title: Small-molecule xenomycins inhibit all stages of the Plasmodium life cycle.
abstract: 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.
authors.affiliation: New York University School of Medicine, Department of Microbiology, Division of Parasitology, New York, New York, USA.
authors.forename: Jessey
authors.initials: J
authors.lastname: Erath
authors.affiliation: New York University School of Medicine, Department of Microbiology, Division of Parasitology, New York, New York, USA.
authors.forename: Julio
authors.initials: J
authors.lastname: Gallego-Delgado
authors.affiliation: New York University School of Medicine, Department of Microbiology, Division of Parasitology, New York, New York, USA.
authors.forename: Wenyue
authors.initials: W
authors.lastname: Xu
authors.affiliation: New York University School of Medicine, Department of Microbiology, Division of Parasitology, New York, New York, USA.
authors.forename: Grasiella
authors.initials: G
authors.lastname: Andriani
authors.affiliation: New York University School of Medicine, Department of Microbiology, Division of Parasitology, New York, New York, USA.
authors.forename: Scott
authors.initials: S
authors.lastname: Tanghe
authors.affiliation: Roswell Park Cancer Institute, Department of Cell Stress Biology, Buffalo, New York, USA.
authors.forename: Katerina V
authors.initials: KV
authors.lastname: Gurova
authors.affiliation: Roswell Park Cancer Institute, Department of Cell Stress Biology, Buffalo, New York, USA.
authors.forename: Andrei
authors.initials: A
authors.lastname: Gudkov
authors.affiliation: Incuron LLC, Buffalo, New York, USA.
authors.forename: Andrei
authors.initials: A
authors.lastname: Purmal
authors.affiliation: Roswell Park Cancer Institute, Department of Cell Stress Biology, Buffalo, New York, USA.
authors.forename: Elena
authors.initials: E
authors.lastname: Rydkina
authors.affiliation: New York University School of Medicine, Department of Microbiology, Division of Parasitology, New York, New York, USA ana.rodriguez@nyumc.org.
authors.forename: Ana
authors.initials: A
authors.lastname: Rodriguez
mesh_terms: D000818:Animals; D000852:Anopheles / Q000469:parasitology; D000962:Antimalarials / Q000494:pharmacology*; D004912:Erythrocytes / Q000469:parasitology; D005260:Female; D008018:Life Cycle Stages / Q000187:drug effects*; D008297:Male; D051379:Mice; D041681:NIH 3T3 Cells; D010961:Plasmodium / Q000187:drug effects* / Q000254:growth & development
chemical_list: D000962:Antimalarials