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<p>Fluorescence image-guided photodynamic therapy (PDT) enables real-time monitoring of photosensitizer biodistribution and metabolism for optimized treatment timing. However, its application remains limited, in part, by the reliance on high-end imaging systems. To address this, we designed three novel small-molecule photosensitizers (TTNb, TTAn and TTPh) based on a 2-vinylbenzoic acid scaffold, functionalized at the 5-position with nitro, amino, or hydrogen groups, respectively. Strikingly, replacing the nitro group with amino or hydrogen switched their aggregation behavior from aggregation-induced emission (AIE) to aggregation-caused quenching (ACQ), accompanied by a red-to-green fluorescence shift and subcellular relocation from liposomes to lysosomes. These findings not only establish key design principles for developing ratiometric nitroreductase probes—a currently underexplored class of sensors—but also enable systematic comparison between AIE and ACQ photosensitizers. Among these compounds, TTAn exhibited superior cellular uptake (2800 times higher than the clinical photosensitizer Ce6 in Eca-109 cells), specific lysosomal targeting, balanced reactive oxygen species (singlet oxygen/superoxide anion) generation, and intense fluorescence. Under white light irradiation, TTAn achieved an exceptional IC<sub>50</sub> of 21 nM, surpassing Ce6 by 50-fold. Notably, TTAn produced strong fluorescence in mice tumors under both one- and two-photon excitation, detectable using conventional imaging tools (e.g., smartphones, DSLR cameras) or even visible to the naked eyes, confirming its outstanding tumor specificity. Leveraging these advantages, TTAn enabled successful image-guided two-photon PDT in Eca-109 tumor-bearing mice with just a single treatment, demonstrating potent therapeutic efficacy and biosafety. This work provides a strategic blueprint for developing small-molecule theranostic agents that operate without complex fluorescence imaging systems.</p>

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A highly fluorescent tumor-targeting photosensitizer for DSLR camera image-guided two-photon photodynamic therapy

  • 期刊论文

  • 发表日期：

    2026年7月3日

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  • Qiuyu Yang,
  • Xiaohong Pan,
  • Yaqi Wang,
  • Hongyu Wang,
  • Liangzhi Cai,
  • Xiaoying Shang,
  • Wenzhen Liu,
  • Jincan Chen,
  • Zhuo Chen

摘要

Fluorescence image-guided photodynamic therapy (PDT) enables real-time monitoring of photosensitizer biodistribution and metabolism for optimized treatment timing. However, its application remains limited, in part, by the reliance on high-end imaging systems. To address this, we designed three novel small-molecule photosensitizers (TTNb, TTAn and TTPh) based on a 2-vinylbenzoic acid scaffold, functionalized at the 5-position with nitro, amino, or hydrogen groups, respectively. Strikingly, replacing the nitro group with amino or hydrogen switched their aggregation behavior from aggregation-induced emission (AIE) to aggregation-caused quenching (ACQ), accompanied by a red-to-green fluorescence shift and subcellular relocation from liposomes to lysosomes. These findings not only establish key design principles for developing ratiometric nitroreductase probes—a currently underexplored class of sensors—but also enable systematic comparison between AIE and ACQ photosensitizers. Among these compounds, TTAn exhibited superior cellular uptake (2800 times higher than the clinical photosensitizer Ce6 in Eca-109 cells), specific lysosomal targeting, balanced reactive oxygen species (singlet oxygen/superoxide anion) generation, and intense fluorescence. Under white light irradiation, TTAn achieved an exceptional IC50 of 21 nM, surpassing Ce6 by 50-fold. Notably, TTAn produced strong fluorescence in mice tumors under both one- and two-photon excitation, detectable using conventional imaging tools (e.g., smartphones, DSLR cameras) or even visible to the naked eyes, confirming its outstanding tumor specificity. Leveraging these advantages, TTAn enabled successful image-guided two-photon PDT in Eca-109 tumor-bearing mice with just a single treatment, demonstrating potent therapeutic efficacy and biosafety. This work provides a strategic blueprint for developing small-molecule theranostic agents that operate without complex fluorescence imaging systems.