title: Cellular Uptake, DNA Binding and Apoptosis Induction of Cytotoxic Trans-[PtCl(2)(N,N-dimethylamine)(Isopropylamine)] in A2780cisR Ovarian Tumor Cells.
abstract: Trans-[PtCl(2)(N,N-dimethylamine)(isopropylamine)] is a novel trans-platinum compound that shows cytotoxic activity in several cisplatin resistant cell lines. The aim of this paper was to analyse, by means of molecular cell biology techniques and total reflection X-ray fluorescence (TXRF), the cytotoxic activity, the induction of apoptosis, the cellular uptake and the DNA binding of trans-[PtCl(2)(N,N-dimethylamine)(isopropylamine)] in the cisplatin resistant cell line A2780cisR. The results show that this drug is more cytotoxic and induces a higher amount of apoptotic cells than cisplatin in A2780cisR cells. However, the intracellular accumulation and extent of binding to DNA of trans-[PtCl(2)(N,N-dimethylamine)( isopropylamine)] is lower than that of cis-DDP. Moreover, trans-[PtCl(2)(N,N-dimethylamine)(isopropylaminae)] is partially inactivated by intracellular levels of glulathione. The result suggest that circumvention of ciplatin resistance by trans-[PtCl(2)(N,N-dimethylamine)(isopropylamine)] in A2780cisR cells might be related with the ability of this drug to induce apoptosis.
authors.affiliation: Departamento de Química Inorgánica Facultad de Ciencias Universidad Autónoma de Madrid, Cantoblanco Madrid 28049 Spain.
authors.forename: J M
authors.initials: JM
authors.lastname: Pérez
authors.forename: E I
authors.initials: EI
authors.lastname: Montero
authors.forename: A G
authors.initials: AG
authors.lastname: Quiroga
authors.forename: M A
authors.initials: MA
authors.lastname: Fuertes
authors.forename: C
authors.initials: C
authors.lastname: Alonso
authors.forename: C
authors.initials: C
authors.lastname: Navarro-Ranninger