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Planta Med 2001; 67(8): 718-721
DOI: 10.1055/s-2001-18356
Original Paper
Pharmacology
© Georg Thieme Verlag Stuttgart · New York

In Vitro Activity of Aurones against Plasmodium falciparum Strains K1 and NF54

Oliver Kayser1,*, Albrecht F. Kiderlen2 , Reto Brun3
  • 1 Freie Universität Berlin, Institut für Pharmazie, Berlin, Germany
  • 2 Robert Koch-Institut, Berlin, Germany
  • 3 Schweizerisches Tropeninstitut, Basel, Switzerland
Further Information

Publication History

October 20, 2000

March 4, 2001

Publication Date:
09 November 2001 (online)

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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