Cytotoxic and anticancer properties of new ruthenium polypyridyl complexes with different lipophilicities

Anjong Florence Tikum, Yu Jeong Jeon, Ju Hyun Lee, Min Hee Park, In Yeong Bae, Sang Heon Kim, Hye Jin Lee, Jinheung Kim

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13 Scopus citations


Three ruthenium complexes containing a bidentate piq ligand, [(piq)Ru(bpy)2]2+ (1), [(piq)Ru(phen)2]2+ (2), and [(piq)Ru(DIP)2]2+ (3) (piq = phenylisoquinolinate, bpy = 2,2′-bipyridine, phen = 1,10-phenanthroline, DIP = 4,7-diphenyl-1,10-phenanthroline), were prepared. The DNA binding properties of complexes 1–3 to double-stranded DNA were studied. The binding of 1–3 to calf-thymus DNA (ct-DNA) yielded lower emission intensities than those observed with the corresponding Ru complexes alone. To explore potential interactions of complexes 1–3 with lipid-rich organs in live cells, the emission properties of the Ru probes were studied with liposomes. The emission intensities of complexes 1–3 were enhanced to similar extents upon interaction with liposomes. The cytotoxic activities of the complexes against MDA-MB-231 and HUVECs were evaluated in vitro. The effects of complexes 1–3 on the survival of MDA-MB-231 cells were examined and compared with that of cis-platin. Complexes 2 and 3 were more cytotoxic to cancer cells than cis-platin. Complexes 1–3 showed cellular uptakes of 1.1, 10.6, and 76.6%, respectively, indicating that the greatest amount of complex 3 entered the cancer cells. Inhibition of cell migration by complexes 1–3 was also evaluated by the wound healing assay.

Original languageEnglish
Pages (from-to)204-210
Number of pages7
JournalJournal of Inorganic Biochemistry
StatePublished - Mar 2018

Bibliographical note

Publisher Copyright:
© 2018 Elsevier Inc.


  • Anticancer activity
  • Cell migration
  • Cellular uptake
  • Cytotoxic activity
  • Polypyridyl ruthenium complex


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