Fiche publication
Date publication
août 2019
Journal
International journal of molecular sciences
Auteurs
Membres identifiés du Cancéropôle Est :
Dr BELLEMIN-LAPONNAZ Stéphane
,
Dr HARLEPP Sébastien
Tous les auteurs :
Harlepp S, Chardon E, Bouché M, Dahm G, Maaloum M, Bellemin-Laponnaz S
Lien Pubmed
Résumé
A platinum (II) complex stabilized by a pyridine and an N-heterocyclic carbene ligand featuring an anthracenyl moiety was prepared. The compound was fully characterized and its molecular structure was determined by single-crystal X-ray diffraction. The compound demonstrated high in vitro antiproliferative activities against cancer cell lines with IC ranging from 10 to 80 nM. The presence of the anthracenyl moiety on the N-heterocyclic carbene (NHC) Pt complex was used as a luminescent tag to probe the metal interaction with the nucleobases of the DNA through a pyridine-nucleobase ligand exchange. Such interaction of the platinum complex with DNA was corroborated by optical tweezers techniques and liquid phase atomic force microscopy (AFM). The results revealed a two-state interaction between the platinum complex and the DNA strands. This two-state behavior was quantified from the different experiments due to contour length variations. At 24 h incubation, the stretching curves revealed multiple structural breakages, and AFM imaging revealed a highly compact and dense structure of platinum complexes bridging the DNA strands.
Mots clés
AFM and optical tweezers microscopy, N-heterocyclic carbene, antitumoral activity, platinum, two-state interaction
Référence
Int J Mol Sci. 2019 Aug 27;20(17):
