Zheng Xi-yuan, Zhang Zi-jia, Chou Gui-xin, Wu Tao, Cheng Xue-mei, Wang Chang-hong, Wang Zheng-tao
The MOE Key Laboratory for Standardization of Chinese Medicines and The SATCM Key Laboratory for New Resources and Quality Evaluation of Chinese Medicines, Institute of Chinese Materia Medica, Shanghai University of Traditional Chinese Medicine, 1200 Cailun Road, Shanghai, 201210, China.
Arch Pharm Res. 2009 Sep;32(9):1245-51. doi: 10.1007/s12272-009-1910-x. Epub 2009 Sep 26.
Acetylcholinesterase inhibitors (AChEIs) currently form the basis of the newest drugs available for the treatment of Alzheimer's disease. For the aim of screening effective AChEIs, the methanol extracts of the seeds of genus Peganum were found to show significant inhibitory activity of acetylcholinesterase enzyme (AChE) using an in vitro TLC-bioautographic assay. In further studies to seed of P. nigellastrum Bunge, activity-guided fractionation led to the isolation of two new alkaloids nigellastrine I (9) and nigellastrine II (10), and along with eight known alkaloids, vasicinone (1), vasicine (2), harmine (3), deoxyvasicinone (4), deoxyvasicine (5), harmaline (6), harmol (7), harman (8), in which harmol and harman were first isolated from species P. nigellastrum Bunge. As active constituents, all compounds showed good inhibitory activities against AChE. The results of in vitro semi-quality TLC-bioautographic assay showed that harmine, harmaline and harmol displayed a similar AChE inhibitive activities comparing to galanthamine. These results indicated that these alkaloids in P. nigellastrum Bunge could be a potent class of AChEIs.
乙酰胆碱酯酶抑制剂（AChEIs）目前构成了可用于治疗阿尔茨海默病的最新药物的基础。为了筛选有效的AChEIs，使用体外薄层色谱-生物自显影测定法发现骆驼蓬属种子的甲醇提取物对乙酰胆碱酯酶（AChE）显示出显著的抑制活性。在对黑种草种子的进一步研究中，活性导向分离得到了两种新生物碱黑种草碱I（9）和黑种草碱II（10），以及八种已知生物碱，鸭嘴花酮碱（1）、鸭嘴花碱（2）、去氢骆驼蓬碱（3）、去氧鸭嘴花酮碱（4）、去氧鸭嘴花碱（5）、骆驼蓬灵（6）、去氢骆驼蓬酚（7）、哈尔满（8），其中去氢骆驼蓬酚和哈尔满首次从黑种草中分离得到。作为活性成分，所有化合物对AChE均表现出良好的抑制活性。体外半定量薄层色谱-生物自显影测定结果表明，与加兰他敏相比，去氢骆驼蓬碱、骆驼蓬灵和去氢骆驼蓬酚表现出相似的AChE抑制活性。这些结果表明，黑种草中的这些生物碱可能是一类有效的AChEIs。
