Correlation Engine 2.0
Clear Search sequence regions

Sizes of these terms reflect their relevance to your search.

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 IC(50) around 1.8 muM. This product was moderately active in vitro against a FcB1 P. falciparum strain (IC(50) = 12 muM). 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.


Nicolas Lebouvier, Valérie Jullian, Isabelle Desvignes, Séverine Maurel, Arnaud Parenty, Dominique Dorin-Semblat, Christian Doerig, Michel Sauvain, Dominique Laurent. Antiplasmodial activities of homogentisic acid derivative protein kinase inhibitors isolated from a Vanuatu marine sponge Pseudoceratina sp. Marine drugs. 2009;7(4):640-53

Expand section icon Mesh Tags

Expand section icon Substances

PMID: 20098604

View Full Text