甘草苷和异甘草苷在Caco-2细胞单层模型中的肠吸收研究

doi:10.5246/jcps.2010.06.060

甘草苷和异甘草苷在Caco-2细胞单层模型中的肠吸收研究

张力勤, 黄应栋, 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:2010-08-07 修回日期:2010-10-15 出版日期:2010-11-30 发布日期:2010-11-30
通讯作者: 杨秀伟*

Intestinal permeability of liquiritin and isoliquiritin in the Caco-2 cell monolayer model

Li-Qin Zhang, Ying-Dong Huang, 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:2010-08-07 Revised:2010-10-15 Online:2010-11-30 Published:2010-11-30
Contact: Xiu-Wei Yang*

摘要/Abstract

摘要：

甘草苷和异甘草苷是中药甘草中的主要黄酮类成分, 前者归属为二氢黄酮类化合物, 后者归属为查耳酮类化合物。本文利用体外人源Caco-2细胞单层模型进行甘草苷和异甘草苷的肠吸收研究。通过双向转运研究, 对两个化合物在该模型的渗透性进行评价, 并借此预测其在人体的肠吸收机制。采用HPLC-UV方法测定化合物的浓度, 并计算相关渗透参数。甘草苷和异甘草苷的表观渗透系数分别为(5.40±0.16)×10^–7和(8.69±0.15)×10^–7 cm/s。虽然甘草苷和异甘草苷为两个不同类型的化合物, 但均为吸收较差的化合物, 吸收程度与糖基密切相关。从吸收时间、浓度依赖性上判断2个化合物主要吸收机制均为被动扩散。

关键词: 甘草苷, 异甘草苷, Caco-2细胞单层模型, 肠吸收

Abstract:

The intestinal permeability of two flavonoid compounds liquiritin (LQ) and isoliquiritin (ILQ) was investigated using the Caco-2 cell monolayer model. In order to evaluate the permeability and predict the absorption mechanism of the two compounds, the study on bidirectional permeability from the apical (AP) side to the basolateral (BL) side as well as from the BL side to the AP side was carried out. The determination was performed by HPLC-UV method. And the permeability parameters, especially the apparent permeability coefficients (Papp), were then calculated. The Papp values of LQ and ILQ are (5.40±0.16)×10^–7 and (8.69±0.15)×10^–7 cm/s, respectively. The results of time- and concentration-dependent transport experiments indicate that both LQ and ILQ are poor absorbed mainly through passive diffusion.

Key words: Liquiritin, Isoliquiritin, Caco-2 cell monolayer model, Intestinal permeability

中图分类号:

Supporting:

Foundation items: National New Drug R & D Program (Grant No. 2009ZX09301-010), National High Technology Program (Grant No. 2002AA2Z343C, 2004AA2Z3783) of China, and Ability Enhancing Project of National Science Fund for Talent Training in Basic Science (Grant No. J0830836).

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

张力勤, 黄应栋, 杨秀伟^*. 甘草苷和异甘草苷在Caco-2细胞单层模型中的肠吸收研究[J]. , DOI: 10.5246/jcps.2010.06.060.

Li-Qin Zhang, Ying-Dong Huang, Xiu-Wei Yang^*. Intestinal permeability of liquiritin and isoliquiritin in the Caco-2 cell monolayer model [J]. , DOI: 10.5246/jcps.2010.06.060.

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