Hypoxia and nonspecific killing always hinder the photodynamic therapy of malignant tumors and infectious diseases that both severely threatening human health. Herein, we report a type I photosensitizer (MTOTPy) with aggregation-induced near-infrared (NIR) emission feature and specific identification ability by rational molecular design. Enhanced electron-donating effect and electron-rich anion-π⁺ structure endow MTOTPy with strong NIR fluorescence and intensive type I reactive oxygen species generation in aggregation. It is demonstrated that MTOTPy can achieve fast identification of tumor cells by targeting mitochondria and specific recognition of Staphylococcus aureus (S. aureus) among other kinds of microbes. Moreover, MTOTPy can kill more than 90% tumor cells and S. aureus upon visible light irradiation at low concentration of 5.0 μM and 0.5 μM, respectively. The work provides a feasible idea for designing photosensitizers to overcome the hypoxic limitation of photodynamic therapy and advance the development of image-guided therapy with high efficiency.

缺氧和非特异性杀伤始终阻碍着严重威胁人类健康的恶性肿瘤和传染病的光动力治疗。在此，我们通过合理的分子设计报道了一种具有聚集诱导近红外（NIR）发射特征和特异性识别能力的I型光敏剂（MTOTPy）。增强的给电子效应和富电子阴离子π ⁺结构赋予MTOTPy强烈的近红外荧光和聚集时强烈的I型活性氧生成。证明MTOTPy可以通过靶向线粒体和特异性识别金黄色葡萄球菌（S. aureus ）实现对肿瘤细胞的快速识别）以及其他种类的微生物。此外，MTOTPy在可见光照射下分别在5.0 μM和0.5 μM的低浓度下可杀死90%以上的肿瘤细胞和金黄色葡萄球菌。该工作为设计光敏剂克服光动力治疗的缺氧局限性、推进图像引导治疗的高效发展提供了可行的思路。