Absorption Mechanism of Dauricine based on Caco-2 Cell Line

GAO Xiu-rong1; JIANG Xue-hua2; DU Qing-qing2

doi:10.13422/j.cnki.syfjx.2012.15.049

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Absorption Mechanism of Dauricine based on Caco-2 Cell Line

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- Absorption Mechanism of Dauricine based on Caco-2 Cell Line
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 18, Issue 15, Pages: 139-143(2012)
- 作者机构：
  
  1. 成都医学院药学院药剂教研室
  2. 四川大学华西药学院临床药学与药事管理学系
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.2012.15.049
  CLC： R285.5
- Published：2012
- 稿件说明：
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[1]高秀蓉,蒋学华,杜青青.基于Caco-2细胞模型研究蝙蝠葛碱的跨膜吸收机制[J].中国实验方剂学杂志,2012,18(15):139-143.

GAO Xiu-rong1, JIANG Xue-hua2, DU Qing-qing2. Absorption Mechanism of Dauricine based on Caco-2 Cell Line[J]. Chinese journal of experimental traditional medical formulae, 2012, 18(15): 139-143.
[1]高秀蓉,蒋学华,杜青青.基于Caco-2细胞模型研究蝙蝠葛碱的跨膜吸收机制[J].中国实验方剂学杂志,2012,18(15):139-143. DOI： 10.13422/j.cnki.syfjx.2012.15.049.

GAO Xiu-rong1, JIANG Xue-hua2, DU Qing-qing2. Absorption Mechanism of Dauricine based on Caco-2 Cell Line[J]. Chinese journal of experimental traditional medical formulae, 2012, 18(15): 139-143. DOI： 10.13422/j.cnki.syfjx.2012.15.049.

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。

Abstract

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.

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Related Institution

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