Screening of Plasmodium falciparum iron superoxide dismutase inhibitors and accuracy of the SOD-assays.
In vitro evaluation of a chemical library of synthetic compounds using two consecutive assays has led to the discovery of fifteen compounds which have the ability to inhibit recombinant Plasmodium falciparum iron superoxide dismutase (PfSOD), suggested as a highly selective target for design of antiparasitic drugs. A large number of compounds were in fact excluded, because they were found to significantly interfere with the components of the assays, thus outlining the drawbacks relative to the use of standard SOD-assays for the research of compounds targeting SODs. The best of the selected compounds showed significant antimalarial activities against two strains of P. falciparum, including a strain moderately resistant to chloroquine.
Soulère
Laurent
L
UMR/CNRS 5068, Université Paul Sabatier, Toulouse, France.
Delplace
Patrick
P
Davioud-Charvet
Elisabeth
E
Py
Sandrine
S
Sergheraert
Christian
C
Périé
Jacques
J
Ricard
Isabelle
I
Hoffmann
Pascal
P
Dive
Daniel
D
D000818:Animals; D004791:Enzyme Inhibitors / Q000494:pharmacology*; D066298:In Vitro Techniques; D010963:Plasmodium falciparum / Q000201:enzymology*; D013482:Superoxide Dismutase / Q000037:antagonists & inhibitors* / Q000378:metabolism
D004791:Enzyme Inhibitors; D013482:Superoxide Dismutase