title: Transmission-blocking activity of tafenoquine (WR-238605) and artelinic acid against naturally circulating strains of Plasmodium vivax in Thailand.
abstract: The sporontocidal activity of tafenoquine (WR-238605) and artelinic acid was determined against naturally circulating isolates of Plasmodium vivax in western Thailand. Primaquine was used as a negative control and a dihydroacridine-dione (WR-250547) was used as a positive control. Laboratory-reared Anopheles dirus mosquitoes were infected with P. vivax by allowing mosquitoes to feed on blood (placed in an artificial-membrane feeding apparatus) collected from gametocytemic volunteers reporting to local malaria clinics in Tak province, Thailand. Four days post-infection, mosquitoes were refed on uninfected mice treated 90 minutes earlier with a given drug. Drug activity was determined by assessing oocyst and sporozoite development. Neither primaquine nor artelinic acid affected oocyst or sporozoite development at a dose of 100 mg of base drug/kg of mouse body weight. In contrast, tafenoquine and WR-250547 affected sporogonic development at doses as low as 25.0 and 0.39 mg/kg, respectively. The potential role of these compounds in the prevention of malaria transmission is discussed, as are alternative strategies for the use of transmission-blocking antimalarial drugs.
authors.affiliation: Department of Entomology, Armed Forces Research Institute of Medical Sciences, Bangkok, Thailand.
authors.forename: Narong
authors.initials: N
authors.lastname: Ponsa
authors.forename: Jetsumon
authors.initials: J
authors.lastname: Sattabongkot
authors.forename: Pattamaporn
authors.initials: P
authors.lastname: Kittayapong
authors.forename: Nantana
authors.initials: N
authors.lastname: Eikarat
authors.forename: Russell E
authors.initials: RE
authors.lastname: Coleman
mesh_terms: D000634:Aminoquinolines / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000852:Anopheles / Q000469:parasitology*; D000962:Antimalarials / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D037621:Artemisinins / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D006801:Humans; D007303:Insect Vectors / Q000469:parasitology; D016780:Malaria, Vivax / Q000188:drug therapy* / Q000469:parasitology; D051379:Mice; D021261:Parasitic Sensitivity Tests; D010966:Plasmodium vivax / Q000187:drug effects* / Q000254:growth & development; D011319:Primaquine / Q000008:administration & dosage / Q000494:pharmacology / Q000627:therapeutic use; D012717:Sesquiterpenes / Q000008:administration & dosage / Q000494:pharmacology* / Q000627:therapeutic use
chemical_list: D000634:Aminoquinolines; D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes; C062768:artelinic acid; C055852:tafenoquine; D011319:Primaquine