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
Chemistry, School of Environmental and Life Sciences, The University of Newcastle, Callaghan, NSW 2308, Australia.
J Nat Prod. 2009 Jan;72(1):102-6. doi: 10.1021/np800688f.
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.
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。