Cellular Uptake, DNA Binding and Apoptosis Induction of CytotoxicTrans‐[PtCl2(N,N‐dimethylamine)(Isopropylamine)] in A2780cisROvarian Tumor Cells

Authors:
Open Access
Publisher website
Google Scholar
Abstract
Trans‐[PtCl2(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‐[PtCl2(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‐[PtCl2(N,N‐dimethylamine)( isopropylamine)] is lower than that of cis‐DDP. Moreover, trans‐[PtCl2(N,N‐dimethylamine)(isopropylaminae)] is partially inactivated by intracellular levels of glulathione. The result suggest that circumvention of ciplatin resistance by trans‐[PtCl2(N,N‐dimethylamine)(isopropylamine)] in A2780cisR cells might be related with the ability of this drug to induce apoptosis.