| Stereoselective regulation of MDR1 expression in Caco-2 cells by cetirizine enantiomers. | |
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MedLine Citation:
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PMID: 17394131 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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MDR1-encoded P-glycoprotein (P-gp) is a drug efflux transporter mainly expressed in liver, kidney, intestine, brain (at the level of the blood-brain barrier), and placenta. It thus plays important roles in drug absorption, distribution, and excretion. Cetirizine is a second-generation nonsedating antihistamine used to treat allergic disease of respiratory system, skin and eyes. To evaluate P-gp expression and function in Caco-2 cells pretreated with cetirizine enantiomers, we assessed the sensitivity of Caco-2 cells to paclitaxel using the MTT assay and the polarized transport of rhodamine-123 and doxorubicin across Caco-2 monolayers. RT-PCR and flow cytometry were used to assay MDR1 mRNA and P-gp protein respectively. The sensitivity of Caco-2 cells to paclitaxel decreased significantly after cells were pretreated with 100 microM R-cetirizine but increased upon treatment with S-cetirizine. The efflux of rhodamine-123 and doxorubicin was enhanced significantly after Caco-2 monolayers were pretreated with 100 microM R-cetirizine but was reduced by S-cetirizine. The MDR1 mRNA and P-gp levels in Caco-2 cells were increased by 100 microM R-cetirizine and decreased by 100 microM S-cetirizine. These results suggest that R-cetirizine up-regulates MDR1 expression while S-cetirizine down-regulates MDR1 expression. |
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Authors:
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Shuijie Shen; Ying He; Su Zeng |
Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Chirality Volume: 19 ISSN: 0899-0042 ISO Abbreviation: Chirality Publication Date: 2007 Jun |
Date Detail:
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Created Date: 2007-04-30 Completed Date: 2007-09-05 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 8914261 Medline TA: Chirality Country: United States |
Other Details:
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Languages: eng Pagination: 485-90 Citation Subset: IM |
Affiliation:
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Department of Pharmaceutical Analysis and Drug Metabolism, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Biological Transport Caco-2 Cells Cetirizine / chemistry*, pharmacology* Dose-Response Relationship, Drug Drug Interactions Drug Resistance, Neoplasm Flow Cytometry Gene Expression Regulation, Neoplastic* Histamine H1 Antagonists, Non-Sedating / pharmacology* Humans P-Glycoprotein / biosynthesis*, chemistry, physiology* P-Glycoproteins / metabolism Paclitaxel / pharmacology Rhodamine 123 / pharmacology Stereoisomerism |
| Chemical | |
Reg. No./Substance:
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0/Histamine H1 Antagonists, Non-Sedating; 0/P-Glycoprotein; 0/P-Glycoproteins; 33069-62-4/Paclitaxel; 62669-70-9/Rhodamine 123; 83881-51-0/Cetirizine |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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