New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia |
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| Authors: | Arlette Longeon Brent R. Copp Mélanie Roué Joëlle Dubois Alexis Valentin Sylvain Petek Cécile Debitus Marie-Lise Bourguet-Kondracki |
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| Affiliation: | 1. Laboratoire des Molécules de Communication et Adaptation des Micro-organismes, FRE 3206 CNRS, Muséum National d’Histoire Naturelle, 57 rue Cuvier (C.P. 54), 75005 Paris, France;2. Department of Chemistry, the University of Auckland, Private Bag 92019, Auckland, New Zealand;3. Institut de Chimie des Substances Naturelles, CNRS UPR 2301, Centre de Recherche de Gif, avenue de la Terrasse, 91198 Gif sur Yvette Cedex, France;4. Pharmacochimie des Substances Naturelles et Pharmacophores Redox, UMR 152 IRD-UPS, Université Paul Sabatier, Faculté de Pharmacie, 35 chemin des Maraîchers, 31062 Toulouse Cedex 4, France;5. Centre Polynésien de recherche sur la biodiversité insulaire, UMR 7138, B.P. 529, 98713 Papeete, Tahiti, Polynésie française, France |
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| Abstract: | Bioassay-directed fractionation of South Pacific marine sponges of the genus Xestospongia has led to the isolation of a number of halenaquinone-type polyketides, including two new derivatives named xestosaprol C methylacetal 7 and orhalquinone 8. Chemical characterization of these two new compounds was achieved by extensive 1D and 2D NMR spectroscopic studies. Evaluation of anti-phospholipase A2, anti-farnesyltransferase and antiplasmodial activities of this series is presented and structure/activity relationships are discussed. Orhalquinone 8 displayed a significant inhibition of both human and yeast farnesyltransferase enzymes, with IC50 value of 0.40 μM and was a moderate growth inhibitor of Plasmodium falciparum. |
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