Taurine-modified Ru(ii)-complex targets cancerous brain cells for photodynamic therapyElectronic supplementary information (ESI) available: Experimental details, characterization data, and supplementary figures. See DOI: 10.1039/c7cc03337k

• Main Authors: Du, Enming, Hu, Xunwu, Roy, Sona, Wang, Peng, Deasy, Kieran, Mochizuki, Toshiaki, Zhang, Ye
• Format: Journal Article
• Language: English
• Published: 30.05.2017
• ISSN: 1359-7345; 1364-548X
• DOI: 10.1039/c7cc03337k

The precision and efficacy of photodynamic therapy (PDT) is essential for the treatment of brain tumors because the cancer cells are within or adjacent to the delicate nervous system. Taurine is an abundant amino acid in the brain that serves the central nervous system (CNS). A taurine-modified polypyridyl Ru-complex was shown to have optimized intracellular affinity in cancer cells through accumulation in lysosomes. Symmetrical modification of this Ru-complex by multiple taurine molecules enhanced the efficiency of molecular emission with boosted generation of reactive oxygen species. These characteristic features make the taurine-modified Ru-complex a potentially effective photosensitizer for PDT of target cancer cells, with outstanding efficacy in cancerous brain cells. Symmetrical taurine modification not only enhances the intracellular affinity of a polypyridyl Ru-complex to cancer cells, but also boosts the quantum yield in a pH-independent manner without sacrificing water solubility for cytosolic photosensitizers of photodynamic therapy, with prominent efficacy in cancerous brain cells.