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维拉帕米对胡桃醌Caco-2细胞转运特性的影响 被引量:2

Influence of Verapamil on Juglone Caco- 2 Cell Transport Characteristics
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摘要 目的研究维拉帕米对胡桃醌Caco-2细胞转运特性的影响。方法应用Caco-2细胞模型考察时间、浓度对胡桃醌转运吸收特性的影响,应用P-糖蛋白抑制剂维拉帕米对胡桃醌转运吸收机制进行研究,采用高效液相色谱(HPLC)法测定胡桃醌的浓度,计算其表观渗透系数(Papp)。结果 Caco-2细胞模型,随浓度增加和时间延长,胡桃醌的累积转运量逐渐增加;加用维拉帕米(100μmol/L)后,使AP侧到BL侧的表观渗透系数Papp AP→BL显著增加,而从BL侧到AP侧的表观渗透系数Papp BL→AP降低。结论胡桃醌的转运以被动转运为主,存在P-糖蛋白参与的主动外排,加用维拉帕米后胡桃醌经吸收转运增加,提示维拉帕米可能促进吸收。 Objective To investigate the influence of verapamil on transport characteristics of juglone Caco- 2 cells model. Methods The juglone Caco- 2 cells model was adopted to investigate the influence of time and concentration on juglone transport and absorption characteristics. The P- glycoprotein( P- gp) inhibitor verapamil was used to investigate the juglone transport mechanism. The HPLC method was adopted to detect the juglone concentration. The apparent permeability coefficient( Papp) was calculated. Results In the Caco- 2cells model, the cumulative transport quantity of juglone was gradually increased with the concentration increase and the time extending. After adding verapamil( 100 μmol / L), Papp( AP → BL) was significantly increased, while Papp( BL → AP) was decreased. Conclusion The absorption of juglone in Caco- 2 cells model is dominated by the passive transference,and the active efflux participated by P- gp exists,after adding juglone in Caco- 2 cells,the absorption and transference of juglone,which suggesting that verapamil could promote the absorption.
出处 《中国药业》 CAS 2014年第21期31-33,共3页 China Pharmaceuticals
关键词 胡桃醌 CACO-2细胞 维拉帕米 juglone Caco-2 cells model verapamil
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