Antimicrobial Agents and Chemotherapy 2015-03-01

Small-molecule xenomycins inhibit all stages of the Plasmodium life cycle.

Jessey Erath, Julio Gallego-Delgado, Wenyue Xu, Grasiella Andriani, Scott Tanghe, Katerina V Gurova, Andrei Gudkov, Andrei Purmal, Elena Rydkina, Ana Rodriguez

文献索引：Antimicrob. Agents Chemother. 59(3) , 1427-34, (2015)

全文：HTML全文

摘要

Widespread resistance to most antimalaria drugs in use has prompted the search for novel candidate compounds with activity against Plasmodium asexual blood stages to be developed for treatment. In addition, the current malaria eradication programs require the development of drugs that are effective against all stages of the parasite life cycle. We have analyzed the antimalarial properties of xenomycins, a novel subclass of small molecule compounds initially isolated for anticancer activity and similarity to quinacrine in biological effects on mammalian cells. In vitro studies show potent activity of Xenomycins against Plasmodium falciparum. Oral administration of xenomycins in mouse models result in effective clearance of liver and blood asexual and sexual stages, as well as effective inhibition of transmission to mosquitoes. These characteristics position xenomycins as antimalarial candidates with potential activity in prevention, treatment and elimination of this disease. Copyright © 2015, American Society for Microbiology. All Rights Reserved.