Citation: XU Li, CHEN Yu, WU Jia-Huan, WEN Ban-Kang. DNA Interaction and Antitumor Activities of Ruthenium(Ⅱ) Polypyridyl Complex[J]. Chinese Journal of Inorganic Chemistry, ;2013, 29(3): 613-620. doi: 10.3969/j.issn.1001-4861.2013.00.107
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The interactions of the Ru(Ⅱ) complex, [Ru(phen)2(Hecip)]2+ (phen=1,10-phenanthroline, Hecip=N-ethyl-4-([1,10]-phenanthroline[5,6-f]imidazol-2-yl)carbazole), with calf thymus DNA (CT DNA) were studied by using absorption spectroscopy, binding stoichiometry, viscosity measurement and photoactivated cleavage. A tight 2:1 complex is formed by the Ru(Ⅱ) polypyridyl complex and CT DNA with a binding constant exceeding 105 mol-1·L and with a binding mode of intercalation. Furthermore, the complex exhibits efficient DNA cleavage activity on UV (365 nm) irradiation via a mechanistic pathway involving formation of singlet oxygen as the reactive species. On the other hand, the cytotoxic activity of the complex was tested by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide (MTT) method. The complex shows prominent anticancer activity against selected tumor cell lines with IC50 values lower than those of cisplatin. Further flow cytometry experiments show that the cytotoxic Ru(Ⅱ) complex can cause cell cycle arrest in the S phase.
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