| HPLC考察小檗碱和黄连提取物中小檗碱在Caco-2细胞模型的转运 |
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| 引用本文： | 吴安国,曾宝,王春玲,陈建南,赖小平.HPLC考察小檗碱和黄连提取物中小檗碱在Caco-2细胞模型的转运[J].中国药理学通报,2011,27(7):1007-1011. |
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| 作者姓名： | 吴安国 曾宝 王春玲 陈建南 赖小平 |
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| 作者单位： | 1. 广州中医药大学新药开发研究中心,广东,广州,510006
2. 广州中医药大学新药开发研究中心,广东,广州,510006;东莞广州中医药大学中医药数理工程研究院,广东,东莞,523808 |
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| 基金项目： | 国家科技支撑计划资助项目 |
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| 摘 要： | 目的同时考察小檗碱和黄连提取物中小檗碱在Ca-co-2细胞模型的转运。方法以Caco-2细胞单层模型研究药物的双向转运,首先系统考察时间、药物浓度、抑制剂、pH、温度对小檗碱单体吸收转运的影响,然后比较相同浓度的小檗碱单体与黄连提取物中的小檗碱在Caco-2细胞模型的转运差异。运用高效液相色谱法检测药物浓度,计算其表观渗透系数。结果相同浓度的小檗碱从底端(BL)到顶端(AP)的转运量大于顶端(AP)到底端(BL)的转运量,在AP→BP和BP→AP方向,其转运量随时间呈增长趋势。维拉帕米可以明显降低其在BL→AP方向的转运量;在AP→BL方向,其在pH=5的HBSS中的转运量最大;在BL→AP方向的转运对温度有较高的依赖性。在AP→BL和BL→AP方向,提取物中的小檗碱比单一的小檗碱的转运量要低。结论小檗碱在AP→BL方向以被动转运为主,在BL→AP方向以主动转运为主;同时还受到P-gp糖蛋白的调节。提取物中的小檗碱在Caco-2模型中转运的影响因素呈多样化。
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| 关 键 词： | 小檗碱 Caco-2 高效液相色谱法 表观渗透系数 被动转运 主动转运 P-gp |
Transport of berberine as single compound and berberine in extract in Caco-2 cell model |
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| WU An-guo,ZENG Bao,WANG Chun-ling,CHEN Jian-nan,LAI Xiao-ping.Transport of berberine as single compound and berberine in extract in Caco-2 cell model[J].Chinese Pharmacological Bulletin,2011,27(7):1007-1011. |
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| Authors: | WU An-guo ZENG Bao WANG Chun-ling CHEN Jian-nan LAI Xiao-ping |
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| Institution: | WU An-guo1,ZENG Bao1,2,WANG Chun-ling1,CHEN Jian-nan1,LAI Xiao-ping1,2 (1.Research and Development Center of New Drugs,Guangzhou University of TCM,Guangzhou 510006,China,2.Dongguan Mathematical Engineering Academy of Chinese Medicine,Dongguan Guangdong 523808,China) |
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| Abstract: | Aim To study the transport of bererine as single compound and berberine in extract in Caco-2 cell model.Methods The two-way transport of drugs was studied with the use of Caco-2 cell monolayer model.Firstly,the effects of time,drug concentration,inhibitors,pH and temperature on the absorption and transport of berberine were studied systematically.Secondly,the differences were compared between the transport of the same concentration berberine as single compound and that in extract in Caco-2 cell model.The dr... |
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| Keywords: | Caco-2 P-gp |
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