体循环肠灌流法研究红禾麻提取物在类风湿性关节炎大鼠与正常大鼠体内的肠吸收差异  

Intestinal absorption difference of Laportea bulbifera extract in rats with rheumatoid arthritis and normal rats by in situ intestinal circulating perfusion model

作　　者：李莹 康宁芳 巩仔鹏[1] 陈思颖[1] 兰燕宇[1] LI Ying;KANG Ning-fang;GONG Zi-peng;CHEN Si-ying;LAN Yan-yu(Provincial Key Laboratory of Pharmaceutics in Guizhou,State Key Laboratory of Functions and Applications of Medicinal Plants,Guizhou Provincial Engineering Research Center for the Development and Application of Ethnic Medicine and TCM,School of Pharmacy,Guizhou Medical University,Guiyang 550004,China)

机构地区：[1]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民族药与中药开发应用教育部工程研究中心药学院

出　　处：《天然产物研究与开发》2019年第11期1896-1906,共11页Natural Product Research and Development

基　　金：国家自然科学基金(81560693、U1812403);贵州省民族药药效物质基础研究科技创新人才团队(黔科合平台人才[2016]5613);中央引导地方科技专项(黔科中引地[2018]4006)

摘　　要：比较红禾麻提取物在AA大鼠与正常大鼠体内的肠吸收差异。实验采用体循环肠灌流法,建立大鼠RA模型,应用UPLC-MS/MS检测肠灌流液中新绿原酸、绿原酸、隐绿原酸、芦丁、异槲皮苷、槲皮苷、山奈酚-3-O-芸香糖苷、木犀草苷的含量,探究各成分在不同因素(pH值、药物浓度、肠段、胆汁和P-gp抑制剂)下的肠吸收特性。结果表明,槲皮苷的吸收方式为主动转运,其余7个成分的吸收方式为被动扩散。除绿原酸、隐绿原酸外,正常状态下各成分以回肠吸收最好,病理状态下以十二指肠吸收最好,推测药物吸收的特定部位会受疾病状态的影响而发生改变。各成分的吸收均受pH、胆汁和P-gp的影响,其中,槲皮苷可能是P-gp的底物。RA能影响红禾麻提取物在大鼠体内的肠吸收,其作用机制尚需进一步研究。To compare the intestinal absorption characteristics of Laportea bulbifera extract in AA and normal rats.This experiment adopts the systemic intestinal perfusion method,set up big rats model of rheumatoid arthritis,application of UPLC-MS/MS detection of intestinal perfusion fluid in neochlorogenic acid,chlorogenic acid,cryptochlorogenic acid,rutin,isoquercetin,quercetin,kaempferol-3-O-rutinoside and galuteolin content,explore various components in the different factors(pHvalue,the concentration of the drug,the intestine,bile and P-gp inhibitors)under the intestinal absorption characteristics.The results showed that the absorption mode of quercetin was active transport,and the absorption mode of the other 7 components was passive diffusion.Except chlorogenic acid and cryptochlorogenic acid,the best absorption of each component was in ileum under normal condition and duodenum under pathological condition,so it was speculated that the specific sites of drug absorption would be affected by the disease.The absorption of each component is affected by pH,bile and p-gp,among which quercetin may be the substrate of p-gp.Rheumatoid arthritis can affect the intestinal absorption of Laportea bulbifera extract in rats,and its mechanism needs to be further studied.

关 键 词：红禾麻提取物 在体循环肠灌流法 类风湿性关节炎大鼠 肠吸收特性 

分 类 号：R945[医药卫生—微生物与生化药学]