| 延胡索甲素和乙素的人源肠内菌丛生物转化及在人源Caco-2细胞单层模型的吸收转运 |
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| 引用本文： | 刘扬子,杨鑫宝,杨秀伟,姚春梅,冉丽,吴帅,徐嵬,刘建勋.延胡索甲素和乙素的人源肠内菌丛生物转化及在人源Caco-2细胞单层模型的吸收转运[J].中国中药杂志,2013,38(1):112-118. |
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| 作者姓名： | 刘扬子 杨鑫宝 杨秀伟 姚春梅 冉丽 吴帅 徐嵬 刘建勋 |
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| 作者单位： | 1. 北京大学药学院天然药物学系,天然药物及仿生药物国家重点实验室,北京100191
2. 北京中医药大学,北京100102;中国中医科学院西苑医院,北京100091 |
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| 基金项目： | 国家科技支撑计划项目(2012BAI29B02,2011BAI07B00);国家"重大新药创制"科技重大专项(2009ZX09301-005-028);国家自然科学基金重点项目(30830118) |
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| 摘 要： | 目的:研究延胡索甲素(d-corydaline,CDL)和延胡索乙素(tetrahydropalmatine,THP)的人源肠内菌丛生物转化,在入源结肠腺癌细胞系Caco-2细胞单层模型的吸收转运.方法:应用人源肠内菌丛在厌氧、37℃条件下分别与CDL和THP共温孵培养;利用人源结肠腺癌细胞系Caco-2细胞单层模型测试CDL和THP从绒毛面(AP端)到基底面(BL端)、BL端到AP端双向的转运过程.计算转运参数和表观渗透系数(Papp),并与吸收良好的阳性对照药普萘洛尔和吸收不良的阿替洛尔进行比较.应用高效液相色谱法对CDL和THP进行分析.结果:CDL和THP在人源肠内菌丛温孵体系没有发生生物转化.它们与普萘洛尔在Caco-2细胞单层模型双向转运的Papp皆在1×10-5cm·s-1数量级;在0～ 180 min,转运效率与转运时间呈正相关.结论:CDL和THP在人源肠内菌丛温孵体系中稳定;在Caco-2细胞单层模型的转运机制可能为被动扩散.
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| 关 键 词： | 延胡索 延胡索甲素 延胡索乙素 人源肠内菌丛 人源Caco-2细胞单层模型 吸收转运 |
| 收稿时间： | 2012/9/29 0:00:00 |
Biotransformation by human intestinal flora and absorption-transportation characteristic in a model of Caco-2 cell monolayer of d-corydaline and tetrahydropalmatine |
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| LIU Yang-zi,YANG Xin-bao,YANG Xiu-wei,YAO Chun-mei,RAN Li,WU Shuai,XU Wei and LIU Jian-xun.Biotransformation by human intestinal flora and absorption-transportation characteristic in a model of Caco-2 cell monolayer of d-corydaline and tetrahydropalmatine[J].China Journal of Chinese Materia Medica,2013,38(1):112-118. |
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| Authors: | LIU Yang-zi YANG Xin-bao YANG Xiu-wei YAO Chun-mei RAN Li WU Shuai XU Wei and LIU Jian-xun |
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| Affiliation: | Department of Natural Medicines, School of Pharmaceutical Sciences, State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China;Beijing University of Chinese Medicines, Beijing 100102, China;Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing 100091, China;Department of Natural Medicines, School of Pharmaceutical Sciences, State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China;Department of Natural Medicines, School of Pharmaceutical Sciences, State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China;Department of Natural Medicines, School of Pharmaceutical Sciences, State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China;Department of Natural Medicines, School of Pharmaceutical Sciences, State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China;Department of Natural Medicines, School of Pharmaceutical Sciences, State Key Laboratory of Natural and Biomimetic Drugs, Peking University, Beijing 100191, China;Beijing University of Chinese Medicines, Beijing 100102, China;Xiyuan Hospital, China Academy of Chinese Medical Sciences, Beijing 100091, China |
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| Abstract: | |
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| Keywords: | Corydalis yanhusuo d-corydaline tetrahydropalmatine human intestinal flora human Caco-2 cell monolayer absorption and transportation |
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