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目的研究蛇床子素在Caco-2细胞模型中的转运机制。方法通过研究蛇床子素在Caco-2细胞模型中的转运,考察蛇床子素浓度、PEG600、P-gp抑制剂维拉帕米(verapamil)及温度对蛇床子素转运的影响。结果随着蛇床子素溶液浓度和温度的升高,蛇床子素在Caco-2细胞中AP-BL的转运量增加;PEG600对蛇床子素在Caco-2细胞中的AP-BL的转运量有显著增加;P-gp抑制剂维拉帕米对蛇床子素在Caco-2细胞中转运的表观通透系数PAP和PBL无显著影响。结论蛇床子素表观通透系数PAP大于10×10-6cm.s-1,较易被Caco-2细胞吸收,但由于3个浓度蛇床子素溶液的PAP和PBL比值无明显变化、P-gp抑制剂对PAP和PBL无明显影响及转运的活化能较低(17.31 kJ.mol-1),因此,蛇床子素在Caco-2细胞模型中的转运机制主要是被动转运。
Objective To study the transport mechanism of osthole in Caco-2 cell model. Methods The translocation of osthole in Caco-2 cell model was investigated to investigate the effects of osthole concentration, PEG600, verapamil, a P-gp inhibitor, and oseltamivir on osthole transport. Results With the increase of osthole solution concentration and temperature, the translocation of osthole to AP-BL in Caco-2 cells increased. The translocation of osthole-AP-BL in Caco-2 cells by PEG600 P-gp inhibitor verapamil had no significant effect on the apparent permeability coefficients PAP and PBL of osthole transport in Caco-2 cells. Conclusion The osmolality of osthole is larger than 10 × 10-6cm · s-1, which is more likely to be absorbed by Caco-2 cells. However, the PAP and PBL ratios of the three osthole solutions did not change significantly. P- The GPP inhibitor had no obvious effect on PAP and PBL and had a lower activation energy (17.31 kJ · mol-1). Therefore, the translocation mechanism of osthole in Caco-2 cell model was mainly passive.