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Ruthenium (II) polypyridyl complexes stabilize the bcl-2 promoter quadruplex and induce apoptosis of Hela tumor cells

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Abstract

In the present study, the interaction between GC-rich sequence of bcl-2 gene P1 promoter (Pu39) and two ruthenium (II) polypyridyl complexes, [Ru(bpy)2(tip)]2+ (1) and [Ru(phen)2(tip)]2+ (2), was investigated by UV–Visible, fluorescence spectroscopy, circular dichroism, fluorescence resonance energy transfer melting assay and polymerase chain reaction stop assay. Those experimental results indicated that the two complexes can effectively stabilize the G-quadruplex of Pu39. It was found that the complex 2 exhibited greater cytotoxic activity than 1 against human Hela cells and can enter into Hela cells in a short period of time to effectively induce apoptosis of cells. Further experiments found that complexes 1 and 2 had as potent inhibitory effects on ECV-304 cell migration as suramin. Those noteworthy results provide new insights into the development of anticancer agents for targeting G-quadruplex DNA.

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Acknowledgments

This work was supported by the National Natural Science Foundation of China (20871056, 21171070), the Planned Item of Science and Technology of Guangdong Province (c1011220800060), and the Planned Item of Science and The Fundamental Research Foundation of Shenzhen City (Major Project) (JC201005250058A).

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Correspondence to Jie Liu.

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Wang, C., Yu, Q., Yang, L. et al. Ruthenium (II) polypyridyl complexes stabilize the bcl-2 promoter quadruplex and induce apoptosis of Hela tumor cells. Biometals 26, 387–402 (2013). https://doi.org/10.1007/s10534-013-9622-6

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  • DOI: https://doi.org/10.1007/s10534-013-9622-6

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