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Antimicrobial Agents and Chemotherapy, October 2004, p. 4067-4071, Vol. 48, No. 10
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.10.4067-4071.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.

The Antiparasitic Compound Licochalcone A Is a Potent Echinocytogenic Agent That Modifies the Erythrocyte Membrane in the Concentration Range Where Antiplasmodial Activity Is Observed

Hanne L. Ziegler,1 Harald S. Hansen,2 Dan Stærk,1 Søren Brøgger Christensen,1 Henry Hägerstrand,3 and Jerzy W. Jaroszewski1*

Department of Medicinal Chemistry,1 Department of Pharmacology, The Danish University of Pharmaceutical Sciences, Copenhagen, Denmark,2 Department of Biology, Åbo Akademi University, Åbo/Turku, Finland3

Received 29 January 2004/ Returned for modification 8 March 2004/ Accepted 9 July 2004

The well-known antiparasitic compound licochalcone A is a potent membrane-active agent that transforms normal erythrocytes into echinocytes in parallel with the inhibition of growth of Plasmodium falciparum cultures, the in vitro antiplasmodial effect apparently being an indirect effect on the host cell. In vitro experiments with synchronous cultures demonstrate that inhibition of invasion is the principal mechanism of growth inhibition. The erythrocyte membrane-modifying effect was also transiently observed in vivo in mice after intravenous administration.

* Corresponding author. Mailing address: Department of Medicinal Chemistry, The Danish University of Pharmaceutical Sciences, Universitetsparken 2, DK-2100 Copenhagen, Denmark. Phone: 45-3530-6372. Fax: 45-3530-6040. E-mail: jj{at}dfuni.dk.

Antimicrobial Agents and Chemotherapy, October 2004, p. 4067-4071, Vol. 48, No. 10
0066-4804/04/$08.00+0     DOI: 10.1128/AAC.48.10.4067-4071.2004
Copyright © 2004, American Society for Microbiology. All Rights Reserved.



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