Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, PR China.
J Chromatogr B Analyt Technol Biomed Life Sci. 2013 Sep 15;935:1-9. doi: 10.1016/j.jchromb.2013.07.015. Epub 2013 Jul 25.
Yuanhu Zhitong prescription (YZP) is well known for its analgesic effect. However, its multiple bioactive components in vivo remain unclear. In this paper, a rapid resolution liquid chromatography/quadrupole time-of-flight (RRLC-ESI-Q/TOF) was employed to identify the bioactive components and partial metabolites after oral administration of YZP extracts. Meanwhile, a RRLC-ESI-Q/TOF method was established and validated for the simultaneous quantification of protopine, α-allocryptopine, tetrahydropalmatine, corydaline, tetrahyberberine and byakangelicin in rat plasma and applied for their pharmacokinetic research. The results showed that twenty-one bioactive components of YZP were absorbed into the blood circulation and seventeen components were detected in cerebrospinal fluid (CSF). Moreover, the kinetic profiles of six analytes were obtained and the results suggested that the six analytes peaked between 3.5 and 5.0h and Cmax ranged from 214.6 to 858.3. The works could provide key information for identification of bioactive constituents and understanding the metabolism as well as pharmacological actions for YZP.
元胡止痛方（YZP）以其镇痛作用而闻名。然而，其体内的多种生物活性成分仍不清楚。在本文中，采用快速解析液相色谱/四极杆飞行时间（RRLC-ESI-Q/TOF）法鉴定了 YZP 提取物口服后的生物活性成分和部分代谢产物。同时，建立并验证了一种 RRLC-ESI-Q/TOF 方法，用于同时定量测定大鼠血浆中的原阿片碱、α-Allocryptopine、延胡索乙素、紫堇碱、四氢巴马汀和比克白芷素，并应用于其药代动力学研究。结果表明，YZP 的 21 种生物活性成分被吸收到血液循环中，在脑脊液（CSF）中检测到 17 种成分。此外，获得了六种分析物的动力学曲线，结果表明，六种分析物在 3.5 至 5.0 小时之间达到峰值，Cmax 范围为 214.6 至 858.3。该工作可为鉴定生物活性成分以及理解 YZP 的代谢和药理作用提供关键信息。
