白术内酯类在人源Caco-2细胞单层模型中的肠吸收研究

doi:10.5246/jcps.2011.05.064

白术内酯类在人源Caco-2细胞单层模型中的肠吸收研究

郭洁, 徐嵬, 杨秀伟^*

北京大学医学部天然药物及仿生药物国家重点实验室; 药学院天然药物学系, 北京 100191

收稿日期:2011-05-30 修回日期:2011-08-10 出版日期:2011-09-20 发布日期:2011-09-20
通讯作者: 杨秀伟*

Intestinal permeability of atractylenolides across the human Caco-2 cell monolayer model

Jie Guo, Wei Xu, Xiu-Wei Yang^*

State Key Laboratory of Natural and Biomimetic Drugs; Department of Natural Medicines, School of Pharmaceutical Sciences, Peking University Health Science Center, Beijing 100191, China

Received:2011-05-30 Revised:2011-08-10 Online:2011-09-20 Published:2011-09-20
Contact: Xiu-Wei Yang*

摘要/Abstract

摘要： 采用人源Caco-2细胞单层模型, 研究了倍半萜内酯类的白术内酯I、II和III的肠渗透性。研究了它们从顶端到基底侧以及从基底侧到顶端的双向渗透性。HPLC法测定其浓度。白术内酯I、II、III的Papp 值皆在10^-5 cm/s水平, 表明其具有高肠渗透率和良好吸收的特性。它们的双向转运具有时间和浓度依赖性, 提示其吸收转运的主要机制为被动扩散。此外, 白术内酯I的吸收转运可能部分存在主动转运机制。

关键词: 白术内酯I, 白术内酯II, 白术内酯III, Caco-2细胞单层模型, 肠吸收

Abstract:

The intestinal permeability of three sesquiterpene lactones, atractylenolide I, II, and III, was investigated using the human Caco-2 cell monolayer model. The bidirectional permeability of the three compounds from the apical (AP) to the basolateral (BL) side and in the reserved direction was studied. The three compounds were assayed using HPLC. The Papp values of atractylenolide I, II, and III were all at the level of 10^-5 cm/s, suggesting high intestinal permeability and good absorption. The bidirectional transport of the three compounds was time- and concentration-dependent, and indicated the main mechanism of the passive diffusion of the three compounds across the intestinal epithelium membrane. Moreover, atractylenolide I might be partly actively transported.

Key words: Atractylenolide I, Atractylenolide II, Atractylenolide III, Caco-2 cell monolayer model, Intestinal permeability

中图分类号:

Supporting:

Foundation item: "Major New Medicine Project" in National Science and Technology Major Project of China (Grant No. 2009ZX09301-010).

^*Corresponding author. Tel.: 86-10-82805106

郭洁, 徐嵬, 杨秀伟^*. 白术内酯类在人源Caco-2细胞单层模型中的肠吸收研究[J]. , DOI: 10.5246/jcps.2011.05.064.

Jie Guo, Wei Xu, Xiu-Wei Yang^* . Intestinal permeability of atractylenolides across the human Caco-2 cell monolayer model [J]. , DOI: 10.5246/jcps.2011.05.064.

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