Cytotoxic metabolites from an Indonesian sponge Lendenfeldia sp.
Cytotoxic metabolites from an Indonesian sponge Lendenfeldia sp.
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DOI：
10.1021/np070337f
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发表时间：
2007-11-01
影响因子：
5.1
通讯作者：
Nagle, Dale G.
中科院分区：
文献类型：
--
作者：
Dai, Jingqiu;Liu, Yang;Nagle, Dale G.
印尼海绵脂质提取物抑制T47D乳腺肿瘤细胞缺氧诱导的缺氧诱导因子-1 （HIF-1）的激活。色谱分离得到新的取代萘二聚体1、新的呋喃脂体2和3个已知的均己二烷酯萜，3-5。化合物1和3-5抑制缺氧诱导的HIF-1激活（IC50值：0.64-6.9 μ M），但也降低T47D和MDA-MB- 231乳腺肿瘤细胞的活力。化合物4是最有效的，在NCI 60细胞系面板中显示出独特的肿瘤细胞系选择性。这些化合物的一般细胞毒性阻止了它们作为HIF-1抑制剂的进一步考虑。
The lipid extract of an Indonesian Lendenfeldia sp. sponge inhibited hypoxia-induced hypoxia-inducible factor-1 (HIF-1) activation in T47D breast tumor cells. Chromatographic separation yielded the new substituted naphthalene dimer 1, the new furanolipid 2, and three known homoscalarane sesterterpenes, 3-5. Compounds 1 and 3-5 inhibited hypoxia-induced HIF-1 activation (IC50 values: 0.64-6.9 mu M), but also reduced the viability of T47D and MDA-MB- 231 breast tumor cells. Compound 4 was the most potent and showed a unique tumor cell line selectivity in the NCI 60-cell line panel. The general cytotoxicity of these compounds precluded their further consideration as HIF-1 inhibitors.