Lopinavir: acute exposure inhibits P-glycoprotein; extended exposure induces P-glycoprotein

被引：59
|
作者：
Vishnuvardhan, D [1 ]
von Moltke, LL
Richert, C
Greenblatt, DJ
机构：
[1] Tufts Univ, Sch Med, Dept Pharmacol & Expt Therapeut, Boston, MA 02111 USA
[2] Univ Konstanz, Dept Chem, D-7750 Constance, Germany
来源：
AIDS | 2003年 / 17卷 / 07期
关键词：
D O I：
10.1097/00002030-200305020-00023
中图分类号：
R392 [医学免疫学]; Q939.91 [免疫学];
学科分类号：
100102 ;
摘要：
The effect of lopinavir on P-glycoprotein-mediated rhodamine 123 efflux was studied in Caco-2 monolayer cells. Lopinavir is a potent inhibitor of Rh123 efflux in Caco-2 monolayers (IC50 1.7 muM). Chronic lopinavir exposure (72 h) in LS 180V cells reduced the content of intracellular Rh123 by approximately 50%, indicating increased efflux activity. In LS 180V cells, lopinavir induced P-glycoprotein immunoreactive protein (up to threefold) and messenger RNA levels in a concentration-dependent fashion.
引用
收藏
页码：1092 / 1094
页数：3
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