Journal
EUROPEAN JOURNAL OF INORGANIC CHEMISTRY
Volume -, Issue 12, Pages 1764-1771Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejic.201601129
Keywords
Iridium; N ligands; Mitochondria; Photodynamic therapy; Cytotoxicity; Cancer
Categories
Funding
- 973 program [2014CB845604, 2015CB856301]
- National Natural Science Foundation of China [21471164, 21525105]
- Fundamental Research Funds for the Central Universities
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Photodynamic therapy (PDT) is an attractive therapeutic modality with high therapeutic efficacy and less side effects compared with other therapies. Herein, we developed a series of cyclometalated Ir-III complexes based on 2,2'-biimidazole with different alkyl substitutions (methyl, ethyl, propyl, and butyl). These complexes can efficiently produce singlet oxygen upon light irradiation. In vitro photocytotoxicity towards four cell lines (HeLa, A549, A549R, and LO2) was examined. Ir1-Ir5 show quick penetration of cells, remarkable mitochondrial accumulation, strong phototoxicity, and they exhibit high selectivity between tumor cells and normal cells. With the highest O-1(2) quantum yields, Ir5 presents the best PDT efficiency with a high phototoxicity index (PI) value (PI = 150) towards HeLa cells. This work provides a valuable avenue to improve the PDT effect by tuning the lipophilicity and other properties with variation of the alkyl substitution on the photosensitizer. In addition, their satisfying PDT effect to a cisplatin-resistant cell line (A549R) may contribute to the future development of improved chemotherapeutics.
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