期刊
JOURNAL OF INFECTIOUS DISEASES
卷 205, 期 8, 页码 1278-1286出版社
OXFORD UNIV PRESS INC
DOI: 10.1093/infdis/jis184
关键词
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资金
- FCT [BPD/64539/2010]
- Alexander von Humboldt foundation
- Chemical Computing Group
- Fundacao para a Ciencia e Tecnologia [PTDC/SAU-MII/099118/2008, PTDC/SAU-GMG/100313/2008, HMSP-CT/SAU-ICT/10068/2009]
- German Ministry of Education and Research
- European Union [242095]
- Fundação para a Ciência e a Tecnologia [PTDC/SAU-GMG/100313/2008, PTDC/SAU-MII/099118/2008] Funding Source: FCT
Plasmodium parasites undergo a clinically silent and obligatory developmental phase in the host's liver cells before they are able to infect erythrocytes and cause malaria symptoms. To overcome the scarcity of compounds targeting the liver stage of malaria, we screened a library of 1037 existing drugs for their ability to inhibit Plasmodium hepatic development. Decoquinate emerged as the strongest inhibitor of Plasmodium liver stages, both in vitro and in vivo. Furthermore, decoquinate kills the parasite's replicative blood stages and is active against developing gametocytes, the forms responsible for transmission. The drug acts by selectively and specifically inhibiting the parasite's mitochondrial bc(1) complex, with little cross-resistance with the antimalarial drug atovaquone. Oral administration of a single dose of decoquinate effectively prevents the appearance of disease, warranting its exploitation as a potent antimalarial compound.
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