| 引用本文: | 付达华，李妍，王二丽，郭素华.矢车菊黄素在Caco-2细胞模型中的吸收机制研究[J].中国现代应用药学,2011,28(12):1076-1080. |
| FU Dahua, LI Yan, WANG Erli, GUO Suhua.Transepithelial Transport of Centaureidin Across Caco-2 Cell Monolayers[J].Chin J Mod Appl Pharm(中国现代应用药学),2011,28(12):1076-1080. |
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| 摘要: |
| 目的 研究矢车菊黄素(centaureidin)在Caco-2细胞单层模型中的吸收机制。方法 以HPLC分析矢车菊黄素浓度，用Caco-2 细胞单层模型评价吸收时间、药物浓度、介质pH值、抑制剂等对矢车菊黄素吸收的影响，研究矢车菊黄素的吸收机制，计算表观渗透系数(apparent permeability coefficient, Papp)。结果 药物的吸收与药物浓度和吸收时间正相关；弱酸性介质条件下有利于药物的吸收；2,4-二硝基酚(DNP)对药物吸收无影响，但异博定(verapamil)可增加药物的吸收；从肠腔侧到基底侧的转运小于基底侧到肠腔侧的转运。结论 矢车菊黄素在Caco-2细胞模型中的吸收主要是被动转运，受P-糖蛋白的外排作用。 |
| 关键词: 矢车菊黄素 Caco-2细胞单层 跨膜转运 表观渗透系数 P-糖蛋白 |
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| 基金项目:福建省教育厅基金课题(JB10248) |
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| Transepithelial Transport of Centaureidin Across Caco-2 Cell Monolayers |
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FU Dahua, LI Yan, WANG Erli, GUO Suhua1,2
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1.Zhangzhou Health Vocational College, Zhangzhou 363000, China;2.Institute of Medical Biotechnology, Chinese Academy of Medical Sciences & Peking Union Medical College, Beijing 100050, China
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| Abstract: |
| OBJECTIVE To investigate the transepithelial transport of centaureidin across Caco-2 cell monolayers. METHODS The permeated amounts of centaureidin across Caco-2 cell momnolayers were measured by HPLC to calculate the permeation rate and the apparent permeability coefficient (Papp), based on the effect of absorption time, drug concentration, pH in apical side, and inhibitors, the Papp was determined. RESULTS Transport of centaureidin was concentration-dependent and time-dependent and nonsatuable. The acidic pH in apical side conduced to transepithelial transport of centaureidin. Though 2,4-dinitrophenol had no effect on transport of centaureidin, verapamil improved it. And the apical-to-basolateral Papp was less than the basolateral-to-apical Papp. CONCLUSION Transport of centaureidin across Caco-2 cell monolayers is via passive diffusion with efflux by P-glycoprotein. |
| Key words: centaureidin Caco-2 cell monolayers transport apparent permeability coefficient(Papp) P-glycoprotein |
