饮食类黄酮对运输的影响通过22西咪替丁和阳离子转运蛋白在Caco-2和LLC-PK1细胞模型。
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Taur JS, Rodriguez-Proteau R
饮食类黄酮对运输的影响通过22西咪替丁和阳离子转运蛋白在Caco-2和LLC-PK1细胞模型。
Xenobiotica。2008年12月,38 (12):1536 - 50。doi: 10.1080 / 00498250802499467。
- PubMed ID
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18951251 (在PubMed]
- 文摘
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1。假设测试是研究西咪替丁的衬底22 (P-gp)和有机阳离子运输系统和八个黄酮苷配基的调节效应和苷在这些运输系统使用Caco-2和LLC-PK1细胞。2。运输和吸收实验(20 microM) (3) H-cimetidine进行有或没有一氧化碳暴露槲皮素,quercetrin,芸香苷,柚苷配基、柚皮苷、染料木素、精制,xanthohumol。基底Co-treatment下降到顶端(B)渗透率(P (app))的西咪替丁从2.02到1.24(槲皮素),1.06(柚苷配基),1.24(染料木黄酮),和0.96 (xanthohumol) x 10 s(1)(6)厘米Caco-2细胞和从10.76到1.65(槲皮素),2.05(柚苷配基),2.88(染料木黄酮)和1.95 (xanthohumol) x 10(6)厘米LLC-PK1细胞(1)。萃取精制显著降低B P (app)的西咪替丁1.24 x 10(6)厘米s在Caco-2细胞(1)。西咪替丁的基底细胞内吸收速率增强当co-treated与类黄酮145 - 295%。Co-treatment 22和有机阳离子转运蛋白抑制剂,维拉帕米和酚苄明,导致减少B渗透率和西咪替丁的基底细胞内吸收速率较慢。细胞内吸收的速度(14)C-tetraethylammonium(茶)降低了槲皮素的存在,柚苷配基和染料木黄酮LLC-PK1细胞。3所示。 In conclusion, quercetin, naringenin, genistein, and xanthohumol reduced P-gp-mediated transport and increased the basolateral uptake rate of cimetidine. Quercetin, naringenin, genistein, but not xanthohumol, reduced intracellular uptake rate of TEA in LLC-PK1 cells. These results suggest that flavonoids may have potential to alter the disposition profile of cimetidine and possibly other therapeutics that are mediated by P-gp and/or cation transport systems.