| 蜕皮甾酮在Caco-2细胞模型中的摄取和跨膜转运研究 |
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| 引用本文： | 郑姣妮,龙潇鸿,邱峰,邱宗荫.蜕皮甾酮在Caco-2细胞模型中的摄取和跨膜转运研究[J].中国药理学通报,2009,25(4). |
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| 作者姓名： | 郑姣妮 龙潇鸿 邱峰 邱宗荫 |
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| 作者单位： | 1. 重庆医科大学,药学院,重庆,400016
2. 重庆医科大学,附属第一医院药剂科,重庆,400016 |
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| 基金项目： | 重庆市重大科技专项课题 |
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| 摘 要： | 目的以Caco-2细胞单层模型,首次研究了蜕皮甾酮的口服吸收与转运特性。方法采用普通Caco-2细胞模型、表达活性CYP3A4酶的Caco-2细胞模型,分别从AP→BL方向和BL→AP方向研究蜕皮甾酮的摄取和跨膜转运规律。结果蜕皮甾酮在2种模型中的表观渗透系数(Papp)在0.1×10-6～1×10-6cm.s-1之间,药物吸收情况为1%～10%;在4 h的实验过程中,4种浓度蜕皮甾酮的ER值均小于1.5。结论研究表明,蜕皮甾酮主要以被动扩散的方式被细胞摄取和转运,其跨膜转运特性未受到CYP3A4-介导机制的影响。
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| 关 键 词： | 蜕皮甾酮 Caco-2细胞模型 1α 25-二羟维生素D3 体外吸收 |
Transport and uptake of ecdysterone in Caco-2 cell monolayers |
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| ZHENG Jiao-ni,LONG Xiao-hong,QIU Feng,QIU Zong-yin.Transport and uptake of ecdysterone in Caco-2 cell monolayers[J].Chinese Pharmacological Bulletin,2009,25(4). |
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| Authors: | ZHENG Jiao-ni LONG Xiao-hong QIU Feng QIU Zong-yin |
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| Abstract: | Aim This study examined the uptake and transport of ecdysterone(EDS) using Caco-2 cell monolayers as a model of human intestinal mucosa.Methods Two kinds of Caco-2 cell monolayer model(Caco-2 cell monolayers;CYP3A4 expressing Caco-2 cell monolayers) were set up to study the uptake and transport of EDS.Results Compared bi-directional charaterizaton of Caco-2 cell,the apparent permeability coefficients(Papp) values of EDS were between 0.1×10-6 cm·s-1 and 1×10-6 cm·s-1.EDS absorption was 1%~10% for two kinds of Caco-2 models.The RPapp values were all less than 1.5 for 4 h.Conclusions The uptake and transport of EDS was a passive transcellular diffusion mechanism.Ecdysterone was not influenced by CYP3A4 mediate mechanism. |
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| Keywords: | ecdysterone Caco-2 cell monolayer 1α 25-dihydroxyvitamin D3 in vitro absorption |
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