黄芪川芎主要有效成分配伍的转运研究  

The Transport Studies of the Main Effective Components of Astragalus Membranaceus and Rhizoma Chuanxiong

作　　者：周惠芬[1] 何昱[2] 张宇燕[1] 万海同[1] 戴柳玲 杨洁红 

机构地区：[1]浙江中医药大学心脑血管病研究所,浙江杭州310053 [2]浙江中医药大学药学院,浙江杭州310053

出　　处：《中华中医药学刊》2015年第4期868-871,共4页Chinese Archives of Traditional Chinese Medicine

基　　金：国家自然科学基金项目(81274176;81374053;81202636);浙江省自然科学基金项目(LR12H27001);浙江省中医药(中西医结合)重点学科项目(2012-XK-A06);浙江省教育厅科研项目(Y201329166);浙江中医药大学科研基金项目(2014ZY25)

摘　　要：目的：研究黄芪川芎中有效成分黄芪甲苷、川芎嗪、阿魏酸在Caco-2细胞模型中的正交配伍规律和吸收特性。方法：利用MTT实验研究有效成分在Caco-2细胞中的安全浓度,用Caco-2细胞模型研究黄芪甲苷、川芎嗪、阿魏酸正交配伍后的转运情况,采用高效液相色谱法进行含量测定。结果：在Caco-2细胞单层模型中,各有效成分的吸收转运Papp值皆〉1.0×10^-6cm·s^-1,推断它们配伍后皆为吸收良好的化合物。各有效成分的双向转运程度相近,这3个有效成分配伍后以被动扩散方式转运。3有效成分配伍后组2～8川芎嗪ER值和配伍后阿魏酸组4、6、7、9ER值〉2,川芎嗪与阿魏酸可能为P-gp的底物,组9川芎嗪和组2、8阿魏酸ER值介于1.5和2之间,要通过外加P-gp的抑制剂进行进一步的评价。结论：有效成分配伍后,药物之间的相互作用会改变吸收转运方式,配伍给药后对吸收有明显的促进作用。本研究为复杂的中药体系的活性物质配伍方法提供依据。Objective： To investigate the orthogonal compatibility rules and absorption characteristic of the effective components of Astragalus membranaceus and Rhizoma chuanxiong（ astragaloside,ligustrazine,ferulic acid） across Caco-2 cell model. Method： The safety concentrations of effective components in Caco-2 cell model were selected by the MTT method. The transportation of astragaloside,ligustrazine,ferulic acid orthogonal compatibility was investigated by Caco-2 cell monolayer model,and the drug concentrations were determined by high performance liquid chromatography（ HPLC）. Result： In the Caco-2 cell model,the Pappof all the effective components were more than 1. 0 × 10^-6cm·s^-1,which showed a good absorption. The situation of effective components bidirectional transfer were similar,and the three effective components were deduced as passive transport after orthogonal compatibility. The ER value of ligustrazine group 2 ～ 8 and ferulic acid group4,6,7,9 were over 2 after orthogonal compatibility,the compound may be P-gp substrate. The ER value of ligustrazine group 9 and ferulic acid group2,8 were between 1. 5 to 2,which needed to add P-gp inhibitors for further evaluation. Conclusion： After the effective components compatibility,the interaction between drugs will change the transport way,and have obvious promotive effect on absorption. This research provides the basis for complex traditional Chinese medicine system of active material compatibility.

关 键 词：黄芪甲苷 川芎嗪 阿魏酸 配伍 CACO-2细胞模型 转运 

分 类 号：R284[医药卫生—中药学]