Image-guided combination chemotherapy and photodynamic therapy using a mitochondria-targeted molecular probe with aggregation-induced emission characteristics

Subcellular targeted cancer therapy and monitoring of therapeutic effect are highly desirable for clinical applications. Herein, we report a series of probes by conjugating zero ( ), one ( ) and two ( ) triphenylphosphine (TPP) ligands to a fluorogen with aggregation-induced emission (AIE) character...

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Bibliographic Details
Published in:Chemical science (Cambridge) 2015-08, Vol.6 (8), p.4580-4586
Main Authors: Zhang, Chong-Jing, Hu, Qinglian, Feng, Guangxue, Zhang, Ruoyu, Yuan, Youyong, Lu, Xianmao, Liu, Bin
Format: Article
Language:English
Subjects:
Anticancer properties
Cancer
Chemistry
Chemotherapy
Illumination
Light (illumination)
Mitochondria
Photodynamic therapy
Singlet oxygen
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Summary:Subcellular targeted cancer therapy and monitoring of therapeutic effect are highly desirable for clinical applications. Herein, we report a series of probes by conjugating zero ( ), one ( ) and two ( ) triphenylphosphine (TPP) ligands to a fluorogen with aggregation-induced emission (AIE) characteristics. The probes are almost non-emissive as molecularly dissolved species, but they can light up in cell cytoplasm or mitochondria. is found to be able to target mitochondria, depolarize mitochondria membrane potential and selectively exert potent chemo-cytotoxicity on cancer cells. Furthermore, it can efficiently generate singlet oxygen with strong photo-toxicity upon light illumination, which further enhances its anti-cancer effect. On the other hand, can also target mitochondria and generate singlet oxygen to trigger cancer cell apoptosis, but it shows low cytotoxicity in dark. Meanwhile, can report the cellular oxidative stress by visualizing the morphological changes of mitochondria. However, does not target mitochondria and shows no obvious anticancer effect either in dark or under light illumination. This study thus highlights the importance of molecular probe design, which yields a new generation of subcellular targeted molecular theranostic agents with multi-function, such as cancer cell imaging, chemotherapy, photodynamic therapy, and monitoring of the therapeutic effect in one go.
ISSN:2041-6520
2041-6539
DOI:10.1039/c5sc00826c