中国药理学通报2011,Vol.27Issue(7):1007-1011,5.DOI:10.3969/j.issn.1001-1978.2011.07.027
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
Transport of berberine as single compound and berberine in extract in Caco-2 cell model
摘要
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 drug concentration was determined by high performance liquid chromatography ( HPLC ) to calculate the apparent permeability coefficient. Results As for the same concentration of berberine, the amount of transport from the base side( BL ) to the top side( AP ) was more than the top side ( AP ) to the base side ( BL ). Both in AP→BL and BL→AP directions,the amount of transport was increasing with time. Verapamil significantly decreased the amount of transport in BL→AP direction. In AP→BL direction, the amount of transport in HBSS at pH = 5 was the largest. In BL→AP direction, the transport was more temperature dependent. Both in AP→BL and BL→AP directions,the amount of transport of berberine in extract was less than that of berberine as single compound. Conclusion Berberine in AP→BL direction is mainly passively transported,whereas in BL→AP direction, the transport is mainly active. At the same time the transport is adjusted by P-gp. The effects on the transport of berberine in extract in Caco-2 model include diverse factors.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分类
医药卫生引用本文复制引用
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):1007-1011,5.基金项目
国家科技支撑计划资助项目(No 2006BAI11B00) (No 2006BAI11B00)