Saccharide anions as inhibitors of the malaria parasite |
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Authors: | Diana L Clark Shidong Su Eugene A Davidson |
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Institution: | (1) Department of Biochemistry and Molecular Biology, Georgetown University, 3900 Reservoir Road, Washington, DC 20007, USA |
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Abstract: | The asexual erythrocytic stage of Plasmodium falciparum was grown in culture in the presence or absence of glycoconjugate
polyanions of varying structure, size and substitutions. Heparin, dextran sulfate, fucoidan and pentosan polysulfate had antimalarial
IC50 values between one and 11 μg ml−1. Constituent heparin disaccharides were ineffective against the malaria parasite and
desulfation from either the O- or N-substitution sites of heparin or reduction of the uronic acid carboxyl group neutralized
the antimalarial response to varying degrees. Immobilization of heparin onto agarose beads still permitted antimalarial activity
suggesting that parasite uptake of the glycoconjugate is not required for inhibition. Accordingly, it is concluded that invasion
of free parasites into the erythrocytes was inhibited rather than parasite maturation within the red cell. Merozoite surface
antigen-1 was apparently prevented from binding to human erythrocytes in the presence of highly sulfated polyanions and, in
a dose-dependent fashion, heparin. Abbreviations: MSA-1, merozoite surface antigen-1
This revised version was published online in November 2006 with corrections to the Cover Date. |
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Keywords: | glycoconjugate heparin malaria merozoite surface antigen-1 Plasmodium |
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