New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia
New bioactive halenaquinone derivatives from South Pacific marine sponges of the genus Xestospongia
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DOI：
10.1016/j.bmc.2010.06.066
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发表时间：
2010-08-15
影响因子：
3.5
通讯作者：
Bourguet-Kondracki, Marie-Lise
中科院分区：
文献类型：
--
作者：
Longeon, Arlette;Copp, Brent R.;Bourguet-Kondracki, Marie-Lise
对南太平洋 Xestospongia 海绵进行生物测定指导分离，分离出许多海萘醌型聚酮化合物，包括两种新衍生物，名为 xestosaprol Cmethylacetal 7 和 orhalquinone 8。这两种新化合物的化学表征是通过广泛的 1D 和 2D NMR 光谱研究实现的。对该系列产品的抗磷脂酶 A(2)、抗法尼基转移酶和抗疟原虫活性进行了评价，并讨论了结构/活性关系。 Orhalquinone 8 对人和酵母法呢基转移酶均具有显着抑制作用，IC50 值为 0.40 muM，是恶性疟原虫的中度生长抑制剂。 (C) 2010 Elsevier Ltd. 保留所有权利。
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.