title: Effect of calpain inhibitors on the invasion of human erythrocytes by the parasite Plasmodium falciparum.
abstract: 17 different proteinase inhibitors were screened for their effect on the erythrocyte invasion by the malaria parasite Plasmodium falciparum. The effect was tested when the inhibitors were present in the culture medium and when they were trapped into erythrocyte ghosts. A very strong inhibition of invasion was observed in the presence of calpain inhibitors, with IC50 in the order of 10(-7) M. Chymostatin, leupeptin, pepstatin A and bestatin also caused inhibition of the invasion, but with IC50 in the order of 10(-5) M. The results suggest that participation of various proteinases in the process and point to the possibility of a calpain-mediated proteolytic event. This study may explain previous observations on the role of calcium in the invasion of the human erythrocyte by Plasmodium falciparum.
authors.affiliation: Department of Biochemistry, Instituto Nacional de Salud, Bogotá, Colombia.
authors.forename: P
authors.initials: P
authors.lastname: Olaya
authors.forename: M
authors.initials: M
authors.lastname: Wasserman
mesh_terms: D000818:Animals; D002154:Calpain / Q000037:antagonists & inhibitors*; D015853:Cysteine Proteinase Inhibitors / Q000494:pharmacology*; D004912:Erythrocytes / Q000187:drug effects* / Q000201:enzymology / Q000469:parasitology; D006801:Humans; D007930:Leucine / Q000031:analogs & derivatives / Q000494:pharmacology; D007976:Leupeptins / Q000494:pharmacology; D009842:Oligopeptides / Q000494:pharmacology; D010436:Pepstatins / Q000494:pharmacology; D010963:Plasmodium falciparum / Q000187:drug effects* / Q000201:enzymology
chemical_list: D015853:Cysteine Proteinase Inhibitors; D007976:Leupeptins; D009842:Oligopeptides; D010436:Pepstatins; C014195:Streptomyces pepsin inhibitor; C002101:chymostatin; D002154:Calpain; D007930:Leucine; C012211:ubenimex; C032854:leupeptin; C031375:pepstatin