| Summary: | <p>Abstract</p> <p>Background</p> <p>Malaria is the third most prevalent cause of infectious disease in the world. Resistance of the parasite to classical drugs makes the discovery of new and effective drugs more urgent. The oxidized derivative of hydroxy-<it>cis </it>terpenone (OHCT) is a synthetic molecule that is not toxic to cultured human liver cells at concentrations as high as 60 μM and inhibits activity of cytochrome P450s that metabolize many drugs.</p> <p>Methods</p> <p>OHCT activity against chloroquine-sensitive and -resistant strains of <it>Plasmodium falciparum</it>, and a <it>P. falciparum </it>clone that is partially resistant to artemisinin was assayed <it>in vitro.</it></p> <p>Results</p> <p>OHCT at nanomolar concentrations was effective against all intraerythrocytic stages of <it>P. falciparum </it>and exhibited activity <it>in vitro </it>against both chloroquine-sensitive and -resistant strains of <it>P. falciparum </it>as well as a <it>P. falciparum </it>clone that is partially resistant to artemisinin. Moreover, OHCT exhibited potent activity against gametocytes, the form that is transmitted by mosquitoes and essential for the spread of malaria.</p> <p>Conclusion</p> <p>OHCT displays strong growth inhibitory activity against all stages of <it>P. falciparum </it>and no evidence of toxicity to human cells in culture. It is easily synthesized and has the potential for inhibiting metabolism of drugs used in combination therapies.</p>
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