摘要
目的 研究葛根素在Caco-2细胞中的吸收特性。方法 改变药物浓度、实验温度和使用合适的抑制剂，测定葛根素在Caco-2细胞中的跨膜转运特性。结果 葛根素在Caco-2细胞的转运呈现较强的方向性，随着葛根素质量浓度的增加，其表观渗透率（PDR）降低（2．1～1．4）。随着温度升高PDR增大。当加入代谢抑制剂KCN和2，4-二硝基苯酚时，葛根素的PDR降低（由1．7分别降至1．0和1．2）。当加入100mg／L维拉帕米时，A面到B面的表观渗透系数Papp（A→B）从（0．84±0．18）×10^-7cm／s增加到（1．01±0．17）×10^-7cm／s，而B面到A面的Papp（B→A）从（1．43±0．18）×10^-7cm／s降低到（1．11±0．24）×10^-7cm／s。结论 葛根素在Caco-2细胞模型中的转运受到P-糖蛋白的外排作用。
Objective To study the uptaking characteristics of puerarin in Caco-2 model system. Methods The transepithelial transporting character of puerarin across Caco-2 cells was investigated by changing the concentration, temperature of drug and using appropriate inhibitors. Results The transport of puerarin across Caco-2 cell monolayers was directional. With the increase of the concentration of puerarin, the permeability direction ratio （PDR） was decreased from 2.1 to 1.4. With the increase of temperature, PDR was increased. When the metabolic inhibitors, KCN and 2,4-dinitrophenol, were added, the PDR was decreased from 1.7 to 1.0 and 1.2, respectively. When 100 mg/L Verapamil was added, the permeability coefficient of apical to basolateral was increased from （0. 84±0.18）× 10^-7 cm/s to （1.01± 0.17） × 10^-7 cm/s, and the permeability coefficient of basolateral to apical was decreased from （1.43 ± 0. 18） × 10^-7 cm/s to （1.11 ±0.24） ×10^-7 cm/s. Conclusion The evacuation by P-glycoprotein affects the puerarin transepithelial transport across Caco-2 cells.
出处
《中草药》
CAS
CSCD
北大核心
2007年第6期836-839,共4页
Chinese Traditional and Herbal Drugs
