摘要
目的研究隐丹参酮在Caco-2细胞模型中的吸收机制。方法用Caco-2细胞单层模型研究隐丹参酮的双向转运,并考察时间、药物浓度及抑制剂对隐丹参酮吸收的影响。用高效液相色谱法检测药物浓度,计算其表观渗透系数。结果隐丹参酮在Caco-2细胞模型中,从单层细胞层顶端到基底端的转运大于基底端到顶端的转运,随时间和浓度的增加,药物吸收呈饱和趋势,且可被其结构类似物丹参酮IIA竞争性抑制。结论隐丹参酮在Caco-2细胞模型中的吸收主要是由载体介导的主动转运,且该主动转运的载体位于Caco-2细胞单层的顶端。
Objective to investigate the absorption mechanism of cryptotan- shinone by using Caco -2 monolayer model. Methods Caco -2 cell monolayer model was used to investigate the bi - directional transport of cryptotanshinone. The effect of time, drug concentration and inhibitors on the absorption of cryptotanshinone was studied. Drug concentration was measured by HPLC and the apparent permeability coefficients (Papp)were calculated. Results The apical to basolateral ( AB ) permeability ( Papp ) of cryptotanshinone was bigger than the basolateral to apical (BA) permeability (Papp). The absorption of cryptotanshinone could be of saturation and inhibited by tanshinone IIg. Conclusion The absorption of cryptotanshinone in Caco -2 cell model was an active transportation mediated by transporter, which mainly located in the apical side of Caco -2 cell monolayer.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2005年第4期268-271,共4页
The Chinese Journal of Clinical Pharmacology
基金
广州市重大项目--创新药物药理毒理评价研究技术平台资助项目(2003Z2-E4071)