HPLC-ESI-LTQ-Orbitrap分析芪归银方中黄酮成分体内代谢过程  

Metabolic Processes of Flavonoids in Qi-gui-yingranule(QGY) Based on HPLC-ESI-LTQ-Orbitrap

作　　者：于小杰[1,2] 岳贵娟 薛梦[1] 张娇[1] 刘明玉[1] 梁莉靖 刘湉[1] 马群[1] YU Xiao-jie YUE Gui-juan XUE Meng ZHANG Jiao LIU Ming-yu LIANG Li-jing LIU Tian MA Qun(School of Chinese Pharmacy, Beijing University of Chinese Medicine, Beijing 100102, China Pharmaceutical Department, First Hospital of Qinhuangdao, Qinghuangdao 066000, China)

机构地区：[1]北京中医药大学中药学院,北京100102 [2]秦皇岛市第一医院药学部,河北秦皇岛066000

出　　处：《质谱学报》2017年第1期116-126,共11页Journal of Chinese Mass Spectrometry Society

基　　金：科学技术部"重大新药创制"科技重大专项(2013ZX09102026)资助

摘　　要：为进一步明确芪归银方的药效物质基础,采用HPLC-ESI-LTQ-Orbitrap技术对大鼠灌胃芪归银方后血清中黄酮类活性成分进行表征,并通过鉴别其尿液及粪便中的代谢物对结果进行佐证。从含药血清中鉴定出8个黄酮类化合物,其中,芹菜素-6,8-二葡萄糖苷和芹菜素以原型入血,芒柄花素、木犀草素、毛蕊异黄酮、5,7,4′-三羟基黄酮醇-7-O-β-D-葡萄糖苷、木犀草素-7-O-葡萄糖苷、山奈酚-3-O-葡萄糖苷等6个化合物以Ⅱ相代谢产物入血;从尿液中鉴定出9个黄酮类成分,包括6个入血成分的相应代谢产物;从粪便中检出3个黄酮类化合物的原型形式,未检测到与入血成分相同的成分。实验结果显示,芪归银方中的黄酮类入血成分大部分是经肾脏代谢排出,这可为阐明芪归银方延缓耐药的药效物质基础提供依据。With the extensive use of the antibiotics,especially abuse,the serious problem of bacterial resistance has happened commonly in clinic,and the multi-drug resistant pseudomonas aeruginosa infection has always been the focus and difficulty in clinical anti-infection treatment.After years of clinical trials,it is confirmed that some traditional Chinese medicine have significant antibacterial effect,and can delay or reverse drugresistant in combination with antibiotics.Qi-gui-yin（QGY）,composing of five kinds oftraditional Chinese medicine（Astragalus,Angelica Lonicera,Artemisia apiacea,Polygonum cuspidatum）,is mainly used for the treatment of multi-drug resistant pseudomonas aeruginosa infection,and is certified to have significant synergistic antibacterial effect with imipenem and ceftazidime.Due to the complexity of chemical composition,pharmacodynamic material basis of QGY is not very clear.In order to futher clarify pharmacodynamic material basis of Qi-gui-yingranule（QGY）,HPLC-ESI-LTQ-Orbitrap was used to investigate flavonoids constitutes in serum,urine and feces of rats.In previous studies,the chemical compositions of QGY were analyzed by LC-ESI-MS/MS.By comparing the retention time,accurate molecular weight and MS/MS fragmentation with standards and related literatures,59 compounds were identified or tentatively characterized in QGY,including flavonoids,phenylpropanoid,anthraquinones,isoflavans,isoflavones,saponins and other compounds.Among them,there were 28 flavonoids with the most types,which suggested that the flavonoids were the major constituents of QGY,and would be the medicinal compositions in treatment of resistance bacterial infection.In this work,the metabolic processes of flavonoids in QGY were mainly studied.8flavonoids were identified from medicated serum.Among them,Apigenin-6,8-diC-glu and Apigenin passed into blood with original structure,while the orther 6compounds were phase Ⅱ metabolites（formononetin,calycosin,luteolin-7-O-glucoside,kaempferol-3-O-glrcoside,luteolin and 5,7,4�

关 键 词：芪归银方 黄酮类成分 代谢过程 HPLC-ESI-LTQ-Orbitrap 

分 类 号：O657.63[理学—分析化学]