Bis-intercalative dinuclear platinum(II) 6-phenyl-2,2′-bipyridine complexes exhibit enhanced DNA affinity but similar cytotoxicity compared to the mononuclear unit

Hing Leung Chan, Dik Lung Ma, Mengsu Yang*, Chi Ming Che

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

42 Citations (Scopus)

Abstract

The interactions between a series of platinum complexes, including (pyridyl)(6-phenyl-2,2′-bipyridine) platinum(II) hexafluorophosphate (1), three dinuclear bis[(6-phenyl-2,2′-bipyridine)platinum(II)] complexes (2-4), and (4-aminopyridine)(4,6-diphenyl-2,2′-bipyridine)platinum(II) perchlorate (5) with DNA have been investigated. All Pt(II) complexes, except 5, were demonstrated to be DNA intercalators, based on viscosity measurements. Absorption and fluorescence titration results indicated that the addition of a phenyl ring to the 6-phenyl-2,2′-bipyridine ligand dramatically reduced the DNA binding of the Pt(II) complex 5. The dinuclear complexes 2-4 exhibited multiple binding modes of mono/bisintercalation and groove binding, as revealed by viscosity and fluorescence titration measurements. While complexes 2-4 bound to DNA with significantly enhanced affinities as compared to 1, compounds 1 and 2-4 showed similar IC50 values against a panel of cancer cell lines. In addition, these complexes showed similar cellular uptakes. The results indicated that the cytotoxicity of these (6-phenyl-2,2′ -bipyridine)platinum compounds may not be mediated through DNA binding but may involve interacting mechanisms with cellular components other than DNA.

Original languageEnglish
Pages (from-to)761-769
Number of pages9
JournalJournal of Biological Inorganic Chemistry
Volume8
Issue number7
DOIs
Publication statusPublished - Sep 2003

Scopus Subject Areas

  • Biochemistry
  • Inorganic Chemistry

User-Defined Keywords

  • Bisintercalation
  • Cytotoxicity
  • DNA binding
  • Platinum

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