Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 27, Issue 11, Pages 2201-2208Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2019.04.023
Keywords
Phenylphenalenone; 2-Pyridone; Endoperoxide; Photosensitizer; Cytotoxicity
Funding
- National Key Research and Development Program of China [2018YFD0200100]
- National Natural Science Foundation of China [21877039]
- Science and Technology Commission of Shanghai Municipality [16391902300]
- Shanghai Municipal Education Commission [2017-01-07-00-02-E00037]
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Photosensitizer attracts great attentions and has potential applications in cancer treatment. We developed here a novel pyridone-containing phenalenone-based (PPN-PYR) photosensitizer with excellent singlet oxygen generating ability. Upon light irradiation, PPN-PYR can produce singlet oxygen and transform to its endoperoxide form which in turn release singlet oxygen via thermal cycloreversion at dark. The ability of PPN-PYR to generate reactive oxygen species (ROS) in cell culture and induce corresponding apoptosis both at dark and under light was demonstrated. The efficient PDT performance of PPN-PYR was further verified on cancer cell in vitro. Our study indicate that PPN-PYR can alleviate tumor hypoxia problem and enhance the availability of intermittent photodynamic therapy.
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