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来自澳大利亚海绵Psammoclema sp.的类固醇

Steroids from an Australian sponge Psammoclema sp.

作者信息

Holland Ian P, McCluskey Adam, Sakoff Jennette A, Gilbert Jayne, Chau Ngoc, Robinson Phillip J, Motti Cherie A, Wright Anthony D, van Altena Ian A

机构信息

Chemistry, School of Environmental and Life Sciences, The University of Newcastle, Callaghan, NSW 2308, Australia.

出版信息

J Nat Prod. 2009 Jan;72(1):102-6. doi: 10.1021/np800688f.

Abstract

Investigation of an extract of the Australian marine sponge Psammoclema sp. for dynamin I inhibitory activity led to the isolation of four new trihydroxysterols (1-4) related to aragusterol G. These compounds were largely identified by 1D and 2D NMR spectroscopic methods. While 1 was found to be inactive in the dynamin bioassay, bioassays did reveal that compounds 1-4 inhibited the growth of colorectal, breast, ovarian, and prostate cancer cell lines (GI(50) 5-27 microM). The additional insight that these new compounds give to previous SAR studies is discussed briefly.

摘要

对澳大利亚海洋海绵Psammoclema sp.提取物的动力蛋白I抑制活性进行研究,分离出了四种与aragusterol G相关的新三羟基甾醇(1-4)。这些化合物主要通过一维和二维核磁共振光谱法进行鉴定。虽然在动力蛋白生物测定中发现化合物1无活性,但生物测定确实表明化合物1-4能抑制结肠直肠癌、乳腺癌、卵巢癌和前列腺癌细胞系的生长(半数生长抑制浓度为5-27微摩尔)。简要讨论了这些新化合物为先前的构效关系研究提供的新见解。

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