Preprint Article Version 1 This version is not peer-reviewed

N-Heterocyclic Carbene-PEI Platinum Complexes Inducing Human Cancer Cell Death: Polymer Carrier Impact

Version 1 : Received: 8 October 2018 / Approved: 8 October 2018 / Online: 8 October 2018 (16:05:07 CEST)

A peer-reviewed article of this Preprint also exists.

Wantz, M.; Bouché, M.; Dahm, G.; Chekkat, N.; Fournel, S.; Bellemin-Laponnaz, S. N-Heterocyclic Carbene-Polyethyleneimine (PEI) Platinum Complexes Inducing Human Cancer Cell Death: Polymer Carrier Impact. Int. J. Mol. Sci. 2018, 19, 3472. Wantz, M.; Bouché, M.; Dahm, G.; Chekkat, N.; Fournel, S.; Bellemin-Laponnaz, S. N-Heterocyclic Carbene-Polyethyleneimine (PEI) Platinum Complexes Inducing Human Cancer Cell Death: Polymer Carrier Impact. Int. J. Mol. Sci. 2018, 19, 3472.

Journal reference: Int. J. Mol. Sci. 2018, 19, 3472
DOI: 10.3390/ijms19113472

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 that the activity of these conjugates is modulated by the size of the polymer and the overall density of metal ions onto polymer chains. They displayed an effective activity after only 45 minutes of exposure in vitro correlated with a quick uptake by the cells as shown by the use of various fluorescent-tagged derivatives.

Subject Areas

Antitumoral activity; platinum; N-heterocyclic carbene; polyethyleneimine.

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