中文摘要：

发展了毛细管电泳（CE）和高效液相色谱-质谱（HPLC-MS）相结合的用于天然产物中活性成分筛选和鉴定的方法。该方法中，用HPLC半制备柱对天然产物粗提物进行分离纯化，再用CE对HPLC纯化后的绀分进行活性测试。根据HPLC-MS／MS提供的二级质谱数据，即可确定活性成分的化学结构。以乙酰胆碱酯酶为实验模型，对我们发展的筛选方法进行了验证。从黄连粗提物中确定了药根碱、巴马汀等7种活性成分，并通过CE测定了它们的半抑制率（IC50）值。与传统的天然产物分离纯化和活性筛选办法相比，该方法具有简译、微量、快速、准确的优点、本文建立的方法为天然产物粗提物中活性成分的筛选提供了新技术。

英文摘要：

A new strategy for screening the crude natural extracts and quickly identifying the bioactive compounds was developed. In combination with high performance liquid chromatog- raphy-mass spectrometry. （HPLC-MS）, the biologically active compounds, such as the enzyme inhibitors, in the crude natural extract can be quickly identified by capillary electrophoresis （CE）-based activity assay. The crude natural extracts were assayed by a CE-based enzyme inhibitor screening method, and the active extract was isolated by HPLC-MS/MS with a semi- preparative column, Then, each eluted component was assayed again with the CE-based assay method. Finally, the structures of the identified active compounds were elucidated by MS/MS analysis. Acetylcholinesterase （ ACHE）, its substrate acetylthiocholine chloride （AThCh）, as well as the crude extract of Rhizoma coptidis were utilized for the proof of the methodology. Seven isoquinoline alkaloids, namely jatrorrhizine, epiberberine, columbamine, coptisine, corysamine, palmatine and berberine were identified to be active as the inhibitors of ACHE. Their IC50, values were 40, 442, 38, 182, 419, 54 and 16 μmol/L, respectively. Compared with the traditional screening methods, the method is characterized with several advantages, such as extremely low sample and reagent consumption, high speed of analysis, high sensitivity of detection, high throughput in terms of preparation of the natural products by HPLC. Overall, the results demonstrate that the method is valuable for the screening of the bioactive com- pounds in the crude natural extracts.