GABAergic phthalide dimers from Angelica sinensis (Oliv.) diels
GABAergic phthalide dimers from Angelica sinensis (Oliv.) diels
复制标题
DOI：
10.1002/pca.937
复制
发表时间：
2006-11-01
影响因子：
3.3
通讯作者：
Pauli, Guido F.
中科院分区：
文献类型：
--
作者：
Deng, Shixin;Chen, Shao-Nong;Pauli, Guido F.
当归（Angelica sinensis（Oliv.）已显示Diels根（当归）表现出与GABA α受体的竞争性结合，表明存在GABA能配体。甲醇提取物的色谱分离导致两种GABA能二聚体邻苯二甲酸酯1和2的分离。通过一维和二维NMR、HRESIMS和HRESIMS-MS等波谱分析方法，确定Gelispirolide（1）为一个新的二聚体，由Z-Figustilide和Z-butylidenephthalide单元组成。通过与文献值的比较，确定化合物2为已知的二聚体，riligustilide。通过单晶X-射线衍射实验确定了它的二聚键和立体化学。发现二聚体1和2在体外GABA α受体结合试验中具有活性，IC 50值分别为29和24 μ m。版权所有（c）2006约翰威利父子有限公司。
The methanol extract of Angelica sinensis (Oliv.) Diels roots (Dang Gui) has been shown to exhibit competitive binding to the GABAa receptor, suggesting the presence of GABAergic ligands. Chromatographic fractionation of the methanol extract led to the isolation of two GABAergic dimeric plithalides 1 and 2. Gelispirolide (1) was elucidated as a new plithalide dimer composed of a Z-figustilide and a Z-butylidenephthalide unit on the basis of spectroscopic approaches including one- and two-dimensional NMR, HRESIMS and HRESIMS-MS. Compound 2 was identified as the known dimeric plithalide, riligustilide, by comparison of its spectroscopic data with literature values. Its dimeric linkage and stereochemistry were ascertained by a single crystal X-ray diffraction experiment. Both dimers 1 and 2 were found to be active in an in vitro GABAa receptor-binding assay with IC50 values of 29 and 24 mu m, respectively. Copyright (c) 2006 John Wiley & Sons, Ltd.