A study of the uptake of chloroquine in malaria-infected erythrocytes. High and low affinity uptake and the influence of glucose and its analogues.
A study of concentration- and substrate-dependence of chloroquine uptake has been carried out on mouse erythrocytes infected with the chloroquine-sensitive NK65 and the chloroquine-resistant RC strains of Plasmodium berghei. The presence of drug binding sites of high and low affinity in such strains of P. berghei was confirmed. High affinity uptake sites in cells parasitized with chloroquine-sensitive and chloroquine-resistant parasites have similar characteristics, but in the sensitive strain the major component of chloroquine-uptake is at high affinity and dependent on the availability of ATP whilst in the resistant strain the major component of uptake is at low affinity and independent of energy. An absolute increase in the quantity of the low affinity site in erythrocytes parasitized with chloroquine-resistant P. berghei was noted, which may be related to an increase in quantity of parasite membrane.
D019325:3-O-Methylglucose; D000818:Animals; D001665:Binding Sites / Q000187:drug effects; D002738:Chloroquine / Q000097:blood*; D003847:Deoxyglucose / Q000494:pharmacology; D004912:Erythrocytes / Q000378:metabolism*; D005947:Glucose / Q000031:analogs & derivatives* / Q000494:pharmacology*; D007773:Lactates / Q000097:blood; D019344:Lactic Acid; D008288:Malaria / Q000097:blood*; D008757:Methylglucosides / Q000494:pharmacology; D051379:Mice; D010962:Plasmodium berghei; D013237:Stereoisomerism; D013997:Time Factors
D007773:Lactates; D008757:Methylglucosides; D019325:3-O-Methylglucose; D019344:Lactic Acid; D002738:Chloroquine; D003847:Deoxyglucose; D005947:Glucose