In vitro activity of artemisone compared with artesunate against Plasmodium falciparum.
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.
Ramharter
Michael
M
Medical Research Unit, Albert Schweitzer Hospital, Lambaréné, Gabon. michael.ramharter@meduniwien.ac.at
Burkhardt
Dominik
D
Nemeth
Johannes
J
Adegnika
Ayola A
AA
Kremsner
Peter G
PG
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*
D000962:Antimalarials; D037621:Artemisinins; D012717:Sesquiterpenes; D000077332:Artesunate; C514498:artemisone