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Transport and uptake characteristics of a new derivative of berberine(CPU-86017) by human intestinal epithelial cell line: Caco-2
引用本文:YANG Hai-Tao,WANG Guang-Ji Center of Pharmacokinetics,China Pharmaceutical University,Nanjing 210009,China. Transport and uptake characteristics of a new derivative of berberine(CPU-86017) by human intestinal epithelial cell line: Caco-2[J]. Acta pharmacologica Sinica, 2003, 0(12)
作者姓名:YANG Hai-Tao  WANG Guang-Ji Center of Pharmacokinetics  China Pharmaceutical University  Nanjing 210009  China
作者单位:YANG Hai-Tao,WANG Guang-Ji Center of Pharmacokinetics,China Pharmaceutical University,Nanjing 210009,China
基金项目:Project supported by the National Natural Science Foundation of China.
摘    要:AIM: The characteristics of transepithelial transport and uptake of CPU-86017 {[7-(4-chlorbenzyl)-7,8,13,13α-tetrahydroberberine chloride, CTHB]}, a new antiarrhythmia agent and a new derivative of berberine, were investigated on epithelial cell line (Caco-2) to further understand the absorption mechanism of berberine and its derivatives. METHODS: Caco-2 cell was used. RESULTS: 1) The permeability coefficient from the apical (AP) to basolateral (BL) of CPU-86017 was approximately 5 times higher than that from BL-to-AP transport. The effects of a P-glycoprotein (P-gp) inhibitor-cyclosporin A, some surfactants, and lower pH on the transepithelial transport of CPU-86017 were also observed. Cyclosporine A at 7.5 mg/L had no effect on the transepithelial electrical resistance (TEER); an about 4-fold enhancement on the transepithlial transport of CPU-86017 was observed. Some surfactants (sodium citrate, sodium deoxycholate, and sodium dodecyl sulfate) at 100 μmol/L and low pH (pH=6.0) induced a reversible d


Transport and uptake characteristics of a new derivative of berberine(CPU-86017) by human intestinal epithelial cell line: Caco-2
YANG Hai-Tao,WANG Guang-Ji Center of Pharmacokinetics,China Pharmaceutical University,Nanjing ,China. Transport and uptake characteristics of a new derivative of berberine(CPU-86017) by human intestinal epithelial cell line: Caco-2[J]. Acta pharmacologica Sinica, 2003, 0(12)
Authors:YANG Hai-Tao  WANG Guang-Ji Center of Pharmacokinetics  China Pharmaceutical University  Nanjing   China
Affiliation:YANG Hai-Tao,WANG Guang-Ji Center of Pharmacokinetics,China Pharmaceutical University,Nanjing 210009,China
Abstract:
Keywords:CPU-86017  berberine  Caco-2 cell  cyclosporine A  sodium dodecyl sulfate  sodium citrate  sodium deoxycholate
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