Killing of intraerythrocytic Plasmodium falciparum by lysosomotropic amino acid esters.

摘要: Esters of amino acids are known to penetrate into cells by simple diffusion. Subsequently, they hydrolyzed hydrolases release the parent acid. Due abundance in phagolysosomes, accumulate, there because rate influx and hydrolysis exceed acid efflux through specific carriers. The osmotic effect this accumulation results disruption organelles. This mechanism has been demonstrated be responsible for killing Leishmania amastigotes esters. In investigation, it is shown that all esters tested, including alcohol esters, N-acetyl some dipeptides, inhibit growth Plasmodium falciparum culture. Inhibition time-dependent and, cases, ring-stage parasites more sensitive than trophozoites. Similar findings with Leishmania, Glu, Leu, Met, Phe Trp toxic whereas Ala, Gly, His Ile much less noxious. caused acridine orange selectively accumulates phagolysosome-like food vacuole parasite, attesting ostensible destruction organelle lysis. toxicity probably associated part their ability cytosolic proteases. Since excess can also proteolysis, free on parasite was tested. Of 19 odd only three, namely Cys, Trp, were found at millimolar concentrations reasons possible discussed.