Potent Antimalarial Agent

Science  15 Feb 2002:
Vol. 295, Issue 5558, pp. 1189
DOI: 10.1126/science.295.5558.1189m

Within human beings infected with malaria, the asexual stages of Plasmodium falciparum reside in red blood cells. Unlike their host cells, the parasites synthesize large amounts of membrane, probably to assist nutrient uptake. Wengelnik et al. (p. 1311; see the news story by Taubes) have been working on ways to inhibit parasite phospholipid biosynthesis that have focused on using structural mimics of choline. The lead compound, G25, was tested in monkeys with heavy infections of P. falciparum and P. vivax (5 to 14% parasitized erythrocytes). They were able to cure the monkeys after intramuscular treatment without recrudescence up to 60 days later. G25 cures monkeys of malaria at doses far below those used for current antimalarials and is effective in mice infected with parasites that are resistant to the drugs currently in use.

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