红景天苷在大鼠体内的代谢途径研究  

Study on metabolic pathways of salidroside in rats

作　　者：周宇 刘延平[2] 武丽南[2] 谷元[2] 魏广力[2] 李全胜[2] 夏媛媛[2] 刘万卉[1] 司端运[2] ZHOU Yu;LIU Yan-ping;WU Li-nan;GU Yuan;WEI Guang-li;LI Quan-sheng;XIA Yuan-yuan;LIU Wan-hui;SI Duan-yun(Yantai University, Yantai 264003, China;State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, Tianjin 300193, China)

机构地区：[1]烟台大学,山东烟台264003 [2]天津药物研究院释药技术与药代动力学国家重点实验室,天津300193

出　　处：《中草药》2018年第7期1603-1611,共9页Chinese Traditional and Herbal Drugs

基　　金：国家自然科学基金青年科学基金项目(81503154)

摘　　要：目的研究红景天苷在大鼠体内的代谢物谱,分析其代谢途径。方法大鼠ig给予红景天苷200 mg/kg后,收集胆汁、尿液、粪便和血浆,应用高分辨质谱技术鉴定可能的代谢产物,分析红景天苷在大鼠体内的代谢途径。结果共检测到除原型药物外的20个代谢产物,提示红景天苷在大鼠体内的主要代谢途径为葡萄糖化、乙酰化、硫酸化和甲基化。结论红景天苷在大鼠体内经历了广泛的Ⅰ相和Ⅱ相代谢,代谢物主要通过尿液排出。应用峰面积归一化法计算主要代谢产物相对生成量,提示红景天苷在大鼠尿、粪、胆汁中的主要代谢途径为Ⅱ相代谢,血浆中红景天苷原型药物为体循环系统中主要暴露物质。Objective To analyze the metabolic pathways of salidroside when gavaged to rats, and to identify its in vivo metabolites. Methods A UPLC-Q-TOF-MS method was established and applied to identify the metabolites of salidroside in bile, urine, feces, and plasma samples after ig administration of salidroside 200 mg/kg to rats. Results A total of 20 metabolites were characterized in rats. The dominant metabolic pathways of salidroside include glucuronidation, acetylation, sulfation, and methylation. Conclusion Salidroside undergoes extensive phases Ⅰ and Ⅱ metabolism in rats. The main excretion path is the phase Ⅱ conjugated metabolites via urine, feces, and bile. The parent drug of salidroside is the main exposure material in plasma.

关 键 词：红景天苷 代谢途径 代谢产物 UPLC-Q-TOF-MS 葡萄糖化 乙酰化 硫酸化 甲基化 

分 类 号：R285.5[医药卫生—中药学]