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Mar. Drugs 2009, 7(4), 640-653; https://doi.org/10.3390/md7040640

Antiplasmodial Activities of Homogentisic Acid Derivative Protein Kinase Inhibitors Isolated from a Vanuatu Marine Sponge Pseudoceratina sp.

1
Laboratoire de Chimie, Université de la Nouvelle-Calédonie, BP R4, 98851 Nouméa cedex, New Caledonia
2
Laboratoire de Pharmacochimie des Substances Naturelles et Pharmacophores Redox, Université de Toulouse, UPS, UMR 152, 118, rte de Narbonne, F-31062 Toulouse cedex 9, France
3
Institut de Recherche pour le Développement (IRD); UMR 152, 118, rte de Narbonne, F-31062 Toulouse cedex 9, France
4
INSERM U609, Global Health Institute, Ecole Polytechnique Fédérale de Lausanne, CH-1015 Lausanne, Switzerland
5
Wellcome Centre for Molecular Parasitology, University of Glasgow, Glasgow G12 8TA, Scotland, UK
*
Author to whom correspondence should be addressed.
Received: 19 October 2009 / Revised: 17 November 2009 / Accepted: 23 November 2009 / Published: 23 November 2009
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Abstract

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 μM. This product was moderately active in vitro against a FcB1 P. falciparum strain (IC50 = 12 μM). 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. View Full-Text
Keywords: Pseudoceratina; Pfnek-1; homogentisic acid derivatives; Plasmodium falciparum Pseudoceratina; Pfnek-1; homogentisic acid derivatives; Plasmodium falciparum
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Lebouvier, N.; Jullian, V.; Desvignes, I.; Maurel, S.; Parenty, A.; Dorin-Semblat, D.; Doerig, C.; Sauvain, M.; Laurent, D. Antiplasmodial Activities of Homogentisic Acid Derivative Protein Kinase Inhibitors Isolated from a Vanuatu Marine Sponge Pseudoceratina sp.. Mar. Drugs 2009, 7, 640-653.

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