N-Heterocyclic carbene-polyethyleneimine (PEI) platinum complexes inducing human cancer cell death: Polymer carrier impact

May Wantz, Mathilde Bouché, Georges Dahm, Neïla Chekkat, Sylvie Fournel*, Stéphane Bellemin-Laponnaz

*Corresponding author for this work

Research output: Contribution to journalArticleResearchpeer-review

8 Citations (Scopus)

Abstract

The high interest in N-Heterocyclic platinum carbene complexes in cancer research stems from their high cytotoxicity to human cancer cells, their stability, as well as their ease of functionalization. However, the development of these new molecules as anticancer agents still faces multiple challenges, in particular solubility in aqueous media. Here, we synthesized platinum-NHC bioconjugates that combine water-solubility and cytotoxicity by using polyethyleneimine as polymer carrier. We showed on 8 different types of cells that the activity of these conjugates is modulated by the size of the polymer and the overall density of metal ions onto polymer chains. Using HCT116 cells, the conjugates displayed an effective activity after only 45 min of exposure in vitro correlated with a quick uptake by the cells as shown by the use of various fluorescent-tagged derivatives.

Original languageEnglish
Article number3472
JournalInternational Journal of Molecular Sciences
Volume19
Issue number11
DOIs
Publication statusPublished - 5 Nov 2018
Externally publishedYes

Keywords

  • Antitumoral activity
  • N-heterocyclic carbene
  • Platinum
  • Polyethyleneimine

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