-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
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.
Mots clés
N-Heterocyclic carbene, antitumoral activity, platinum, polyethyleneimine
Référence
Int J Mol Sci. 2018 Nov 5;19(11):