Journal
BIOORGANIC & MEDICINAL CHEMISTRY
Volume 18, Issue 16, Pages 6006-6011Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.06.066
Keywords
Xestospongia; Marine sponge; Marine natural product; Halenaquinone; PLA(2) inhibitor; FTase inhibitor; Antiplasmodial compound
Funding
- Agence Fran aise de Developpement
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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 A(2), 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 mu M and was a moderate growth inhibitor of Plasmodium falciparum. (C) 2010 Elsevier Ltd. All rights reserved.
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