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 shu

DNA Interaction and Antitumor Activities of Ruthenium(Ⅱ) Polypyridyl Complex

XU Li ¹ ,
CHEN Yu ² ,
WU Jia-Huan ¹ ,
WEN Ban-Kang ¹

1.
1. School of Chemistry and Chemical Engineering, Guangdong Pharmaceutical University, Zhongshan, Guangdong 528458, China;

Received Date: 22 September 2012
Available Online: 27 November 2012
Fund Project: 2012年广东省大学生创新创业训练计划(No.1057312013)资助项目。 (No.1057312013)

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.
- ruthenium complex;cytotoxicity;DNA-binding;cell cycle arrest
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