In vitro activity of aurones against Plasmodium falciparum strains K1 and NF54

A series of naturally occurring aurones (e.g., Rubiaceae, Cyperaceae) was s ynthesized and tested for the ability to inhibit erythrocytic stages of Pla smodium falciparum, strains in vitro. Some of the these compounds exhibited antiplasmodial activity in the micromol range, determined as fifty percent -inhibitory concentrations (IC50). Drug activity was not associated with cy totoxicity for the mammalian tumor cell lines KB and SKMel (IC50 > 3.0 muM) . The most active compound was 4,6,4'-triacetyl-3',5' -dimethoxy-2-aurone w ith IC50 values of 0.007 muM and 0.18 muM for the P. falciparum strains K1 and NF54, respectively. Interestingly, the multiple drug-resistant P. falci parum strain K1 was more sensitive to tested aurones than the drug-suscepti ble strain NF54.