stilbamidine and Leishmaniasis--Visceral

The activities of 8 platinum drug complex salts were determined against Leishmania donovani promastigotes. The three most active salts were selected: [PtIVBr6]H2 (pentamidine); [PtIVBr6]H2 (stilbamidine), and [PtIVCl6]H2 (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 [PtIVBr6]H2 (stilbamidine) with a percentage of specific 51Cr release of 58.2% at 24 h of incubation and 100 microg/ml. Meanwhile, assays of the other compounds showed practically no cytotoxicity. The salt [PtIVBr6]H2 (pentamidine) notably inhibited the incorporation of 3H-thymidine in the treated parasites. The ultrastructural alterations observed in the flagellates treated with the salts [PtIVCl6]H2 (2-piperazinyl(1)ethyl amine) and [PtIVBr6]H2 (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.

Topics: Animals; Antiprotozoal Agents; Cell Line; Cricetinae; Drug Evaluation, Preclinical; Humans; Leishmania donovani; Leishmaniasis, Visceral; Mesocricetus; Mice; Mice, Inbred BALB C; Pentamidine; Platinum Compounds; Rats; Rats, Wistar; Stilbamidines

Topics: Humans; Leishmaniasis; Leishmaniasis, Visceral; Stilbamidines

Topics: Asian People; Humans; Leishmaniasis; Leishmaniasis, Visceral; Stilbamidines

Topics: Humans; Leishmaniasis; Leishmaniasis, Visceral; Recurrence; Stilbamidines

Topics: Humans; Leishmaniasis; Leishmaniasis, Visceral; Stilbamidines; United States

Topics: Humans; Leishmaniasis, Visceral; Stilbamidines