从肖特前胡中分离升麻素的高效方法开发及酶抑制活性评估

Development of an Efficient Protocol for Cimifugin Isolation from Peucedanum schottii and Evaluation of Enzyme Inhibitory Activity.

作者信息

Koziol Ewelina, Orhan Ilkay Erdogan, Senol F Sezer, Alipieva Kalina, Georgiev Milen, Skalicka-Woiniak Krystyna

出版信息

Nat Prod Commun. 2016 Aug;11(8):1107-1110.

Abstract

The dichloromethane (DCM) extract of the fruits of Peucedanwn schottii Besser. ex DC. (Apiaceae) was subjected to high-performance counter-current chromatography (HPCCC) for the efficient and fast separation (30 min) and isolation of cimifugin using an ethyl acetate: water (1:1 v/v, K= 1.01) system. The analytical scale-optimized separation was easily scaled to semi-preparative conditions. Cimifugin (11.25% yield, 96.5% purity) was isolated for the first time from P. schottii and characterized by NMR spectroscopy. Cimifugin and the crude DCM extract were evaluated using ELISA microtiter assays for their inhibitory potential against the cholinesterases (acetylcholinesterase - AChE and butyrylcholinesterase - BChE), and tyrosinase (TYR), which are key enzymes for the treatment of some neurodegenerative diseases, i.e. Alzheimer's and Parkinson's. The crude extract exhibited a weak inhibitory activity against-AChE, BChE, and TYR (4.2, 35.5, and 0% at 100 μg mL-1 and 10.3, 40.0, and 12.2% at 200 μg mL-1, respectively), while cimifugin displayed low to moderate inhibition towards AChE and BChE (3.1 and 21.6%, respectively) at 200 μg mL'.

摘要

对欧前胡（Peucedanwn schottii Besser. ex DC.，伞形科）果实的二氯甲烷（DCM）提取物进行了高效逆流色谱（HPCCC）分离，以乙酸乙酯：水（1:1 v/v，K = 1.01）体系高效快速地分离（30分钟）并分离出升麻素苷。分析规模优化后的分离很容易扩大到半制备规模。首次从欧前胡中分离出升麻素苷（产率11.25%，纯度96.5%），并通过核磁共振光谱进行了表征。使用酶联免疫吸附测定微量滴定法评估了升麻素苷和DCM粗提物对胆碱酯酶（乙酰胆碱酯酶 - AChE和丁酰胆碱酯酶 - BChE）以及酪氨酸酶（TYR）的抑制潜力，这些酶是治疗某些神经退行性疾病（即阿尔茨海默病和帕金森病）的关键酶。粗提物对AChE、BChE和TYR表现出较弱的抑制活性（在100 μg mL-1时分别为4.2%、35.5%和0%，在200 μg mL-1时分别为10.3%、40.0%和12.2%），而升麻素苷在200 μg mL-1时对AChE和BChE表现出低至中等程度的抑制（分别为3.1%和21.6%）。