应，同时分别产生发射荧光团 ( 2IBC ) 和 H ⁺用于超分辨率成像和光酸。令人印象深刻的是，线粒体靶向2IBC的荧光强度与治疗效果呈正相关，有利于时空可视化治疗过程和结果。结果，在体外和体内均获得了优异的抗肿瘤性能。这一贡献为多模式癌症诊断和治疗提供了多功能纳米药物范例。