Isolation of new phenylacetylingol derivatives that reactivate HIV-1 latency and a novel spirotriterpenoid from Euphorbia officinarum latex
Isolation of new phenylacetylingol derivatives that reactivate HIV-1 latency and a novel spirotriterpenoid from Euphorbia officinarum latex
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DOI：
10.1016/j.bmc.2007.04.009
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发表时间：
2007-07-01
影响因子：
3.5
通讯作者：
Collado, Isidro G.
中科院分区：
文献类型：
--
作者：
Daoubi, Mourad;Marquez, Nieves;Collado, Isidro G.
从大戟胶乳中分离得到3个新的官能化吲哚二萜化合物：7，8，12-三乙酸三乙酯-3-苯乙酸酯(1)，7，8，12-三乙酸酯-3-(4-甲氧基苯基)乙酸酯(2)和8-甲氧基吲哚-7，12-二乙酸酯-3-苯基乙酸酯(3)，以及新的螺三萜类化合物3S，4S，5R，7S，9R，14R-3，7-dihydroxy-4，14-dimethyl-7[8 9]-Abeo-Cholestan-8-one(4)。根据它们的波谱数据确定了它们的结构，包括二维核磁共振分析和NOE实验。分析了1-3对Jurkat T细胞系细胞周期和HIV-1基因转录的生物学效应。化合物3诱导细胞周期停滞和HIV-1-LTR启动子的激活，可能是一种新的先导化合物，可用于开发抗HIV-1潜伏疗法。(C)2007爱思唯尔有限公司。保留所有权利。
Three new, highly functionalized ingol diterpenes, ingol 7,8,12-triacetate 3-phenylacetate (1), ingol 7,8,12-triacetate 3-(4methoxyphenyl)acetate (2) and 8-methoxyingol 7,12-diacetate 3-phenylacetate (3), together with the novel spirotriterpene, 3S,4S,5R,7S,9R,14R-3,7-dihydroxy-4,14-dimethyl-7[8 9]-Abeo-cholestan-8-one (4), have been isolated from Euphorbia officinarum latex. Structures were established on the basis of their spectroscopic data, including two-dimensional NMR analysis and NOE experiments. The biological effects of 1-3 on cell cycle and HIV-1 gene transcription were analysed in the Jurkat T cell line. Compound 3 induced cell-cycle arrest and HIV-1-LTR promoter activation and could represent a novel lead compound for the development of therapies against HIV-1 latency. (c) 2007 Elsevier Ltd. All rights reserved.