Tumor cytotoxicity of 5,6-dimethyl-1,10-phenanthroline and its corresponding gold(III) complex |
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Authors: | Wein Alexander N Stockhausen Adam T Hardcastle Kenneth I Saadein M Reza Peng Shifang Bruce Wang Dongsheng Shin Dong M Chen Zhuo Georgia Eichler Jack F |
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Affiliation: | a Emory University, Department of Chemistry, Atlanta, GA, United Statesb Oxford College of Emory University, Division of Natural Science and Mathematics, Oxford, GA, United Statesc Winship Cancer Institute, Emory University School of Medicine, Atlanta, GA, United States |
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Abstract: | A gold(III) complex possessing 5,6-dimethyl-1,10-phenanthroline (5,6DMP) was synthesized and fully characterized using standard spectroscopic techniques, as well as X-ray crystallography and elemental analysis. The complex [(5,6DMP)AuCl2][BF4] (2) was found to possess a distorted square planar geometry about the gold(III) center, commonplace for d8 Au(III) cations possessing sterically un-hindered polypyridyl ligands. Compound 2 was evaluated for its potential use as an anticancer therapeutic. It was determined that the complex is stable in phosphate buffer over a 24-hour period, thought it does undergo rapid reduction in the presence of equimolar amounts of reduced glutathione (GSH) and ascorbic acid. The DNA binding and in vitro tumor cytotoxicity of the title compound 2 were also determined. It was found to undergo weak and reversible binding to calf thymus DNA, and was more cytotoxic towards a panel of human cancer cell lines than the commonly used chemotherapy agent cisplatin. Cytotoxicity experiments with the free 5,6DMP ligand indicate that the ligand has IC50 values that are slightly lower than those observed for the gold complex (2), and coupled with the fact that the ligand appears to be released from the gold(III) metal center in reducing environments, this suggests the ligand itself may play an important role in the antitumor activity of the parent gold complex. |
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Keywords: | Gold(III) Anticancer Metallotherapy Phenanthroline Cytotoxicity |
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