首页|舒肝宁注射液及其方中黄芩提取物在大鼠肝微粒体、尿液、粪便、胆汁中的代谢比较研究

舒肝宁注射液及其方中黄芩提取物在大鼠肝微粒体、尿液、粪便、胆汁中的代谢比较研究

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比较舒肝宁注射液和黄芩提取物中黄芩苷及其类似物的代谢差异.12只SD大鼠随机分为舒肝宁注射液组和黄芩提取物组,每组6只,将肝微粒体与药物共孵育后收集样品,采用超高效液相色谱-四极杆-静电场轨道阱高分辨质谱法(UPLC-Q-Exactive Orbitrap-MS)分析肝微粒体中各组药物的原型成分与代谢产物.另取12只SD大鼠随机分为舒肝宁注射液组和黄芩提取物组,每组6只,尾静脉给予4.2 mL·kg-1的舒肝宁注射液或黄芩提取物,给药48 h后收集大鼠尿液、粪便和胆汁,采用UPLC-Q-Exactive Orbitrap-MS分析各生物样品中的原型及代谢产物.结果表明,舒肝宁注射液及黄芩提取物在肝微粒体中共鉴定出原型成分5个,代谢产物8个;在大鼠尿液、粪便和胆汁中均鉴定出5个原型成分,其中,在尿液中鉴定了15个代谢物,粪便中检测到9个代谢物,在胆汁中鉴定了12个代谢物.比较二者黄芩苷在代谢途径及代谢物数量上的差异,发现二者在肝微粒体、尿液、胆汁和粪便中葡萄糖醛酸化为黄芩苷和黄芩素的主要代谢途径,且存在部分甲基化产物及葡萄糖结合产物.舒肝宁注射液复方与黄芩提取物中,黄芩苷在尿样中代谢产物的数量和种类存在差异,表明二者在代谢上存在差异,说明中药成方中其余成分的存在会导致体内主要成分代谢产物发生变化.
Comparative study on metabolites in rat liver microsomes,urine,feces and bile between Shuganning Injection and Scutellariae Radix extract
This study aims to compare the metabolic differences of baicalin and its analogues between Shuganning Injection and Scutellariae Radix extract.Twelve SD rats were randomly divided into a Shuganning Injection group and a Scutellariae Radix extract group,with 6 rats in each group.Their liver microsomes were incubated with the drugs,and then the samples were collected.Ultra performance liquid chromatography-quadrupole/electrostatic field orbitrap high resolution mass spectrometry (UPLC-Q-Exactive Orbitrap-MS) was used to analyze the prototype components and metabolites of the drugs in liver microsomes of each group.Another 12 SD rats were also divided into a Shuganning Injection group and a Scutellariae Radix extract group,with 6 rats in each group.The rats were administrated with 4.2 mL·kg-1 Shuganning Injection or Scutellariae Radix extract by tail vein injection.After 48 h,the rat urine,feces,and bile were collected,and UPLC-Q-Exactive Orbitrap-MS was used to analyze the prototype components and metabolites in each biological sample.The results showed that 5 prototype components and 8 metabolites of Shuganning Injection and Scutellariae Radix extract were identified in liver microsomes.A total of 5 prototype components were identified in rat urine,feces,and bile separately.Fifteen metabolites were identified in the urine,9 metabolites in the feces,and 12 metabolites in the bile.The differences of metabolic pathways and number of metabolites of baicalin were compared between Shuganning Injection and Scutellariae Radix extract.For both Shuganning Injection and Scutellariae Radix extract,the metabolites of baicalin or baicalein in rat liver microsomes,urine,bile,and feces were mainly formed glucuronic acid conjugates,and there were a small amount of glucose conjugates and methylation products.Differences were found in the number and types of metabolites of baicalin in urine samples between Shuganning Injection and Scutellariae Radix extract,indicating that differences existed in metabolism between the two.This suggests that the other components in the formula lead to changes of metabolites in vivo.

Shuganning InjectionYinchenhao DecoctionScutellariae Radix extractUPLC-Q-Exactive Orbitrap-MSliver microsomesurinefecesbile

何峰、周杨、彭玥、郑林、王玲、黄勇、迟明艳

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贵州医科大学药学院,贵州贵阳 550004

贵州医科大学贵州省药物制剂重点实验室省部共建药用植物功效与利用国家重点实验室,贵州贵阳 550004

贵州医科大学民族药与中药开发应用教育部工程研究中心,贵州贵阳 550004

舒肝宁注射液 茵陈蒿汤 黄芩提取物 UPLC-Q-Exactive Orbitrap-MS 肝微粒体 尿液 粪便 胆汁

2024

中国中药杂志
中国药学会

中国中药杂志

CSTPCD北大核心
影响因子:1.718
ISSN:1001-5302
年,卷(期):2024.49(23)