6-去甲氧基-4'-O-甲基茵陈色原酮在Caco-2细胞模型中的转运方式

目的：研究一枝蒿黄酮类成分6-去甲氧基-4'-O-甲基茵陈色原酮（DM）在Caco-2细胞模型中的转运特性。方法：采用Caco-2细胞单层模型研究DM的双向转运，考察药物质量浓度、方向和温度对DM细胞转运的影响。应用HPLC法，采用Agilent Eclipse XDB-C₁₈色谱柱（150 mm×4.6 mm，5 μm），以乙腈-0.1%醋酸水溶液为流动相，流速1.0 mL·min^-1，检测波长280 nm，柱温25℃，检测DM在介质中的含量，计算其表观渗透系数（P_app）。结果：DM的细胞转运P_app随着浓度的增大而减小，呈现浓度依赖性；低温条件下时，DM的双向的P_app值均显著性降低。结论：DM在Caco-2细胞单层模型中的转运过程主要以主动转运载体介导的方式，没有方向依赖性，也不涉及外排蛋白转运载体。

Objective:To research the transport characteristics of 6-demethoxy-4'-O-methylcapillarisin(DM)in Caco-2 cells model.Methods:The two-way transport of DM was studied by using Caco-2 cell monolayer model.The effects of drug concentration,direction and temperature on the transport of DM cells were investigated.The determination of DM was performed by HPLC.The samples were separated on an Agilent Eclipse XDB-C₁₈ column(150 mm×4.6 mm,5 μm)by gradient elution with acetonitrile-0.1% acetic acid aqueous solution at a flow rate of 1.0 mL·min^-1.The detection wavelength was 280 nm.The column temperature was controlled at 25℃.The content of DM in the medium was measured and its apparent permeability coefficient (P_app)was calculated.Results:Cell transport P_app of DM decreased with the increase of concentration in a concentration-dependent manner.At low temperature,the two-way P_app values of DM decreased significantly.Conclusion:The transport of DM in Caco-2 cells monolayer model was mainly mediated by active transport carrier,which had no directional dependence and no involvment the external protein transport carrier.

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