左旋紫草素肠道转运及Caco-2细胞转运特性  

Transport characteristics of L-shikonin in rat intestine and Caco-2 cells model

作　　者：高春艳[1] 聂珍贵[1] 梁翠茵[1] 王世全[1] 苏春梅[1] 陈岩[1] 杨红[1] 

机构地区：[1]首都医科大学燕京医学院,北京101300

出　　处：《中南药学》2014年第10期958-961,共4页Central South Pharmacy

摘　　要：目的研究左旋紫草素肠道及Caco-2细胞转运特征及其机制。方法应用翻转肠囊法和Caco-2细胞模型考察时间、浓度对左旋紫草素转运吸收特性的影响,应用P-糖蛋白抑制剂维拉帕米对左旋紫草素转运吸收机制进行研究,采用HPLC法测定左旋紫草素的浓度,计算其表观渗透系数(Papp)。结果在Caco-2细胞模型,随浓度增加和时间延长,左旋紫草素的累积转运量逐渐增加;加用维拉帕米后,使AP侧到BL侧的表观渗透系数Papp(AP→BL)显著增加,而从BL侧到AP侧的表观渗透系数Papp(BL→AP)显著降低。在翻转肠囊模型,100μmol·L-1左旋紫草素中加入维拉帕米后Papp显著增加。结论左旋紫草素的转运存在被动转运和主动转运2种形式,P糖蛋白参与主动转运过程;该药经肠道吸收中等,加入维拉帕米可能促进吸收。Objective To investigate the transport characteristics and the transport mechanism of L-shikonin in rat intestine and Caco-2 cell model. Methods The transport of L-shikonin was investigated through the time and concentration and dependence assay. The transport mechanism of L-shikonin was studied with the P-gp inhibitor of verapamil. The drug concentration of L-shikonin was determined by HPLC and the apparent permeability coeffi cient was calculated. Results The cumulative transport concentration of L-shikonin in Caco-2 cells was positively correlated with time and concentration. verapamil（100 μmol·L- 1） increased the Papp（ AP → BL）, and decreased the Papp（BL → AP） significantly. At 100 μmol·L- 1, the Papp was increased in the rat intestine model. Conclusion The absorption of L-shikonin in the Caco-2 cell model includes active and passive manner and effl ux transport, and P-gp may play an important role in the effl ux of L-shikonin in the Caco-2 cell. The absorption rate is moderate, verapamil may increase the absorption of L-shikonin.

关 键 词：左旋紫草素 转运特征 翻转肠囊法 CACO-2细胞模型 维拉帕米 

分 类 号：R965[医药卫生—药理学]