Plasmodium falciparum: the potential of the cancer chemotherapeutic agent cisplatin and its analogues as anti-malarials.

The anti-malarial activity of the cancer chemotherapeutic agent cisplatin and cisplatin analogues was determined in Plasmodium falciparum. The cisplatin analogues included DNA-targeted acridine-tethered platinum compounds, carboplatin and transplatin. A [(3)H]-hypoxanthine incorporation assay was utilised to determine the IC(50) of cisplatin and related analogues. The DNA-targeted Pt compounds and cisplatin were shown to have IC(50) values that were less than 1 μM in P. falciparum, with the acridine-tethered compounds having the greatest cytotoxicity. Carboplatin and transplatin had IC(50) values of 12 and 16 μM, respectively. The outcome for transplatin was particularly interesting since it is not cytotoxic in mammalian cells. These results were discussed with respect to the potential use of cisplatin and cisplatin analogues as anti-malarial agents.