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In vitro studies on the mechanism of action of two compounds with antiplasmodial activity: ellagic acid and 3,4,5-Trimethoxyphenyl(6?-O-Galloyl)-β-D-glucopyranoside

Dell'Agli, Mario, Parapini, Silvia, Basilico, Nicoletta, Verotta, Luisella, Taramelli, Donatella, Berry, Colin and Bosisio, Enrica 2003. In vitro studies on the mechanism of action of two compounds with antiplasmodial activity: ellagic acid and 3,4,5-Trimethoxyphenyl(6?-O-Galloyl)-β-D-glucopyranoside. Planta Medica 69 (2) , pp. 162-164. 10.1055/s-2003-37706

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Abstract

To investigate the mechanism of action of two antiplasmodial compounds, ellagic acid and 3,4,5-trimethoxyphenyl (6′-O-galloyl)-β-D-glucopyranoside (TMPGG), we studied in vitro two metabolic reactions of intraerythrocytic parasites: the activity of recombinant plasmepsin II, one of the haemoglobin proteases, and the detoxification of haematin into β-haematin. Both compounds inhibited plasmepsin II activity, but at concentrations ten-fold higher than those needed for inhibiting parasite growth. Moreover, ellagic acid inhibited the formation of β-haematin, with an IC50 only 3-fold higher than that of chloroquine. These data suggest that the antiplasmodial activity of ellagic acid could be related to the inhibition of β-haematin formation, whereas plasmepsin II does not represent the main target of the two compounds.

Item Type: Article
Date Type: Publication
Status: Published
Schools: Biosciences
Subjects: Q Science > Q Science (General)
Publisher: Thieme
ISSN: 0032-0943
Last Modified: 04 Jun 2017 06:47
URI: http://orca.cf.ac.uk/id/eprint/64813

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