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Abstract
The activities of 8 platinum drug complex salts were determined against Leishmania donovani promastigotes. The three most active salts were selected: [Pt<sup>IV</sup>Br<sub>6</sub>]H<sub>2</sub> (pentamidine); [Pt<sup>IV</sup>Br<sub>6</sub>]H<sub>2</sub> (stilbamidine), and [Pt<sup>IV</sup>Cl<sub>6</sub>]H<sub>2</sub> (2-piperazinyl(1) ethyl amine), which induced growth-inhibition rates of more than 50% at 24 h of treatment and at the maximum dosage tested. The cytotoxicity assays on the macrophage cell line J-774 showed high cytotoxicity for the salt [Pt<sup>IV</sup>Br<sub>6</sub>]H<sub>2</sub> (stilbamidine) with a percentage of specific <sup>51</sup>Cr release of 58.2% at 24 h of incubation and 100 µg/ml. Meanwhile, assays of the other compounds showed practically no cytotoxicity. The salt [Pt<sup>IV</sup>Br<sub>6</sub>]H<sub>2</sub> (pentamidine) notably inhibited the incorporation of <sup>3</sup>H-thymidine in the treated parasites. The ultrastructural alterations observed in the flagellates treated with the salts [Pt<sup>IV</sup>Cl<sub>6</sub>]H<sub>2</sub> (2-piperazinyl(1)ethyl amine) and [Pt<sup>IV</sup>Br<sub>6</sub>]H<sub>2</sub> (pentamidine) suggest that both act preferentially at the nuclear level and at the kinetoplast-mitochondrion complex. Both compounds showed a high in vivo activity in parasitized Wistar rats.
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