光动力疗法（PDT）作为一种新型的非侵入性抗癌方法引起了广泛关注。然而，传统光敏剂聚集导致的光敏性降低和氧气暴露有限，极大地损害了其整体治疗效果。在此，合成了一系列以三苯胺为骨架的水溶性聚集诱导发射发光体（AIEgens），并表现出明亮的近红外（NIR）发射和强活性氧（ROS）生成。通过 AIEgens 上的多电荷三苯胺单元和葫芦[10]脲 (CB[10]) 主体分子之间的主客体络合，构建了超分子纳米组装体，并且由于其有限的氧接触，对正常细胞表现出可忽略不计的光毒性。相比之下，通过癌细胞中过表达的肽与CB[10]竞争性结合，从纳米组件中有效释放AIEgens，使得能够充分利用AIEgens的光敏性来产生高效的ROS，从而实现对癌细胞的选择性消融。此外，由于通过静电相互作用锚定在细胞器膜上的分子内运动（RIM）的限制，在生理环境中荧光较弱的阳离子AIEgens表现出强烈的荧光发射，从而实现成像引导的PDT。这项工作可能为使用超分子主客体络合策略开发简单可行的智能响应纳米材料用于癌症治疗开辟了一条途径。版权所有 © 2024 Elsevier B.V. 保留所有权利。

Photodynamic therapy (PDT) has attracted widespread attention as a novel non-invasive anticancer approach. However, the diminished photosensitivity and limited oxygen exposure caused by the aggregation of traditional photosensitizers greatly impair its overall therapeutic efficacy. Herein, a series of water-soluble aggregation-induced emission luminogens (AIEgens) with triphenylamine as skeleton were synthesized and exhibited bright Near-infrared (NIR) emission and strong reactive oxygen species (ROS) generation. Through host-guest complexation between the multicharged triphenylamine units on AIEgens and cucurbit[10]uril (CB[10]) host molecule, supramolecular nanoassemblies were constructed and exhibited negligible phototoxicity to normal cells due to their limited oxygen contact. In contrast, the efficient release of AIEgens from nanoassemblies through competitive binding of overexpressed peptides in cancer cells with CB[10], enabled the full exploitation of the photosensitivity of AIEgens to produce highly efficient ROS, achieving selective ablation of cancer cells. Moreover, due to the restriction of intramolecular motion (RIM) upon anchored on organelle membranes through electrostatic interactions, the cationic AIEgens with weak fluorescence in physiological environment exhibited intense fluorescence emission, thus realizing imaging-guided PDT. This work may open up an avenue for the development of simple and feasible smart responsive nanomaterials for cancer treatment using supramolecular host-guest complexation strategy.Copyright © 2024 Elsevier B.V. All rights reserved.