两种方法测定灯盏花素经Caco-2细胞模型的转运

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。

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

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 bidirection 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 scutellarin 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.