A UPLC coupled with post-column derivatization (PCD) and diode array detector (DAD) collecting biochemical reaction signal analysis technique (UPLC–PDC–DAD) was developed and applied to screen acetylcholinesterase (AChE) inhibitors, 1,1-diphenyl-2-picrylhydrazyl and 2,2ʹ-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) free radical scavengers in Huanglian Jiedu decoction (HLJDD) and its constituent herbs; The main active ingredients in the HLJDD were identified by UPLC–linear ion trap/orbitrap mass spectrometry; The twenty peaks showing obvious free radicals scavenging activity were mainly derived from Coptidis Rhizoma, Scutellariae Radix and Phellodendri Cortex in HLJDD. The five peaks in Coptidis Rhizoma and Phellodendri Cortex exhibiting strong AChE inhibition activity were identified as coptisine, epiberberine, jatrorrhizine, berberine and palmatine, respectively. Jatrorrhizine was found to possess radical scavenging and AchE inhibiting activities; The proposed UPLC–PCD–DAD method could identify rapidly and efficiently the different bioactivities of multiple components in complex matrixes and reveal the different mechanisms of the components in the treatment of some diseases.

开发了 UPLC 结合柱后衍生化 (PCD) 和二极管阵列检测器 (DAD) 收集生化反应信号分析技术 (UPLC-PDC-DAD) 并应用于筛选乙酰胆碱酯酶 (AChE) 抑制剂、1,1-二苯基-2黄连解毒汤（HLJDD）及其组成药材中的-苦基肼和2,2ʹ-azino-双（3-乙基苯并噻唑啉-6-磺酸）自由基清除剂；HLJDD 中的主要活性成分通过 UPLC-线性离子阱/轨道阱质谱进行鉴定；20个具有明显清除自由基活性的峰主要来源于黄连、黄芩和黄柏中的黄连。黄连和黄柏中的五个峰表现出强 AChE 抑制活性的物质分别被鉴定为黄连素、表小檗碱、药根碱、小檗碱和巴马汀。发现药根碱具有清除自由基和抑制 AchE 的活性；所提出的 UPLC-PCD-DAD 方法可以快速有效地识别复杂基质中多种成分的不同生物活性，并揭示这些成分在治疗某些疾病中的不同机制。