Uptake of [3H] dihydroartemisinine by erythrocytes infected with Plasmodium falciparum in vitro.
Artemisinine ( qinghaosu ) was reduced and radio-labelled using tritiated borohydride. The tritiated dihydroartemisinine produced was differentially accumulated from low concentrations in culture medium into erythrocytes infected with Plasmodium falciparum. Uninfected erythrocytes concentrated the drug less than two-fold whereas infected erythrocytes achieved more than 300 times the medium concentration. The uptake process is reversible and saturable, with a dissociation constant (Kd) at the hypothetical receptor of 10.5 nmol.l-1. Competition studies indicate that the receptor is the same as that for artemether , another quinghaosu derivative. Chloroquine showed an interesting partial inhibition of uptake but was unable to release the bound radio-labelled drug from infected cells.
D000841:Anisomycin / Q000494:pharmacology; D000962:Antimalarials / Q000378:metabolism*; D000077549:Artemether; D037621:Artemisinins; D002738:Chloroquine / Q000494:pharmacology; D004912:Erythrocytes / Q000378:metabolism / Q000469:parasitology*; D006801:Humans; D010963:Plasmodium falciparum / Q000378:metabolism*; D011714:Pyrans / Q000494:pharmacology; D012717:Sesquiterpenes / Q000378:metabolism*
D000962:Antimalarials; D037621:Artemisinins; D011714:Pyrans; D012717:Sesquiterpenes; C039060:artenimol; D000841:Anisomycin; D002738:Chloroquine; D000077549:Artemether