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目的:研究P糖蛋白(P-gp)和多耐药相关蛋白2(MRP2)对芒果苷肠吸收的影响。方法:采用大鼠单向在体肠灌流模型,以酚红为标示物;UPLC法测定灌流液中芒果苷的含量,计算芒果苷在空肠和回肠段及加入P-gp抑制剂和MRP2抑制剂后的吸收常数(Ka)和表观渗透系数(Peff)。结果:芒果苷(5μg/ml)在回肠和空肠的吸收差异无统计学意义。在回肠段,加入P-gp抑制剂维拉帕米(0.1mmol/L)和环孢霉素A(0.1mmol/L)或MRP2抑制剂吲哚美辛(0.04mmol/L)后,芒果苷吸收的Peff值和Ka值均明显增加;在空肠段,维拉帕米可明显升高芒果苷吸收的Ka值,而其他各组的Peff值和Ka值虽有一定程度的增加,但无显著性差异。结论:P-gp和MRP2抑制剂对芒果苷的肠吸收,特别是回肠吸收,具有明显的促进作用,提示芒果苷为P-gp和MRP2的底物。
Objective: To study the effects of P-gp and MRP2 on intestinal absorption of mangiferin. Methods: Unilateral rat intestinal perfusion model was used, with phenol red as the marker. The content of mangiferin in the perfusate was determined by UPLC. The content of mangiferin in the jejunum and ileum and the addition of P-gp inhibitor and MRP2 inhibitor After the absorption constant (Ka) and apparent permeability coefficient (Peff). Results: The absorption of mangiferin (5μg / ml) in ileum and jejunum had no statistical significance. In the ileum segment, after adding P-gp inhibitor verapamil (0.1 mmol / L) and cyclosporine A (0.1 mmol / L) or MRP2 inhibitor indomethacin (0.04 mmol / L) The Peff value and Ka value increased significantly in the jejunal segment. Verapamil significantly increased the Ka value in the jejunal segment, while Peff value and Ka value in other groups increased to a certain extent Sex differences. CONCLUSION: P-gp and MRP2 inhibitors have a significant promoting effect on intestinal absorption of mangiferin, especially ileum, suggesting that mangiferin is a substrate of P-gp and MRP2.