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DNA-binding and photocleavage, cytotoxicity, apoptosis and antioxidant activity studies of ruthenium(II) complexes

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Abstract

Two ruthenium(II) polypyridyl complexes, namely [Ru(phen)2(DMDPPZ)](ClO4)2 1 (phen = 1,10-phenanthroline, DMDPPZ = 3,6-dimethyldipyrido[3,2-a:2′,3′-c]phenazine) and [Ru(dmp)2(DMDPPZ)](ClO4)2 2 (dmp = 2,9-dimethyl-1,10-phenanthroline), have been synthesized and characterized. The DNA-binding properties of the complexes were investigated by spectrophotometric methods, viscosity measurements, and photoactivated cleavage studies. The DNA-binding constants for complexes 1 and 2 have been determined as 8.78 (±0.94) × 105 M−1 (s = 3.02) and 1.26 (±0.35) × 105 M−1 (s = 1.69), respectively. The results suggest that these complexes bind to calf thymus DNA through intercalation. When irradiated at 365 nm, the complexes promote the photocleavage of pBR322 DNA, and complex 1 cleaves DNA more effectively than complex 2 under comparable experimental conditions. The cytotoxicities of complexes 1 and 2 have been evaluated by the MTT (3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl-2H-tetrazolium bromide) method. Complex 2 shows higher anticancer potency than complex 1 against four tumor cell lines. The apoptosis-inducing activity was assessed by acridine orange/ethidium bromide staining assay, and the antioxidant activities of these complexes against hydroxyl radical were also explored.

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Acknowledgments

This work was supported by the National Nature Science Foundation of China (Nos. 30800227 and 31070858) and Guangdong Pharmaceutical University.

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Authors and Affiliations

  1. School of Chemistry and Chemical Engineering, Guangdong Pharmaceutical University, Zhongshan, 528458, People’s Republic of China

    Li Xu & Juan He

  2. School of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, 510006, People’s Republic of China

    Yang-Yin Xie, Zhen-Hua Liang & Yun-Jun Liu

  3. School of Food Science, Guangdong Pharmaceutical University, Zhongshan, 528458, People’s Republic of China

    Nan-Jing Zhong

  4. School of Life Science and Biopharmacological, Guangdong Pharmaceutical University, Guangzhou, 510006, People’s Republic of China

    Hong-Liang Huang

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  1. Li Xu
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  2. Yang-Yin Xie
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  4. Zhen-Hua Liang
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  5. Juan He
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Correspondence to Hong-Liang Huang or Yun-Jun Liu.

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Xu, L., Xie, YY., Zhong, NJ. et al. DNA-binding and photocleavage, cytotoxicity, apoptosis and antioxidant activity studies of ruthenium(II) complexes. Transition Met Chem 37, 197–205 (2012). https://doi.org/10.1007/s11243-011-9575-y

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  • DOI: https://doi.org/10.1007/s11243-011-9575-y

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