基于LC-IT-TOF-MS技术的龙血通络胶囊体内代谢研究  

Research on in vivo metabolites of Longxue Tongluo Capsules by liquid chromatography coupled with hybrid ion trap/time-of-flight mass spectrometry

作　　者：孙晶[1,2] 刘佳妮 李月婷 霍会霞[1] 许霞 夏晖 宋月林 张庆英 屠鹏飞[1,3] 李军[1] SUN Jing;LIU Jia-ni;LI Yue-ting;HUO Hui-xia;XU Xia;XIA Hui;SONG Yue-lin;ZHANG Qing-ying;TU Peng-fei;LI Jun(Modern Research Center for Traditional Chinese Medicine,School of Chinese Materia Medica,Beijing University of Chinese Medicine,Beijing 100029,China;Laboratory of Quality&Safety Risk Assessment on Agro-products Processing of the Ministry of Agriculture and Rural Affairs,Key Laboratory of Agricultural Product Quality and Safety Management and Control of the Ministry of Agriculture and Rural Affairs,Institute of Food Science and Technology,Chinese Academy of Agricultural Sciences,Beijing 100193,China;State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Peking University Health Science Center,Beijing 100191,China)

机构地区：[1]北京中医药大学中药学院中药现代研究中心,北京100029 [2]中国农业科学院农产品加工研究所农业农村部农产品加工质量安全风险评估实验室农业农村部农产品质量安全收贮运管控重点实验室,北京100193 [3]北京大学医学部药学院天然药物及仿生药物国家重点实验室,北京100191

出　　处：《中国中药杂志》2021年第18期4841-4848,共8页China Journal of Chinese Materia Medica

基　　金：国家重点研发计划项目(2018YFC1707905,2018YFC1707900);国家自然科学基金面上项目(81573572);中央级公益性科研院所基本科研业务费专项(Y2020XK24)。

摘　　要：龙血通络胶囊(Longxue Tongluo Capsules,LTC)临床上治疗缺血性脑中风恢复期血瘀证有很好疗效,其主要成分为龙血竭酚类提取物。该文在前期阐明了LTC主要酚类成分质谱裂解规律的基础上,采用LC-IT-TOF-MS对LTC主要药效成分龙血素A和龙血素C灌胃大鼠体内成分进行测定,分别鉴定了18个和55个代谢产物,初步阐明了其代谢途径。在此基础上,将LTC(500 mg·kg^(-1))灌胃SD大鼠,研究其在体内的血中移行成分,根据精确相对分子质量、特征碎片离子、对照品比对,结合课题组前期自建LTC化学成分数据库以及天然产物数据库,在给药大鼠血浆中共鉴定了18个原型成分和106个代谢产物,代谢产物主要以葡萄糖醛酸化、磺酸化、甲基化等形式为主,初步阐明了LTC主要成分在体内的血中移行成分,为进一步明确LTC的体内药效物质奠定了基础。Longxue Tongluo Capsules(LTC)has good efficacy against blood stasis syndrome during the recovery period of ischemic stroke.Its main active ingredient is the phenolic extract of Chinese dragon's blood.In our previous study,the primary mass fragmentation pathways of phenolic derivatives from LTC were clarified.Herein,the metabolites in rat plasma were characterized following the oral administration of loureirin A and loureirin C using liquid chromatography coupled with hybrid ion trap/time-of-flight mass spectro-metry(LC-IT-TOF-MS),with 18 and 55 metabolites identified,respectively.On this basis,with the help of the obtained accurate molecular weight,characteristic fragment ions,reference comparison,combined with LTC database and natural products database self-created in our group,18 prototypes and 106 metabolites were tentatively identified in rat plasma after oral gavage of LTC at a dose of 500 mg·kg^(-1).Glucuronidation,sulfonation,and methylation were major biotransformation pathways of LTC.This study preliminarily clarified the LTC constituents absorbed into blood and laid the foundation for clarifying the effective substances of LTC.

关 键 词：龙血通络胶囊 龙血竭 龙血素A 龙血素C LC-IT-TOF-MS 代谢产物 

分 类 号：R285[医药卫生—中药学]