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Titolo:
Experimental conditions for testing the inhibitory activity of chloroquineon the formation of beta-hematin
Autore:
Baelmans, R; Deharo, E; Munoz, V; Sauvain, M; Ginsburg, H;
Indirizzi:
Inst Rech Dev, La Paz, Bolivia Inst Rech Dev La Paz BoliviaInst Rech Dev, La Paz, Bolivia Inst Boliviano Biol Altura, La Paz, Bolivia Inst Boliviano Biol Altura LaPaz Bolivia Biol Altura, La Paz, Bolivia IRD, F-75480 Paris 10, France IRD Paris France 10IRD, F-75480 Paris 10, France Hebrew Univ Jerusalem, Inst Life Sci, Dept Biol Chem, IL-91904 Jerusalem, Israel Hebrew Univ Jerusalem Jerusalem Israel IL-91904 -91904 Jerusalem, Israel
Titolo Testata:
EXPERIMENTAL PARASITOLOGY
fascicolo: 4, volume: 96, anno: 2000,
pagine: 243 - 248
SICI:
0014-4894(200012)96:4<243:ECFTTI>2.0.ZU;2-#
Fonte:
ISI
Lingua:
ENG
Soggetto:
ANTIMALARIAL-DRUGS; HEME POLYMERIZATION;
Keywords:
antimalarial drugs; heme; beta-hematin; polymerization;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
7
Recensione:
Indirizzi per estratti:
Indirizzo: Deharo, E Inst Rech Dev, CP 9214, La Paz, Bolivia Inst Rech Dev CP 9214 LaPaz Bolivia CP 9214, La Paz, Bolivia
Citazione:
R. Baelmans et al., "Experimental conditions for testing the inhibitory activity of chloroquineon the formation of beta-hematin", EXP PARASIT, 96(4), 2000, pp. 243-248

Abstract

Some antimalarial drugs act by inhibiting the process of ferriprotoporphyrin IX polymerization which protects the parasite against the noxious effectof this product of host cell hemoglobin digestion. As the quest for new drugs with a similar mode of action continues, high-throughput screening methods are needed. We demonstrate herein that such a recently described screening technique (Basilico et al., J. Antimicrob. Chemoter. 42, 55-60, 1998) is considerably disturbed by certain ions. Thus, at the assay's pH 2.6, the phosphate ions are responsible for the inhibitory activity of chloroquine phosphate, rather than chloroquine itself. Using a combination of solubilitytests and Fourier transform infrared spectrometry we also show that two alternative methods using higher pH's are also prone to salt effects and demonstrate that these can be minimized by extensive washing of the product with DMSO. (C) 2000 Academic Press.

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Documento generato il 30/11/20 alle ore 19:12:30