杨文宁 韩星 杨海洋 李雪岩 刘洋 林瑞超

摘要 目的：基于中药多成分作用特点，探讨秦艽多成分在体内的代谢情况，遴选秦艽质控成分。方法：制备秦艽水提物，采用相应的实验操作手术，收集秦艽的肠代谢、肝代谢以及综合代谢样品，结合超高效液相色谱-四级杆/静电场高分辨质谱联用技术（UPLC-Q-Exactive MS），对秦艽水提物、肠代谢样品、肝代谢样品及综合代谢样品中的成分进行鉴别，遴选秦艽的质控成分。结果：秦艽水提物中共鉴定出33个化学成分，其中有12个成分在经肠代谢样品中可检测到，有9个成分在先经肠代谢后经肝代谢样品中可检测到，有11个成分在经灌胃给药后的综合代谢样品中检测到。结论：根据质谱数据分析结果，遴选出秦艽中9个可以以原型的形式进入血液循环的成分作为该药材的质控成分，包括马钱苷酸、secologanoside、6′-O-β-葡萄糖龙胆苦苷、獐牙菜苦苷、龙胆苦苷、獐牙菜苷、异牡荆素、淫羊藿苷、齐墩果酸，作为秦艽的质控成分。

关键词 秦艽;多成分药物代谢;质控成分;质量控制;超高效液相色谱-质谱联用技术（UPLC-MS/MS）

Abstract Objective：To investigate the metabolism of Radix Gentianae Macrophyllae and to select the quality control components of Radix Gentianae Macrophyllae based on the action features of multicomponent of Chinese medicines.Methods：The water extract of Radix Gentiana Macrophylla was prepared.Corresponding experimental operations was used.Gentiana macrophylla samples were collected for intestinal metabolism，hepatic metabolism and comprehensive metabolism of Radix Gentianae Macrophyllae，combined with ultra-high performance liquid chromatography-quadrupole/electrostatic field high-resolution mass spectrometry（UPLC-Q-Exactive MS）.The components in the water extract，intestinal metabolism sample，liver metabolism sample and comprehensive metabolism sample were identified，and the quality control components of Gentiana macrophylla were selected.Results：A total of 33 chemical constituents were identified in the water extract，of which 12 components could be detected after intestinal metabolism samples，9 components could be detected after intestinal metabolism followed by liver metabolism，and 11 components could be detected in comprehensive metabolic samples after intragastric administration.Conclusion：According to the results of MS data analysis，9 prototypes that can enter the blood circulation in the form of a prototype can be used as the quality control component of the medicinal material，and they were selected as quality control components of Radix Gentiana Macrophylla，including loganic acid，secologanoside，6′-O-β-D-glucosyl-gentiopicroside，swertiamarine，gentiopicroside，sweroside，isovitexin，icariin and oleanolic acid.

Keywords Radix Gentianae Macrophyllae; Multicomponent drug metabolism; Quality control ingredients; Quality control; UPLC-MS/MS（R）

中圖分类号：R284.1文献标识码：Adoi：10.3969/j.issn.1673-7202.2020.13.009

秦艽药材主产于中国西北地区，为龙胆科植物秦艽Gentiana macrophylla Pall.、麻花秦艽Gentiana straminea Maxim.、粗茎秦艽Gentiana crassicaulis Duthie ex Burk.和小秦艽Gentiana dahurica Fisch.的干燥根。在2015年版的《中华人民共和国药典》中，以龙胆苦苷和马钱苷酸作为秦艽药材含量测定的质控标准[1]。然而，秦艽中含有环烯醚萜苷类、黄酮类及三萜类等多类化学成分[2]，仅仅以这2个指标性成分作为质控无法全面评定药材的质量。……