摘要
目的:研究蝙蝠葛碱在Caco-2细胞模型中的跨膜转运机制。方法:采用Caco-2细胞模型,进行A-B和B-A双向转运实验,计算表观渗透系数(Papp)、外排比率(ER)和累积转运量,考察蝙蝠葛碱不同质量浓度、细胞两侧pH梯度和螯合剂EGTA对蝙蝠葛碱转运的影响。结果:高、中、低浓度下的ER分别为1.11,4.49和7.24,即中、低浓度下转运有明显极化现象;顶侧pH 7.4和6.5时,ER值分别为3.95和9.38,即pH梯度存在时,蝙蝠葛碱吸收减少,外排增加;加入螯合剂EGTA后,Papp,ER和累积转运量均无显著改变。结论:蝙蝠葛碱的吸收有主动转运机制存在;pH梯度能驱动了蝙蝠葛碱的外排转运,偏碱性环境较酸性环境易于吸收;其吸收途径主要为跨细胞通道转运。
Objective： To investigate the absorption mechanism of dauricine based on Caco-2 cell line.Method： Bidirectional transport of dauricine in Caco-2 cell model was used;apparent permeability coefficients（Papp）,efflux ratio（ER） and accumulation transport amount were calculated;the effect of drug concentration,pH gradient and EGTA on the bidirectional transport of dauricine were studied.Result： At high,middle and low concentrations the efflux ratio（ER） was 1.11,4.49,7.24 respectively,so there was significant polar phenomenon for transport of dauricine;at apical lateral when pH was 7.4 and 6.5,ER were 3.95 and 9.38 respectively,so pH gradient could reduce the absorption of dauricine;chelator EGTA couldn＇t affect the Papp,ER and accumulation transport amount of dauricine.Conclusion： The active transport was included in the absorption mechanism of dauricine,pH gradient could increase the polar phenomenon,transmembrane pathway is the main absorption route for dauricine.
出处
《中国实验方剂学杂志》
CAS
北大核心
2012年第15期139-143,共5页
Chinese Journal of Experimental Traditional Medical Formulae
基金
成都医学院院级科研课题(CYZ09-008)
