%0 Journal Article
%9 ACL : Articles dans des revues avec comité de lecture répertoriées par l'AERES
%A Lebouvier, N.
%A Jullian, Valérie
%A Desvignes, I.
%A Maurel, S.
%A Parenty, A.
%A Dorin-Semblat, D.
%A Doerig, C.
%A Sauvain, Michel
%A Laurent, Dominique
%T Antiplasmodial activities of homogentisic acid derivative protein kinase inhibitors isolated from a Vanuatu marine sponge Pseudoceratina sp
%D 2009
%L fdi:010049155
%G ENG
%J Marine Drugs
%@ 1660-3397
%K Pseudoceratina ; Pfnek-1 ; homogentisic acid derivatives ; Plasmodium ; falciparum
%M ISI:000273042200013
%N 4
%P 640-653
%R 10.3390/md7040640
%U https://www.documentation.ird.fr/hor/fdi:010049155
%> https://www.documentation.ird.fr/intranet/publi/2010/01/010049155.pdf
%V 7
%W Horizon (IRD)
%X As part of our search for new antimalarial drugs in South Pacific marine sponges, we have looked for inhibitors of Pfnek-1, a specific protein kinase of Plasmodium falciparum. On the basis of promising activity in a preliminary screening, the ethanolic crude extract of a new species of Pseudoceratina collected in Vanuatu was selected for further investigation. A bioassay-guided fractionation led to the isolation of a derivative of homogentisic acid [methyl (2,4-dibromo-3,6-dihydroxyphenyl)acetate, 4a] which inhibited Pfnek-1 with an IC50 around 1.8 mu M. This product was moderately active in vitro against a FcB1 P. falciparum strain (IC50 = 12 mu M). From the same sponge, we isolated three known compounds [11,19-dideoxyfistularin-3 (1), 11-deoxyfistularin-3 (2) and dibromo-verongiaquinol (3)] which were inactive against Pfnek-1. Synthesis and biological evaluation of some derivatives of 4a are reported.
%$ 052 ; 035