期刊
METALLOMICS
卷 5, 期 7, 页码 844-854出版社
ROYAL SOC CHEMISTRY
DOI: 10.1039/c3mt20270d
关键词
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资金
- National Science Foundation of China [21071155, 21172273, 21171177]
- National High Technology Research and Development Program of China (863 Program) [2012AA020305]
- National Science Foundation of Guangdong Province [9351027501000003]
- Research Fund for the Doctoral Program of Higher Education [20110171110013]
- State Key Laboratory of Optoelectronic Materials and Technologies [2010-ZY-4-5]
- Sun Yat-Sen University
Four ruthenium(II) asymmetric complexes, [Ru(bpy)(2)(PAIDH)](2+) (bpy = 2,2'-bipyridine, PAIDH = 2-pyridyl-1H-anthra[1,2-d]imidazole-6,11-dione, 1), [Ru(phen)(2)(PAIDH)](2+) (phen = 1,10-phenanthroline, 2), [Ru(dmp)(2)(PAIDH)](2+) (dmp = 4,7-dimethyl-1,10-phenanthroline, 3) and [Ru(dip)(2)(PAIDH)](2+) (dip = 4,7-diphenyl-1,10-phenanthroline, 4), have been synthesized and characterized. These complexes displayed potent anti-proliferation activity against various cancer cell lines and had high selectivity between tumor cells and normal cells. HeLa cells exhibited the highest sensitivity to complex 4, accounting for the greatest cellular uptake. Complex 4 was shown to accumulate preferentially in the mitochondria of HeLa cells and induced apoptosis via the mitochondrial pathway, which involved ROS generation, mitochondrial membrane potential depolarisation, and Bcl-2 and caspase family members activation. These results demonstrated that complex 4 induced cancer cell apoptosis by acting on mitochondrial pathways.
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