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

被引：58

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

页码：1092 / 1094

页数：3

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