Abstract
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 (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 4,6,4′-triacetyl-3′,5′-dimethoxy-2-aurone with IC50 values of 0.007 μM and 0.18 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.
Key words
Plasmodium falciparum
- malaria - aurones -
in vitro activity - antiplasmodial
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Dr. Oliver Kayser
Freie Universität Berlin
Institut für Pharmazie
Pharmazeutische Biotechnologie
Kelchstraße 31
12169 Berlin
Germany
Email: kayser@zedat.fu-berlin.de
Fax: +49-30-838 50605
Phone: Tel.: +49-30-838 50689
