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Original Articles

Aliphatic polyamine ruthenium(II) complexes: crystal structure, DNA-binding, photocleavage, cytotoxicity, and antioxidation

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Pages 4408-4422 | Received 09 Feb 2015, Accepted 14 Aug 2015, Published online: 24 Sep 2015
 

Abstract

The DNA-binding behaviors of two aliphatic polyamine Ru(II) complexes, [Ru(dppt)(dien)](ClO4)2 (1) and [Ru(pta)(dien)](ClO4)2 (2) (dppt, pta, and dien standing for 3-(1,10-phenanthrolin-2-yl)-5,6-diphenyl-as-triazine, 3-(1,10-phenanthrolin-2-yl)-5,6-diphenyl-as-triazino[5,6-f]-acenaphthylene, and diethylenetriamine, respectively), were studied through absorption titration, thermal denaturation, and viscosity measurements. The results indicate that the DNA-binding affinity of 2 is much greater than that of 1; 2 binds to CT-DNA in an intercalative mode but 1 binds to CT-DNA through partial intercalation. In addition, the complexes react with DNA in an energy-driven process with a decrease in entropy. The photocleavage of plasmid pBR322 can be triggered by 1 and 2 and strengthened with an increased concentration of both complexes. The scavenging activity of 1 against hydroxyl radical (˙OH) is slightly better than that of 2 according to the antioxidation experiment. The standard cytotoxicity experiments were carried out with MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide); the results indicate that the proliferation of Hela, A549, and 7402 cells is inhibited by these two compounds in a dose-dependent manner. The X-ray crystal structure of 1 and some results of DFT (the density functional theory) calculations were analyzed to further understand the differences in DNA-binding strength of the complexes.

Acknowledgements

We are grateful to Prof. Hui Chao (Sun Yat-Sen University) for his specific directions and Prof. Kang-Cheng Zheng (Sun Yat-sen University) for the good work on the DFT calculation.

Disclosure statement

No potential conflict of interest was reported by the authors.

Additional information

Funding

This work was supported by the National Science Foundation of China [grant number 21071099]; National Science Foundation of Guangdong Province [grant number 2014A030307015]; Featured Innovation in Colleges and Universities of Guangdong Province (Natural Science) Project [grant number 2014KTSCX169] and Shaoguan University.

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