两种方法测定灯盏花素经Caco-2细胞模型的转运  

Transport research of breviscapine across Caco-2 monolayer model using two assay methods

作　　者：齐云[1] 王敏[1] 蔡润兰[1] 谢忱[1] 王翔岩[1] 李晓红[1] 

机构地区：[1]中国医学科学院药用植物研究所,北京100193

出　　处：《中国药理学通报》2009年第6期831-833,共3页Chinese Pharmacological Bulletin

基　　金：国家自然科学基金资助项目(No30672659)

摘　　要：目的研究灯盏花素经Caco-2细胞模型转运的特性。方法用培养于Transwell上的Caco-2单层细胞模型研究灯盏花素双向转运;采用生物活性测定及HPLC的方法测定介质中灯盏花素或灯盏乙素的转运量。结果两种方法测定结果显示灯盏花素与灯盏乙素的双向转运Papp具有高度一致性,两者Papp(A-B)均小于1×10-6cm.s-1,流出率ER均大于2。结论采用生物活性法测定灯盏花素Papp具可行性。灯盏花素在Caco-2细胞单层吸收上存在明显外排,这可能是其生物利用度极低的重要原因。Aim To evaluate transport property of breviscapine across Caco-2 monolayer model by different assay methods. Methods The transwell filter inserts on culturing Caco-2 cell monolayers was used to observe breviscapine bidireetion transportation; bioactivity and HPLC approach were used to determine breviscapine and scutellarin in the receiver compartment. Results There was a good degree of concordance between breviscapine and seutellarin Papp values for apical（AP） to basolateral （BL） or BL to AP, both Papp values for AP-BL were less than 1×10^-6 cm·s^-1. The efflux rates of breviscapine and scutellarin were larger than 2. Conclusions It is feasible to determine Papp, of breviscapine by bioactivity assay method. Breviscapine is obviously secreted by Caco-2 cell monolayer, which is a possible important reason for low oral bioavailability of breviscapine.

关 键 词：灯盏花素 CACO-2细胞单层模型 表观通透系数 双 向转运 

分 类 号：R284.1[医药卫生—中药学] R329.2[医药卫生—中医学]