title: In vitro activity of artemisone compared with artesunate against Plasmodium falciparum.
abstract: Artemisinins show the potential for neurotoxicity in preclinical studies. Artemisone is a leading candidate of second-generation semi-synthetic artemisinin derivatives for antimalarial therapy devoid of neurotoxicity. Artemisone showed 3-5-fold higher in vitro activity (50% effective concentration (EC50) = 0.14 nmol/L, EC90 = 2.55 nmol/L) than artesunate against fresh Plasmodium falciparum isolates from Gabon and a high-activity correlation indicates a shared drug target.
authors.affiliation: Medical Research Unit, Albert Schweitzer Hospital, Lambaréné, Gabon. michael.ramharter@meduniwien.ac.at
authors.forename: Michael
authors.initials: M
authors.lastname: Ramharter
authors.forename: Dominik
authors.initials: D
authors.lastname: Burkhardt
authors.forename: Johannes
authors.initials: J
authors.lastname: Nemeth
authors.forename: Ayola A
authors.initials: AA
authors.lastname: Adegnika
authors.forename: Peter G
authors.initials: PG
authors.lastname: Kremsner
mesh_terms: D000818:Animals; D000962:Antimalarials / Q000494:pharmacology*; D037621:Artemisinins / Q000494:pharmacology*; D000077332:Artesunate; D006801:Humans; D021261:Parasitic Sensitivity Tests; D010963:Plasmodium falciparum / Q000187:drug effects*; D012044:Regression Analysis; D012717:Sesquiterpenes / Q000494:pharmacology*
chemical_list: D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes; D000077332:Artesunate; C514498:artemisone