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利用Caco-2细胞模型研究芦丁在小肠上皮的摄取、跨膜转运及外排动力学机制,评价孵育时间、芦丁浓度、P-糖蛋白抑制剂环孢素A和多药耐药相关蛋白抑制剂维拉帕米对芦丁的细胞摄取与转运的影响。结果表明,药物摄取量与孵育时间、药物浓度呈正相关,环孢素A和维拉帕米对芦丁的细胞摄取量无显著影响(P>0.05)。不同浓度药物从基底侧(basolateral,BL)到肠腔侧(Apical,AP)的表观渗透系数P_(app.BL-AP)与AP到BL的P_(app.AP-BL)比值均在0.5～1.5。试验结果提示芦丁是以被动扩散为主要转运方式被小肠上皮细胞摄取和转运,且不受外排蛋白外排作用的影响。
Caco-2 cell model was used to study the uptake, transmembrane transport and efflux mechanism of rutin in the small intestine. The incubation time, rutin concentration, cyclosporin A and multidrug resistance-related protein Effect of inhibitor verapamil on cellular uptake and transport of rutin. The results showed that there was a positive correlation between drug intake and incubation time and drug concentration. Cyclosporine A and verapamil had no significant effect on the cellular uptake of rutin (P> 0.05). The ratios of P_ (app.BL-AP) and P_ (app.AP-BL) from AP to BL for different concentrations of drugs from the basolateral (BL) to the apical (AP) ~ 1.5. The results suggest that rutin is absorbed and transported by intestinal epithelial cells by passive diffusion as the main transport mode, and is not affected by efflux of efflux protein.