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 ORCID: https://orcid.org/0000-0002-9943-548X 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:	27 Oct 2022 09:12
URI:	https://orca.cardiff.ac.uk/id/eprint/64813

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