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Saudiarabicains A-E, bioactive 19-acetoxyingol diterpenoids from Euphorbia saudiarabica
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2020-07-06 , DOI: 10.1016/j.tetlet.2020.152203
Abdullatif Bin Muhsinah , Alfarius Eko Nugroho , Huifang Li , Sarah Lazzaro , Nicholas A. DaSilva , Dongli Li , Hang Ma , Abdulrhman Alsayari , Hiroshi Morita , Yongqiang Liu , Navindra P. Seeram

Five new 19-acetoxyingols were isolated from the aerial parts of Euphorbia saudiarabica. They included two uncommon pentacyclic acetoxyingols (1, 2) and two 2,3-diepimers (3, 4), representing the first report of 19-acetoxyingols epimers. Their structures were determined by analysis of extensive 1D and 2D NMR spectroscopic data. The absolute configurations were established by experimental and calculated CD analysis. Compounds 35 showed α-glucosidase inhibitory effects superior to the positive control, acarbose (IC50 9.1, 8.0, 1.8 vs 147 µM, respectively). Compounds 1, 2, 4, and 5 showed inhibitory effects on human P-glycoprotein comparable to the positive control, valspodar (IC50 0.1–1.4 vs 0.2 µM, respectively).



中文翻译:

沙特阿拉伯(Saudiarabicains)AE,生物活性的19-乙酰氧基丁二萜,来自大戟

大戟大戟的地上部分中分离出五种新的19-乙酰氧基丁酚。它们包括两个非五环acetoxyingols(12)和两个2,3- diepimers(34),较19差向异构体acetoxyingols的第一份报告。通过分析广泛的1D和2D NMR光谱数据确定了它们的结构。通过实验和计算的CD分析来建立绝对构型。化合物3 - 5表明α葡萄糖苷酶优于阳性对照,阿卡波糖(IC抑制作用50分别9.1,8.0,1.8 VS 147μM)。化合物12图4和图5显示了对人P糖蛋白的抑制作用,与​​阳性对照valspodar相当(IC 50分别为0.1–1.4和0.2 µM)。

更新日期:2020-07-18
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