| Autor: |
Ge F; Beijing Key Laboratory for Optical Materials and Photonic Devices, Department of Chemistry, Capital Normal University, Beijing 100048, P. R. China. wangzhj@cnu.edu.cn., Sun Y; Laboratory of Biomedical Materials and Key Lab of Biomedical Materials of Natural Macromolecules, Beijing University of Chemical Technology, Beijing 100029, P. R. China. yubr@mail.buct.edu.cn., Wang Y; Laboratory of Biomedical Materials and Key Lab of Biomedical Materials of Natural Macromolecules, Beijing University of Chemical Technology, Beijing 100029, P. R. China. yubr@mail.buct.edu.cn., Yu D; Laboratory of Biomedical Materials and Key Lab of Biomedical Materials of Natural Macromolecules, Beijing University of Chemical Technology, Beijing 100029, P. R. China. yubr@mail.buct.edu.cn., Wang Z; Beijing Key Laboratory for Optical Materials and Photonic Devices, Department of Chemistry, Capital Normal University, Beijing 100048, P. R. China. wangzhj@cnu.edu.cn.; Laboratory of Biomedical Materials and Key Lab of Biomedical Materials of Natural Macromolecules, Beijing University of Chemical Technology, Beijing 100029, P. R. China. yubr@mail.buct.edu.cn., Yu F; Key Laboratory of Emergency and Trauma, Ministry of Education, Key Laboratory of Haikou Trauma, Key Laboratory of Hainan Trauma and Disaster Rescue, Engineering Research Centre for Hainan Bio-Smart Materials and Bio-Medical Devices, Key Laboratory of Hainan Functional Materials and Molecular Imaging, The First Affiliated Hospital of Hainan Medical University, Hainan Medical University, Haikou 571199, China. yufabiao@muhn.edu.cn., Yu B; Laboratory of Biomedical Materials and Key Lab of Biomedical Materials of Natural Macromolecules, Beijing University of Chemical Technology, Beijing 100029, P. R. China. yubr@mail.buct.edu.cn., Fu H; Beijing Key Laboratory for Optical Materials and Photonic Devices, Department of Chemistry, Capital Normal University, Beijing 100048, P. R. China. wangzhj@cnu.edu.cn. |
| Abstrakt: |
Tumor microenvironment-activatable photosensitizers have gained significant attention for cancer theranostics. Considering the hypoxic environment of solid tumors, activatable phototheranostic agents with type I PDT are desired to obtain improved cancer treatment efficiency. Herein, we report a simple, effective and multifunctional Bodipy photosensitizer for tumor imaging and type I/II photodynamic therapy. The photosensitizer featuring a methylphenylboronic acid pinacol ester group at the meso -position of Bodipy specifically responds to tumor-abundant H 2 O 2 . Its photophysical properties were characterized using steady-state and time-resolved transient optical spectroscopies. The fluorescence ( Φ F = 0.09%) and singlet oxygen efficacy ( Φ Δ = 10.2%) of the Bodipy units were suppressed in the caged dyads but significantly enhanced ( Φ F = 0.72%, Φ Δ = 20.3%) upon H 2 O 2 activation. Fluorescence emission spectroscopy and continuous wave electron paramagnetic resonance (EPR) spectroscopy confirmed that the Bodipy photosensitizer generates reactive oxygen species (ROS) via both electron transfer-mediated type I and energy transfer-mediated type II mechanisms. In vitro experiments demonstrated rapid internalization into tumor cells, enhanced brightness stimulated by tumor microenvironments, and tumor cell death (phototoxicity, IC 50 = 0.5 μM). In vivo fluorescence imaging indicated preferential accumulation of this Bodipy photosensitizer in tumor sites, followed by decaging by tumor-abundant H 2 O 2 , further elevating the signal-to-background ratio (SBR) of imaging. Besides outstanding performance in tumor imaging, a prominent inhibition of tumor growth was observed. Given its simple molecular skeleton, this Bodipy photosensitizer is a competitive candidate for cancer theranostics. |
