Abstract
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 microM). 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.
Publication types
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / antagonists & inhibitors*
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Anti-HIV Agents / pharmacology*
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Blotting, Western
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Caco-2 Cells
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Dose-Response Relationship, Drug
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Fluorescent Dyes / metabolism
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HIV Protease Inhibitors / pharmacology*
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Humans
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Lopinavir
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Pyrimidinones / pharmacology*
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RNA, Messenger / metabolism
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RNA, Viral / metabolism
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Rhodamine 123 / antagonists & inhibitors
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Time Factors
Substances
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Anti-HIV Agents
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Fluorescent Dyes
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HIV Protease Inhibitors
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Pyrimidinones
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RNA, Messenger
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RNA, Viral
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Rhodamine 123
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Lopinavir