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金丝桃苷在Caco-2细胞模型中的跨膜转运方式

杨希 顾政一 沙先谊 贺金华 方晓玲

中国临床药学杂志2012,Vol.21Issue(2):79-83,5.
中国临床药学杂志2012,Vol.21Issue(2):79-83,5.

金丝桃苷在Caco-2细胞模型中的跨膜转运方式

Absorption mechanism of hyperoside across Caco-2 cells model

杨希 1顾政一 2沙先谊 1贺金华 3方晓玲1

作者信息

  • 1. 新疆医科大学药剂学教研室,乌鲁木齐830054
  • 2. 新疆维吾尔自治区药物研究所,乌鲁木齐830004
  • 3. 复旦大学药学院药剂学教研室,上海201203
  • 折叠

摘要

Abstract

AIM To research the absorption mechanism of hyperoside across Caco-2 cells model. METHODS Depending on Caco-2 cell monolayers drug transport model to study the double transport mechanism of hyperoside, the effect on hyperoside absorption of pH,drug concentration,direction,temperature and inhibitors was explored. The determination of hyperoside was performed by HPLC. RESULTS The absorptive transport of hyperoside in the Caco-2 cells was pH dependence. Papp of Apical to Basolateral was much more than that of Basolateral to Apical, and reduced by the concentration increasing of hyperoside,so it was also concentration dependence. P-gp inhibitor verapamil enhanced the absorptive transport of hyperoside from Apical to Basolateral,and reduced the absorptive transport of hyperoside from Basolateral to Apical. On the high concentration of hyperoside, MRP1 inhibitor indomethacin and ATP inhibitor sodiumazide significantly reduced the absorptive transport of hyperoside. CONCLUSION The absorption transport of hyperoside is pH and concentration dependence, absorption of hyperoside in Caco-2 cell model should be an active transport primarily supplemented by passive diffusion, along with excretion mediated action. The ability of active transport is much more than that of passive diffusion.

关键词

金丝桃苷/Caco-2细胞模型/吸收转运

Key words

hyperoside/ Caco-2 cells model/ absorptive transport

引用本文复制引用

杨希,顾政一,沙先谊,贺金华,方晓玲..金丝桃苷在Caco-2细胞模型中的跨膜转运方式[J].中国临床药学杂志,2012,21(2):79-83,5.

基金项目

国家科技重大专项“重大新药创制”课题——金蒿抗流感滴丸临床前研究(编号2011ZX09102-009-07) (编号2011ZX09102-009-07)

中国临床药学杂志

OACSTPCD

1007-4406

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