| 引用本文:郑琴，周欢，熊文海，王佳，胡鹏翼，杨明.芍药苷对乌头碱在Caco-2细胞模型上转运行为的影响研究[J].世界中医药,2015,10(03):. |
|
| 芍药苷对乌头碱在Caco-2细胞模型上转运行为的影响研究 |
| Effects of Paeoniflorin on Aconitine Transport Behavior in Caco-2 Cell Model |
| 投稿时间：2015-02-02 |
| DOI：10.3969/j.issn.1673-7202.2015.03.005 |
| 中文关键词: 乌头碱 Caco-2细胞 芍药苷 转运 配伍 P-gp抑制剂 |
| English Keywords:Aconitine Caco-2 Monolayer Model Paeoniflorin Transport Behavior P-gp inhibitor |
| 基金项目:国家自然科学基金项目(编号：81060347)；江西省教育厅科学技术研究项目（编号：GJJ08333） |
|
| 摘要点击次数: 1302 |
| 全文下载次数: 1378 |
| 中文摘要: |
| 目的：研究芍药苷对乌头碱在Caco-2细胞模型转运行为的影响。方法：以乌头碱累积转运量及表观渗透系数Papp值为指标，采用高效液相色谱法对乌头碱含量进行检测，考察不同浓度、不同孵育时间、不同方向乌头碱在Caco-2细胞上的转运行为，以及与芍药苷不同配伍后转运行为的变化，并考察P-gp抑制剂存在与否对乌头碱转运行为的影响。结果：乌头碱累积转运量与给药浓度、孵育时间呈正相关，不同浓度乌头碱Papp值均大于1×10-6cm·s-1，且保持恒定，无统计学意义，但外排作用明显强于吸收，外排比接近1.5。在P-gp抑制剂维拉帕米存在条件下乌头碱转运量显著增加。当乌头碱与芍药苷配伍比例为1∶60时，乌头碱转运量显著减小。结论：乌头碱为吸收良好的一类药物，以被动转运为主，但仍存在外排蛋白P-gp的参与。当芍药苷配伍乌头碱达到一定比例时，对乌头碱的肠吸收具有显著的抑制作用。 |
| English Summary: |
| To explore effects of Paeoniflorin on Aconitine transport behavior in CacCo-2 cell monolayer model. Methods: Bi-direction transport behaviors of Aconitine and effects of concentrations, incubation time on Aconitine transport behavior were studied on Caco-2 cell. The concentration of Aconitine was analyzed on a reverse-phase HPLC column, Papp value and total transport amount were calculated. The effect of P-gp inhibitor on Aconitine transport behavior was investigated as well. Results: The transport volume of Aconitine was correlated positively with the incubation time and drug concentration. There were no significant differences in the Papp value at the selected concentrations. Bi-directional transport studies on Aconitine showed that the ratio of permeability in the Basolateral to Apical direction is about 1.5 times that of the Apical to Basolateral direction. The Papp value of Aconitine was above 1×10-6 cm·s-1. The transport amount of Aconitine was significantly increased in the presence of Verapamil. The transport amount of Aconitine was significantly reduced, when the ratio of Aconitine and Paeoniflorin compatibility was 1∶60. Conclusion:The results suggested that Aconitine could be easily absorbed on the Caco-2 monolayer model by a passive transportation. However, efflux protein may also play an important role in the transport process. When the compatibility of Paeoniflorin and Aconitine reached a certain percentage, intestinal absorption of Aconitine would be reduced remarkably. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
