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两种非甾体抗炎药:吲哚美辛和酮洛芬的细胞摄取及亚细胞分布

Cellular uptake and subcellular distribution of two non-steroidal anti-inflammatory drugs: indomethacin and ketoprofen.

作者信息

Blanchard J C, Schneider Y J, Tulkens P, Trouet A

出版信息

Arch Int Pharmacodyn Ther. 1979 Jul;240(1):4-16.

PMID:507996
Abstract

The cellular uptake and intracellular localization of indomethacin and ketoprofen were studied on rat embryo fibroblasts in vitro. The two drugs are taken up by the cells, but to a lesser extent for ketoprofen than for indomethacin. Inside fibroblasts ketoprofen is rapidly metabolized whereas indomethacin seems accumulated as such inside the cells. After different incubation times, ketoprofen is partly associated to the cytosol and partly to another cellular component, probably the endoplasmic reticulum. Indomethacin on the other hand is almost exclusively distributed inside the cytosol. No clear association of the two drugs can be found with the lysosomes.

摘要

在体外对大鼠胚胎成纤维细胞进行了吲哚美辛和酮洛芬的细胞摄取及细胞内定位研究。这两种药物都能被细胞摄取,但酮洛芬的摄取程度低于吲哚美辛。在成纤维细胞内,酮洛芬迅速代谢,而吲哚美辛似乎以原样在细胞内蓄积。经过不同的孵育时间后,酮洛芬部分与细胞质溶胶相关,部分与另一种细胞成分(可能是内质网)相关。另一方面,吲哚美辛几乎完全分布在细胞质溶胶内。未发现这两种药物与溶酶体有明显关联。

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