A Mitochondria‐Targeted Photosensitizer Showing Improved Photodynamic Therapy Effects Under Hypoxia

• DOI: 10.1002/ange.201604130
• Publication Date: 2016-07-06T08:44:03Z
• Authors: Wen Lv; Zhang Zhang; Kenneth Yin Zhang; Huiran Yang; Shujuan Liu; Aqiang Xu; Song Guo; Qiang Zhao; Wei Huang
• Keywords: Photosensitizing Agents; Molecular Structure; Cell Survival; Iridium; 01 natural sciences; Mitochondria; 0104 chemical sciences; 3. Good health; Photochemotherapy; Coordination Complexes; Humans; Hypoxia; HeLa Cells

AbstractOrganelle‐targeted photosensitizers have been reported to be effective photodynamic therapy (PDT) agents. In this work, we designed and synthesized two iridium(III) complexes that specifically stain the mitochondria and lysosomes of living cells, respectively. Both complexes exhibited long‐lived phosphorescence, which is sensitive to oxygen quenching. The photocytotoxicity of the complexes was evaluated under normoxic and hypoxic conditions. The results showed that HeLa cells treated with the mitochondria‐targeted complex maintained a slower respiration rate, leading to a higher intracellular oxygen level under hypoxia. As a result, this complex exhibited an improved PDT effect compared to the lysosome‐targeted complex, especially under hypoxia conditions, suggestive of a higher practicable potential of mitochondria‐targeted PDT agents in cancer therapy.