Caco-2细胞研究黄芪中活性成分毛蕊异黄酮的吸收转运  

Absorption and transportation of calycosin in Astragali Radix by using Caco-2 monolayer model

作　　者：周乐[1] 赵晓莉[1,2,3] 狄留庆[1,2,3] 

机构地区：[1]南京中医药大学药学院,江苏南京210046 [2]江苏省中药高效给药系统工程技术研究中心,江苏南京210046 [3]南京市中药微丸产业化工程技术研究中心,江苏南京210046

出　　处：《中国中药杂志》2014年第9期1709-1713,共5页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81102825;81073071;81273655);江苏省高校"青蓝工程"科技创新团队支持计划项目[苏教师(2008)30号];江苏省优势学科建设项目(YSXK-2010)

摘　　要：黄酮类成分是中药中一类重要的活性成分,其药理活性和体内过程是近些年研究的重点。毛蕊异黄酮是中药黄芪中黄酮类的主要活性成分,近些年的研究表明其具有多种药理活性,但在体内的吸收转运特性尚不明确。该实验运用Caco-2细胞模型,用芹菜素作为内标物质,采用高效液相法测定药物浓度的方法,分别研究不同浓度以及加入不同类型的蛋白抑制剂后的吸收转运特性。数据进行Q检验,结果表明毛蕊异黄酮低、中、高3种浓度的Papp(BL-AP)/Papp(AP-BL)=1.38<1.5,加入不同类型的蛋白抑制剂后,和空白组的Papp(BL-AP)/Papp(AP-BL)进行比较,均无显著性差异。说明毛蕊异黄酮的吸收可能主要以被动转运为主,同时有主动转运机制参与,其转运可能不受P-糖蛋白、MRP2蛋白、SGLT蛋白影响。Flavonoids are a class of important active ingredients in traditional Chinese medicine, pharmacological activity and in vivo process is the focus of research in recent years. Calycosin is the main active ingredients of flavonoids in Astragali Radix, recent studies indicate that it has many kinds of pharmacological activity, but the absorption and transport characteristics in vivo is unclear. The experiment using Caco-2 cell model, with apigenin as internal standard substance, using the method for the determination of drug concentration by HPLC, were studied at different concentrations and absorption transport characteristics of respectively adding different types of protein inhibitors. Data were analyzed by Q test, the results show that low, middle, high concentration of PappPapp（BL-AP）/Papp（AP-BL） = 1. 38 〈 1. 5, respectively adding different types of protein inhibitors, compared with the control group of Papp（BL-AP）/Papp（AP-BL）. there were no significant differences. Calycosin absorption may mainly passive transport, also involved in active transport mechanism, the transport may not be affected by the P-protein, MRP2 protein, SGLT protein.

关 键 词：CACO-2细胞 毛蕊异黄酮 吸收 转运 

分 类 号：R284[医药卫生—中药学]