There has been a continuing effort for the discovery of novel
platinum(IV)-based antitumor compounds with better therapeutic performances than
cisplatin. In the present work, the anticancer action of recently synthesized Pt(IV)-based complex [Pt(HPxSC)Cl(3)] was investigated using rat and human
astrocytoma cell lines C6 and U251. [Pt(HPxSC)Cl(3)] markedly reduced the number of cultured
astrocytoma cells (IC(50), 80 microM), as determined by
crystal violet assay. The Pt(IV) complex induced apoptotic death of
tumor cells, as flow cytometry analysis of the
propidium iodide-stained cellular
DNA revealed approx. 30% of hypodiploid cells in [Pt(HPxSC)Cl(3)]-treated
astrocytoma cell cultures. On the other hand, [Pt(HPxSC)Cl(3)] at 200 microM did not affect the viability of rat primary astrocytes, unlike the established anticancer
drug cisplatin, which displayed high toxicity toward both
astrocytoma cells (IC(50), 15 microM) and primary astrocytes (IC(50), 20 microM). Moreover, [Pt(HPxSC)Cl(3)] at 100 microM did not interfere with the ability of rat peritoneal macrophages to produce important antitumor molecules
nitric oxide and
tumor necrosis factor-alpha. Finally, we assessed the ability of [Pt(HPxSC)Cl(3)] to restrain growth of some bacterial and yeast strains, but it showed rather limited antimicrobial activity.