【摘要】 目的建立C aco-2细胞模型,探讨其在药物吸收研究方面的可靠性及作用。方法建立C aco-2细胞单层模型,采用几种标准的标记物在模型中行转运试验,对模型的完整性、通透性以及P-糖蛋白(P-gp)的表达进行验证,将结果与文献报道值比较。结果细胞旁转运及跨细胞被动转运的标记物荧光黄和普奈洛尔的表观渗透系数(Papp)值均与文献报道一致;P-gp的标准底物维拉帕米在模型中的外排能被P-gp的强抑制剂酮康唑抑制。结论本实验室建立的C aco-2细胞模型在模型完整性、通透性以及P-gp的表达方面能够满足胃肠道吸收化合物机制研究的需要。更多还原

【Abstract】 Objective:To explore the establishment of Caco-2 cell model and its value.Methods:Established the Caco-2 cell monolayer model and validated its integrality,permeability and the expression of P-glycoprotein(P-gp) using some standard markers.Compared the results with the reported ones.Results:The apparent permeability coefficients(Papp)of Lucifer yellow and propranolol markers of the paracellular and transcellular respectively were all within the range of the reported ones.The efflux of the standard substrate of P-gp verapamil could be effectively inhibited by ketoconazole,the potent inhibitor of P-gp.Conclusion:The Caco-2 cell monolayer model can be used to study major mechanisms of gastro-intestinal(GI)absorption.更多还原