本文關(guān)鍵詞：芍藥苷類化合物在人源腸Caco-2細胞單層模型中的吸收轉(zhuǎn)運研究，由筆耕文化傳播整理發(fā)布。

芍藥苷類化合物在人源腸Caco-2細胞單層模型中的吸收轉(zhuǎn)運研究

Absorption and transport characteristic of paeoniflorin and its derivatives in model of Caco-2 cell monolayers

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YANG Xiu-wei, GUO Jie, XU Wei State Key Laboratory of Natural and Biomimetic Drugs, Department of Natural Medicines, College of Pharmaceutical Sciences, Peking University, Beij

北京大學(xué)天然藥物及仿生藥物國家重點實驗室北京大學(xué)藥學(xué)院天然藥物學(xué)系,北京100191

文章摘要：目的研究芍藥苷、羥基芍藥苷、苯甲酰芍藥苷、四乙酰芍藥苷、五乙酰芍藥苷和五乙酰芍藥內(nèi)酯苷在人源結(jié)腸腺癌細胞系Caco-2細胞單層模型中的吸收特性。方法利用Caco-2細胞單層模型檢測上述6個化合物從孔板頂端（AP）→底端（BL）、BL→AP的雙向轉(zhuǎn)運過程。應(yīng)用偶聯(lián)紫外檢測器的HPLC法測定上述6個化合物,計算轉(zhuǎn)運參數(shù)和表觀滲透系數(shù)（Papp）,并與陽性對照藥普萘洛爾和阿替洛爾進行比較。結(jié)果芍藥苷雙向轉(zhuǎn)運的Papp值與阿替洛爾的Papp值皆在10 7cm/s數(shù)量級;其他5個化合物的Papp值介于在Caco-2細胞單層模型中吸收良好的普萘洛爾與難以吸收的阿替洛爾的Papp值之間。芍藥苷、羥基芍藥苷、苯甲酰芍藥苷濃度為10～200μmol/L,四乙酰芍藥苷和五乙酰芍藥內(nèi)酯苷濃度為10～150μmol/L,五乙酰芍藥苷濃度為10～100μmol/L時,其轉(zhuǎn)運效率與濃度呈正相關(guān)。結(jié)論 6個受試化合物可以通過小腸上皮細胞被動吸收進入體內(nèi),芍藥苷屬于難吸收的化合物,羥基芍藥苷、苯甲酰芍藥苷、四乙酰芍藥苷、五乙酰芍藥苷和五乙酰芍藥內(nèi)酯苷屬于中等吸收的化合物;苯甲酰芍藥苷具有促進阿替洛爾在Caco-2細胞單層模型吸收轉(zhuǎn)運的作用。

Abstr：Objective To study the absorption and transport characteristic of paeoniflorin （PF）, oxypaeoniflorin （OP）, benzoylpaeoniflorin （BP）, tetraacetylpaeoniflorin （TP）, pentaacetylpaeoniflorin （PP）, and pentacacetylalbiflorin （PA） in human colon adenocarcinoma cell line Caco-2 cell monolayer model. Methods The Caco-2 cell monolayers were used as an intestinal epithelial cell model. The permeability of the tested compounds from apical （AP） side to basolateral （BL） side or from BL side to AP side was evaluated. The concentration of the tested compounds was measured by HPLC coupled with UV detector. The transport parameters and apparent permeability coefficients （Papp） were calculated, and the Papp values were compared with the reported values for model compounds, Propranolol and AtenoloL Results The Papp values of PF in the bi-directional transport and atenolol were at the quantitative degree of 10-7 cm/s. Whereas those of OP, BP, TP, PP, and PA were between atenolol and propranolol used as a controt substance for low and high permeability, respectively. The absorption and transport of the tested compounds were concentration-dependent at the concentration range of 10--200 μmol/L for PF, OP, and BP, 10-- 150 I.tmol/L for TP and PA, and 10-- 100 μmol/L for PP. Conclusion The six tested compounds could be absorbed across the intestinal epithelial cells by passive diffusion mechanism. PF is poorly absorbed compound and OP, BP, TP, PP, and PA are moderately absorbed compounds. BP has a role to promote atenolol uptake transporters in Caco-2 cell monolayer model.

文章關(guān)鍵詞：

Keyword：:paeoniflorin oxypaeoniflorin benzoylpaeoniflorin tetraacetylpaeoniflorin pentaacetylpaeoniflorin pentacacetyl-albiflorin Caco-2 cell monolayers apparent permeability coefficients

課題項目：“十二五”國家科技支撐計劃資助項目（2011BAI07B08）

作者信息：會員可見

  本文關(guān)鍵詞：芍藥苷類化合物在人源腸Caco-2細胞單層模型中的吸收轉(zhuǎn)運研究，由筆耕文化傳播整理發(fā)布。