Chloroquine resistance in Plasmodium falciparum is not reversed by BIBW-22, a compound reversing the multidrug resistance phenotype in mammalian cancer cells.
The pteridine derivative BIBW-22 (4-[N-(2-hydroxy-2-methyl-propyl)-ethanolamino]-2,7-bis(cis-2,6-di methyl-morpholino)-6-phenylpteridine), which had been developed for the treatment of multidrug-resistant cancer and binds to P-glycoprotein, was tested against chloroquine resistant Plasmodium falciparum strains in culture. Based on the result that BIBW-22 enhanced rather than lowered chloroquine resistance in vitro, it is concluded that chloroquine resistance in malaria parasites may not be mechanistically linked to the multidrug-resistant phenotype of chloroquine resistant P. falciparum.
Dieckmann-Schuppert
A
A
Zentrum für Hygiene und Medizinische Mikrobiologie, University of Marburg, Germany.
Bamberger
U
U
Schwarz
R T
RT
D000818:Animals; D002470:Cell Survival; D002738:Chloroquine / Q000494:pharmacology*; D004351:Drug Resistance; D008826:Microbial Sensitivity Tests; D009025:Morpholines / Q000494:pharmacology*; D010641:Phenotype; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000235:genetics; D014223:Triamterene / Q000031:analogs & derivatives* / Q000494:pharmacology; D014407:Tumor Cells, Cultured / Q000187:drug effects
D009025:Morpholines; C080982:BIBW 22; D002738:Chloroquine; D014223:Triamterene