Caco—2细胞研究黄芪中活性成分毛蕊异黄酮的吸收转运

Caco—2细胞研究黄芪中活性成分毛蕊异黄酮的吸收转运
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）=1.381.5，则提示可能存在主动转运机制。

本实验Papp（BL-AP）/Papp（AP-BL）=1.38<1.5，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。

加入含P-糖蛋白抑制剂维拉帕米、MRP2蛋白抑制剂丙磺舒、SGLT 蛋白抑制剂甘露醇，各组与空白组比较均无显著性差异，进一步表明毛蕊异黄酮的转运可能不受P-糖蛋白、MRP2蛋白、SGLT蛋白影响。

近些年，毛蕊异黄酮的药理活性成为研究的热点，研究其吸收转运情况，有利于单体的开发应用，以及黄芪与其他药材配伍使用，起到协同增效提供一定的基础。

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ZHOU Le1，ZHAO Xiao-li1，2，3*，DI Liu-qing1，2，3*
（1.College of Pharmacy，Nanjing University of Chinese Medicine，Nanjing 210046，China；
2.Jiangsu Engineering Research Center for Efficient Delivery System of Traditional Chinese Medicine，Nanjing 210046，China；
3. Nanjing Engineering and Technology Research Center of Traditional Chinese Medicine Pellets，Nanjing 210046，China）
[Abstract] 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 Papp（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.
[Key words] Caco-2 model；calycosin；absorption；transportation
doi：10.4268/cjcmm20140932。