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Mitochondrion‐Anchoring Photosensitizer with Aggregation‐Induced Emission Characteristics Synergistically Boosts the Radiosensitivity of Cancer Cells to Ionizing Radiation
Author(s) -
Yu Chris Y. Y.,
Xu Huae,
Ji Shenglu,
Kwok Ryan T. K.,
Lam Jacky W. Y.,
Li Xiaolin,
Krishnan Sunil,
Ding Dan,
Tang Ben Zhong
Publication year - 2017
Publication title -
advanced materials
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 10.707
H-Index - 527
eISSN - 1521-4095
pISSN - 0935-9648
DOI - 10.1002/adma.201606167
Subject(s) - photosensitizer , radiosensitizer , mitochondrion , ionizing radiation , cancer cell , materials science , biophysics , fluorescence , radiosensitivity , singlet oxygen , irradiation , photochemistry , chemistry , biology , biochemistry , cancer , radiation therapy , oxygen , medicine , optics , organic chemistry , physics , nuclear physics , genetics
The first mitochondrion‐anchoring photosensitizer that specifically generates singlet oxygen ( 1 O 2 ) in mitochondria under white light irradiation that can serve as a highly effective radiosensitizer is reported here, significantly sensitizing cancer cells to ionizing radiation. An aggregation‐induced emission luminogen (AIEgen), namely DPA‐SCP, is rationally designed with α‐cyanostilbene as a simple building block to reveal AIE, diphenylamino (DPA) group as a strong electron donating group to benefit red emission and efficient light‐controlled 1 O 2 generation, as well as a pyridinium salt as the targeting moiety to ensure specific mitochondrial localization. The AIE signature endows DPA‐SCP with the capacity to visualize mitochondria in a fluorescence turn‐on mode. It is found that under optimized experimental condition, DPA‐SCP with white light does not lead to apoptosis/death of cancer cells, whereas provides an elevated 1 O 2 environment in the mitochondria. More importantly, increasing intracellular level of 1 O 2 originated from mitochondria is demonstrated to be a generic method to enhance the radiosensitivity of cancer cells with a supra‐additive synergistic effect of “0 + 1 > 1.” Noteworthy is that “DPA‐SCP + white light” achieves a high SER10 value of 1.62, which is much larger than that of the most popularly used radiosensitizers, gold nanoparticles (1.19), and paclitaxel (1.32).