2-Deoxyglucose: inhibition of parasitemia and of glucosamine incorporation into glycosylated macromolecules, in malarial parasites (Plasmodium falciparum).
Cultured malarial parasites were incubated with various doses of 2-deoxyglucose (0.5, 1.0, 5.0, and 10.0 mM) for 48 h. Effects of 2-deoxyglucose on parasite survival were determined by counting the number of parasites/10,000 erythrocytes. Effects of 2-deoxyglucose on synthesis of membrane proteins and glycosylated macromolecules were monitored by metabolic labelling using radioactive isoleucine and glucosamine, respectively. 2-deoxyglucose significantly reduced parasite survival and synthesis of glycosylated macromolecules. Further incorporation of radioactive isoleucine was reduced at dose levels of 1.0, 5.0 and 10.0 mM. Inhibition of parasite survival was related closely to inhibition of incorporation of radioactive glucosamine into macromolecules. These results suggest that the antimalarial action of 2-deoxyglucose involves reduced synthesis of membrane glycosylated macromolecules by cultured parasites.
D000962:Antimalarials; D002462:Cell Membrane / Q000378:metabolism; D002478:Cells, Cultured; D003837:Deoxy Sugars / Q000494:pharmacology*; D003847:Deoxyglucose / Q000494:pharmacology*; D004912:Erythrocytes / Q000469:parasitology; D005944:Glucosamine / Q000378:metabolism*; D006801:Humans; D066298:In Vitro Techniques; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000378:metabolism; D014176:Protein Biosynthesis
D000962:Antimalarials; D003837:Deoxy Sugars; D003847:Deoxyglucose; D005944:Glucosamine