千层纸素A在Caco-2细胞模型中的吸收机制研究  

Absorption of oroxylin A across Caco-2 cell monolayer model

作　　者：冯志强[1] 谢智勇[1] 廖琼峰[2] 姚美村[1] 马燕[2] 张蕾[2] 

机构地区：[1]中山大学药学院,广州510006 [2]广州中医药大学,广州510006

出　　处：《中南药学》2011年第7期481-485,共5页Central South Pharmacy

基　　金：国家自然科学基金项目(No.30901953);国家教育部新教师基金项目(No.20094425120001);"重大新药创制"国家科技重大专项(No.2009ZX09304-003和2009ZX09501-017)

摘　　要：目的研究千层纸素A在Caco-2细胞模型中的吸收机制。方法 MTT实验考察千层纸素A在Caco-2细胞中的安全浓度范围,再利用Caco-2细胞单层模型研究千层纸素A的双向转运机制,以转运量及表观渗透系数(Papp)为指标,考察时间、浓度、pH和P-gp抑制药维拉帕米对其吸收的影响。结果千层纸素A在Caco-2细胞模型中的转运与时间和浓度呈正相关;并受pH值影响,P-gp抑制药维拉帕米对其转运无影响,从单层细胞层顶端(AP)到基底端(BL)的转运与基底端到顶端的转运大致相同。结论千层纸素A在Caco-2细胞模型中的吸收是被动转运。Objective To investigate the absorption mechanism of oroxylin A across Caco-2 cell monolayer model.Methods The safety concentration of oroxylin A in Caco-2 cell was first selected by MTT method.The Caco-2 cell monolayer drug transport model was assigned to study the bi-direction transport mechanism of oroxylin A by evaluating the influence factors such as time,concentration,pH,and P-gp inhibitor of verapamil on its absorption characterization.Results In the Caco-2 cell monolayer model,the transport volume was positively correlated with the time and concentration of oroxylin A,and affected by pH value.Verapamil had no influence on its transport since the transport of oroxylin A from apical to basolateral was similar to the transport from basolateral to apical.Conclusion The intestinal absorption mechanism of oroxylin A is deduced as passive transference by Caco-2 cell monolayer model.

关 键 词：千层纸素A CACO-2细胞模型 高效液相色谱 被动转运 

分 类 号：R966[医药卫生—药理学] R927.2[医药卫生—药学]