EVIDENCE THAT DESFERRIOXAMINE CANNOT ENTER CELLS BY PASSIVE DIFFUSION
EVIDENCE THAT DESFERRIOXAMINE CANNOT ENTER CELLS BY PASSIVE DIFFUSION
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DOI：
10.1016/0006-2952(91)90109-i
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发表时间：
1991-05-01
影响因子：
5.8
通讯作者：
RICEEVANS, C
中科院分区：
文献类型：
--
作者：
LLOYD, JB;CABLE, H;RICEEVANS, C
比较了[C-14]去铁胺在大鼠内脏卵黄囊和[C-14]蔗糖的体外蓄积，[C-14]蔗糖是液体相胞饮的探针。这两种底物的动力学参数非常相似，缓蚀剂的效果也是如此。从这些数据和理论考虑得出结论，去铁胺不能进入细胞，除非通过胞饮作用，一旦内化，它将留在溶酶体中。结果表明，需要重新评估传统上被接受的药物消耗细胞和组织中铁的能力的药代动力学机制。
Accumulation of [C-14]desferrioxamine by rat visceral yolk sac in vitro has been compared with that of [C-14]sucrose, a probe for fluid-phase pinocytosis. Kinetic parameters for both substrates are closely similar, as are the effects of inhibitors. It is concluded from these data, and from theoretical considerations, that desferrioxamine cannot enter cells other than by pinocytosis and that, once internalized, it will remain in the lysosomes. The results indicate the need for a re-evaluation of the pharmacokinetic mechanisms traditionally accepted for the drug's ability to deplete iron from cells and tissues.