Kayser O, Kiderlen AF, Brun R (2001): In vitro activity of aurones against Plasmodium falciparum strains K1 and NF54
Planta Med. 67: 718-721.
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 these compounds exhibited antiplasmodial activity in the micromolar range, determined as fifty percent-inhibitory concentrations (IC50). Drug activity was not associated with cytotoxicity for the mammalian tumor cell lines KB and SKMel (IC50 > 3.0 µM). The most active compound was 4,5,4'-triacetyl-3',5'-dimethoxy-2-aurone with IC50 values of 0.007 µM and 0.180 µM 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.