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目的研究紫花前胡苷元(NANI)、紫花前胡苷(ND)、前胡苷V(DEV)和羌活苷(FDE)4个线型二氢呋喃香豆素类化合物在人源肠Caco-2细胞单层模型中的吸收特性。方法利用人源结肠腺癌细胞系Caco-2细胞单层模型测试4个香豆素类化合物从绒毛面(AP端)到基底面(BL端)、BL端到AP端2个方向的转运过程。应用偶联紫外检测器的高效液相色谱法对上述4个香豆素进行定量分析,计算转运参数和表观渗透系数(Papp),并与阳性对照药普萘洛尔和阿替洛尔进行比较。结果NANI双向转运的Papp值在1×10-6cm/s数量级,介于在Caco-2细胞单层模型上呈良好吸收的普萘洛尔和难吸收的阿替洛尔的Papp值之间。ND、DEV和FDE的Papp值与阿替洛尔的Papp值皆在1×10-7cm/s数量级。4个香豆素在25~400μmol/L的转运效率与浓度呈正相关。结论4个线型二氢呋喃类香豆素可以通过小肠上皮细胞被动吸收进入体内,NANI属于中等吸收的化合物;ND、DEV和FDE属于难吸收的化合物。
Objective To investigate the effects of four linear dihydrofumarin coumarins, including NANI, ND, VDE and FDE, in human intestinal Caco-2 cells Absorption characteristics in a single-layer model. Methods The monolayer model of human colon adenocarcinoma cell line Caco-2 was used to test the transport process of four coumarins from villus surface (AP end) to basal surface (BL end) and BL end to AP end . The four coumarins were quantitatively analyzed by HPLC coupled with UV detector to calculate the transport parameters and apparent permeability coefficient (Papp), and were compared with the positive control drugs propranolol and atenolol Compare Results The Papp value of NANI bidirectional transport was on the order of 1 x 10-6 cm / s, between the Papp values of propranolol which is well absorbed on the Caco-2 cell monolayers model and the less-absorbable atenolol. The Papp values for ND, DEV and FDE are all in the order of 1 x 10-7 cm / s with those of atenolol. The transport efficiency and concentration of four coumarins at 25 ~ 400μmol / L were positively correlated. CONCLUSION: Four linear coumarins of dihydrofuran can passively enter into the body through small intestine epithelial cells. NANI belongs to moderately absorbed compounds. ND, DEV and FDE are refractory compounds.