连翘叶抑制胆碱酯酶活性部位筛选

Screening of Inhibiting-cholinesterase Active Fractions from Forsythia Suspensa Leaves

关键词:  连翘叶  洗脱物  乙酰胆碱酯酶  丁酰胆碱酯酶  抑酶活性

Key words:  Forsythia suspensa leaves  separated parts  acetylcholinesterase  butyrylcholinesterase  inhibitory effects

摘要:

目的 筛选连翘叶中抑制胆碱酯酶活性的部位。方法 加热回流法制备连翘叶粗提物，再以不同浓度梯度的乙醇溶液过大孔树脂洗脱，制得5种洗脱物。用HPLC指认粗提物和各洗脱物中主要成分。Ellman法研究抑酶活性。结果 连翘叶粗提物对乙酰胆碱酯酶(acetylcholinesterase，AChE)的抑制效果明显好于丁酰胆碱酯酶(butyrylcholinesterase，BChE)；抑制AChE活性最佳部位为20%乙醇洗脱物；连翘苷和连翘脂素对AChE酶均表现出一定程度的促进作用，而连翘酯苷E和连翘酯苷I能够抑制AChE的活性。结论 连翘叶不同洗脱物抑制胆碱酯酶活性的作用与其主要成分对AChE酶活性的不同作用相关。

Abstract:

OBJECTIVE To screen the inhibiting-cholinesterase active fractions from Forsythia suspensa leaves.METHODS The crude extract of Forsythia suspensa leaves was prepared by heating reflux method,and then the macroporous resin with ethanol solution of different concentration gradient was used to prepare five kinds of separated parts.The main components in crude extract and separated parts were identified by HPLC.Ellman method was used to study the inhibitory effects on cholinesterase.RESULTS The inhibition effect of the crude extract from Forsythia suspensa leaves on acetylcholinesterase (AChE) was better than that of butyrylcholinesterase (BChE).The separated part in 20% ethanol showed the best ability to inhibit AChE activity.Phillyrin and phillygenin promoted the activity of AChE to a certain extent,while forsythoside E and forsythoside I inhibited the activity of AChE.CONCLUSION The inhibitory effects of separated parts of Forsythia suspensa leaves on cholinesterase was related to the different effects of its main components on AChE activity.