Rollinger Judith M, Ewelt Julia, Seger Christoph, Sturm Sonja, Ellmerer Ernst P, Stuppner Hermann
Institute of Pharmacy, Pharmacognosy, Leopold-Franzens University of Innsbruck, Austria.
Planta Med. 2005 Nov;71(11):1040-3. doi: 10.1055/s-2005-873130.
Looking for acetylcholinesterase (AChE) inhibiting compounds within the plant kingdom, we came across the triterpene alpha-onocerin, which has recently been described as the active principle (IC(50) of 5.2 microM) of Lycopodium clavatum L. In order to discover related terpenoid structures with similar AChE inhibitory activity, we investigated the roots of Ononis spinosa L. using Ellman's reagent in a microplate assay. No inhibitory effect could be measured, not even with the isolated alpha-onocerin (1), which is in contrast to previous findings. Bioassay-guided fractionation of L. clavatum resulted in the isolation of lyclavatol (2), showing a weak, but dose-dependent inhibitory effect on AChE. (1)H- and (13)C NMR shift assignments for 1 and 2 are presented and discussed.
为了在植物界寻找乙酰胆碱酯酶（AChE）抑制化合物，我们发现了三萜类化合物α-芒柄花素，它最近被描述为石松的活性成分（IC50为5.2微摩尔）。为了发现具有类似AChE抑制活性的相关萜类结构，我们在微孔板分析中使用埃尔曼试剂研究了棘豆的根。未检测到抑制作用，即使使用分离出的α-芒柄花素（1）也是如此，这与之前的研究结果相反。对石松进行生物测定导向的分级分离，得到了石松醇（2），它对AChE显示出微弱但剂量依赖性的抑制作用。本文给出并讨论了1和2的（1）H-和（13）C NMR化学位移归属。
