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本文应用MDCK-pHaMDR细胞单层模型,评价20(S)-原人参三醇(1)和20(R)-原人参三醇(2)差向异构体及达玛-20(22)E,24-二烯-33,6α,12β-三醇(3)在血脑屏障的吸收性.为了评价三个化合物的吸收性和预测其吸收机制,对它们的双向透过性进行了研究,并计算了相应的表观渗透系数(Papp).在三个受试化合物中,原人参三醇差向异构体化合物1和2显示了良好的吸收性,Papp值在1×10-5 cm/s数量级;而化合物3判断为吸收不良的化合物,其Papp值小于1×10-7 cm/s.三个化合物由于结构上的差异,在细胞内产生了不同程度的蓄积.维拉帕米抑制P糖蛋白的转运实验结果表明,化合物1和2在MDCK-pHaMDR细胞单层模型中的转运机制不仅仅是单纯的被动扩散.本文的研究结果为化合物1和2作用于脑的研究提供了实验依据.“,”The blood-brain barrier permeability of 20(S) and 20(R)-protopanaxatriol epimers and dammar-20(22)E,24-diene-33,6t,123-triol were investigated using the MDCK-pHaMDR cell monolayer model.The bidirectional permeability tests were carried out,and the apparent permeability coefficients (Papp) were calculated.The two protopanaxatriol epimers showed good permeability with Papp values of～10-5 cm/s,whereas dammar-20(22)E,24-diene-3β,6α,12β-triol showed poor permeability with Papp of ＜1 x 10-7 cm/s.The three compounds showed differences in intracellular accumulations due to their different structures.Inhibition of P-gp with verapamil showed that the transport mechanisms in MDCK-pHaMDR cell monolayer for compounds 1 and 2 epimers were not only simple passive diffusion but also involving an efflux way mediated by P-gp.These findings provided new basis for the further study of compounds 1 and 2 acting on the brain.