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>An AIE photosensitizer with unquenched fluorescence based on nitrobenzoic acid for tumor-targeting and image-guided photodynamic therapy
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An AIE photosensitizer with unquenched fluorescence based on nitrobenzoic acid for tumor-targeting and image-guided photodynamic therapy
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机译：An AIE photosensitizer with unquenched fluorescence based on nitrobenzoic acid for tumor-targeting and image-guided photodynamic therapy
Fluorescence quenching occurs in most nitroaromatic compounds due to photoinduced electron transfer (PET) effects, limiting their use as image-guided photosensitizers for anticancer photodynamic therapy (PDT) or as probes for nitroreductase in hypoxic cells. Herein, we developed a tumor-targeting aggregation-induced emission photosensitizer (AIE-PS), Biotin-TTVBA, by binding TTVBA (a nitrobenzoic acid-based AIE-PS with a free carboxylic acid group) to biotin. Biotin-TTVBA has near-infrared emission characteristics in DMSO containing 99 toluene, a large Stoke's shift (210 nm), high photostability, wash-free cell staining ability and type I/II photosensitivity. Compared with TTVBA, Biotin-TTVBA significantly increased cellular uptake (a 60-fold increase) and selective uptake of tumor cells (a 250 increase in the ratio of tumor cells to normal cells), resulting in enhanced antitumor activity against tumor cells (HeLa and MCF-7) and a decreased IC50 value (from >40 μM to 2.5 μM). Taken together, the results of this study call attention to AIE-PSs based on nitroaromatic groups because of their strong fluorescence and ROS generation ability, which can be used in image-guided photodynamic therapy and provide a new approach for tumor-targeting design of AIE-PSs.
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