In vitro activity of aurones against Plasmodium falciparum strains K1 and NF54.
A series of naturally occurring aurones (e. g., Rubiaceae, Cyperaceae) was synthesized and tested for the ability to inhibit erythrocytic stages of Plasmodium falciparum strains in vitro. Some of the these compounds exhibited antiplasmodial activity in the micromol range, determined as fifty percent-inhibitory concentrations (IC(50)). Drug activity was not associated with cytotoxicity for the mammalian tumor cell lines KB and SKMel (IC(50) > 3.0 microM). The most active compound was 4,6,4'-triacetyl-3',5'-dimethoxy-2-aurone with IC(50) values of 0.007 microM and 0.18 microM for the P. falciparum strains K1 and NF54, respectively. Interestingly, the multiple drug-resistant P. falciparum strain K1 was more sensitive to tested aurones than the drug-susceptible strain NF54.
Kayser
O
O
Freie Universität Berlin, Institut für Pharmazie, Berlin, Germany. kayser@zedat.fu-berlin.de
Kiderlen
A F
AF
Brun
R
R
D000818:Animals; D000962:Antimalarials / Q000737:chemistry / Q000494:pharmacology*; D000981:Antiprotozoal Agents / Q000737:chemistry / Q000494:pharmacology*; D001572:Benzofurans / Q000737:chemistry / Q000494:pharmacology*; D004912:Erythrocytes / Q000187:drug effects / Q000469:parasitology; D006801:Humans; D066298:In Vitro Techniques; D020128:Inhibitory Concentration 50; D019684:Magnoliopsida; D016778:Malaria, Falciparum / Q000188:drug therapy; D015394:Molecular Structure; D008517:Phytotherapy; D028321:Plant Preparations / Q000494:pharmacology*; D010963:Plasmodium falciparum / Q000187:drug effects*; D013045:Species Specificity; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
D000962:Antimalarials; D000981:Antiprotozoal Agents; D001572:Benzofurans; D028321:Plant Preparations