AsianScientist (Mar. 25, 2013) – An international team of researchers has identified a new class of anti-malarial compounds that target multiple stages of the malaria parasite’s life cycle.
Known as 4-(1H)-quinolone-3-diarylethers, these compounds are selective potent inhibitors of the parasite mitochondrial cytochrome bc1 complex, and could potentially be developed into drugs that treat and prevent malaria infection.
The study, published in Science Translational Medicine, details how the candidate anti-malarials are derived from a compound called endochin that effectively treats malaria in birds. When tested in the laboratory and in mice, the compounds demonstrated strong activity against Plasmodium falciparum and Plasmodium vivax, the two parasites that cause most human cases of malaria.
Of the 4-(1H)-quinolones, the researchers focused their efforts on the compound ELQ-300, which inhibited malaria parasites during the erythrocytic stage, when they cause symptoms in humans; as well as during the gametocyte and developmental stages in the mosquito, when the parasites are transmitted.
The ELQ-300 candidate has been demonstrated to be very effective at blocking transmission in the mouse models. The study results suggest that the compound could be adapted into a once-daily dose in humans and would be slow to engender resistance. The researchers are currently proceeding with preclinical development of ELQ-300.
Transmitted via a mosquito bite, malaria causes cycles of chills, fever, and fatigue, and is responsible for roughly 660,000 deaths per year, according to the World Health Organization. New drugs are needed because of the emergence of malaria-inducing parasites that are resistant to existing medications.
The article can be found at: Nilsen A et al. (2013) Quinolone-3-Diarylethers: A New Class of Antimalarial Drug.
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Source: NIAID; Photo: Gates Foundation/Flickr/CC.
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