甘蒙锦鸡儿中乙酰胆碱酯酶抑制剂的分离及结构鉴定

Separation of acetylcholine esterase inhibitor fromCaragana opulens and chemical structure identification

从传统中药甘蒙锦鸡儿(Caragana opulens)树皮中提取分离具有乙酰胆碱酯酶抑制活性的化合物.利用各种色谱法分离化学成分,然后通过理化性质和现代波谱技术鉴定其结构.得到的化合物采用薄层色谱生物自显影法初步筛选其乙酰胆碱酯酶抑制活性,再用改良的Ellman法进一步测定其对乙酰胆碱酯酶的抑制率.共分离得到7个化合物,分别鉴定为1,4-二(苯并恶唑-2-基)萘(1)、9,12,13-三羟基-10反式十八烯酸(2)、对羟基苯乙酮(3)、香草酸(4)、对羟基反式肉桂酸(5)、反式肉桂酸(6)、间羟基苯甲酸(7).其中化合物3能在薄层板上形成明显白斑,进一步测定其对乙酰胆碱酯酶抑制的IC50为1.4mmol/L,结果表明化合物3具有乙酰胆碱酯酶抑制活性.

Extraction and separation of compounds with acetylcholinesterase inhibitory activity from the peel of Caragana opulens were conducted.The chemical compositions of compounds were identified by chromatographic methods and their structures were identified by physciochemical and modern spectroscopy.Then,the AChE inhibitory activity and inhibitory rate was tested by using TLC bioautographic method and modified Ellman＇s colorimetric method,respectively.Seven compounds were separated and identified as（1）1,4-di（benzoxazol-2-yl）naphthalene,（2）pinellic acid,（3）p-hydroxy-acetophenone,（4）vanillic acid,（5）p-hydroxy-trans-cinnamic acid,（6）trans-cinnamic acid,（7）3-hydroxy benzoic acid.Compound #3 can form a white spot on the thin-layer board and its AChE inhibitory IC50 value is measured as1.4mmol/L,showing that the compound #3 has acetylcholinesterase inhibitory activity.