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Issue 48, 2009
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The role of bridging ligands in determining DNA-binding ability and cross-linking patterns of dinuclear platinum(II) antitumour complexes

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Abstract

The DNA binding ability and binding mode of platinum complexes are crucial factors that govern their cytotoxic activity. In this work, circular dichroism spectroscopy, gel electrophoresis and MALDI-TOF MS spectrometry combined with enzymatic degradation have been used to elucidate the role of bridging ligands in DNA-binding ability and cross-linking patterns of two dinuclear antitumour active platinum(II) complexes, {[cis-Pt(NH3)2Cl]2L1}(NO3)2 (1, L1= 4,4′-methylenedianiline) and {[cis-Pt(NH3)2Cl]2L2}(NO3)2 (2, L2 = α,α′-diamino-p-xylene). Although both complexes have two cis-diammine-Pt(II) moieties (1,1/c,c), complex 1 exhibits much higher DNA-binding ability than complex 2. The former readily forms both 1,3- and 1,4-intrastrand cross-links with DNA oligonucleotides, while the latter preferentially forms 1,4- rather than 1,3-intrastrand cross-links. Cytotoxicity studies against a human non-small-cell lung cancer cell line (A549) demonstrate that complex 1 has higher activity than 2. These results show that the linker properties play a critical role in controlling the DNA-binding and cross-linking abilities and in modulating the cytotoxicity of dinuclear platinum complexes.

Graphical abstract: The role of bridging ligands in determining DNA-binding ability and cross-linking patterns of dinuclear platinum(ii) antitumour complexes

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Publication details

The article was received on 03 Jul 2009, accepted on 28 Oct 2009 and first published on 13 Nov 2009


Article type: Paper
DOI: 10.1039/B913236H
Citation: Dalton Trans., 2009,0, 10889-10895
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    The role of bridging ligands in determining DNA-binding ability and cross-linking patterns of dinuclear platinum(II) antitumour complexes

    J. Zhu, M. Lin, D. Fan, Z. Wu, Y. Chen, J. Zhang, Y. Lu and Z. Guo, Dalton Trans., 2009, 0, 10889
    DOI: 10.1039/B913236H

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