-Heterocyclic Carbene-Polyethyleneimine (PEI) Platinum Complexes Inducing Human Cancer Cell Death: Polymer Carrier Impact.

Fiche publication

Date publication

novembre 2018

Journal

International journal of molecular sciences

Auteurs

Membres identifiés du Cancéropôle Est :
Dr BELLEMIN-LAPONNAZ Stéphane , Pr FOURNEL Sylvie

Tous les auteurs :
Wantz M, Bouché M, Dahm G, Chekkat N, Fournel S, Bellemin-Laponnaz S

Lien Pubmed

https://www.ncbi.nlm.nih.gov/pubmed/30400637

Résumé

The high interest in -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.