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.
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 / M. Dell'Agli, S. Parapini, N. Basilico, L. Verotta, D. Taramelli, C. Berry, E. Bosisio. - In: PLANTA MEDICA. - ISSN 0032-0943. - 69:2(2003 Feb), pp. 162-164.
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
M. Dell'AgliPrimo
;S. ParapiniSecondo
;N. Basilico;L. Verotta;D. Taramelli;E. BosisioUltimo
2003
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.File | Dimensione | Formato | |
---|---|---|---|
s-2003-37706.pdf
accesso aperto
Tipologia:
Publisher's version/PDF
Dimensione
107.25 kB
Formato
Adobe PDF
|
107.25 kB | Adobe PDF | Visualizza/Apri |
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.