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本文应用MDCK-p Ha MDR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-3β,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-p Ha MDR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。
In this study, the MDCK-p Ha MDR cell monolayer model was used to evaluate the effects of 20 (S) - protopanaxantriol (1) and 20 (R) ) E, 24-diene-3β, 6α, 12β-triol (3) Absorbance to the blood-brain barrier. In order to evaluate the absorption of the three compounds and predict their absorption mechanism, their bi-directional permeability was studied and the corresponding apparent permeability coefficient (Papp) was calculated. Among the three tested compounds, the protopanaxeritol epimer compounds 1 and 2 showed good absorbency with a Papp value of the order of 1 × 10 -5 cm / s; and the compound 3 was judged as a malabsorption compound , Its Papp value is less than 1 × 10-7 cm / s. The three compounds, due to structural differences, produced varying degrees of accumulation in the cells. Verapamil inhibits the transport of P-glycoprotein The experimental results show that the transport mechanism of compounds 1 and 2 in MDCK-p Ha MDR cell monolayer model is not only passive diffusion. The results of this study provide experimental evidence for the study of compounds 1 and 2 acting on the brain.