| Ezetimibe inhibits expression of acid sphingomyelinase in liver and intestine. | |
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MedLine Citation:
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PMID: 19777283 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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Ezetimibe inhibits cholesterol absorption in the intestine. Sphingomyelin has strong interactions with cholesterol. We investigated the effects of ezetimibe on Sphingomyelinase (SMase) expression in intestine and liver. After feeding rats with ezetimibe (5 mg/kg per day) for 14 days, acid SMase activities in the liver and in the proximal part of small intestine were reduced by 34 and 25%, respectively. Alkaline SMase (alk-SMase) was increased in the proximal part of the small intestine. Administration of lower doses of ezetimibe reduced acid SMase only in the liver by 14% (P < 0.05). In cell culture studies, ezetimibe decreased acid SMase activity in Hep G2 and Caco-2 cells dose-dependently. The reductions were more rapid for Hep G2 cells than for Caco-2 cells. Western blot showed that acid SMase protein was decreased in both Hep G2 and Caco-2 cells by 100 microM ezetimibe. The SM content was increased in Hep G2 cells but not Caco-2 cells, and total cholesterol content was increased in both cell lines 24 h after stimulation with 100 microM ezetimibe. Mevastatin, the inhibitor of cholesterol synthesis, induced a mild increase in acid SMase activity in Hep G2 cells but not Caco-2 cells. Following the reduction of acid SMase, ezetimibe at high dose slightly increased alk-SMase activity. In conclusion, the study demonstrates an inhibitory effect of ezetimibe on acid SMase activity and expression in both liver and intestine. |
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Authors:
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Yajun Cheng; Fuli Liu; Jun Wu; Yao Zhang; Ake Nilsson; Rui-Dong Duan |
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Publication Detail:
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Type: Comparative Study; Journal Article; Research Support, Non-U.S. Gov't Date: 2009-09-24 |
Journal Detail:
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Title: Lipids Volume: 44 ISSN: 1558-9307 ISO Abbreviation: Lipids Publication Date: 2009 Oct |
Date Detail:
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Created Date: 2010-01-29 Completed Date: 2010-08-27 Revised Date: - |
Medline Journal Info:
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Nlm Unique ID: 0060450 Medline TA: Lipids Country: Germany |
Other Details:
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Languages: eng Pagination: 897-906 Citation Subset: IM |
Affiliation:
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Gastroenterology and Nutrition Lab, BMC, B11, Institution of Clinical Sciences, Lund University, 221 84, Lund, Sweden. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Azetidines / administration & dosage, pharmacology* Caco-2 Cells Cell Line, Tumor Female Gene Expression Regulation, Enzymologic / drug effects Humans Intestine, Small / drug effects, enzymology* Liver / drug effects, enzymology* Phosphodiesterase Inhibitors / pharmacology* Rats Rats, Sprague-Dawley Sphingomyelin Phosphodiesterase / antagonists & inhibitors*, biosynthesis* |
| Chemical | |
Reg. No./Substance:
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0/Azetidines; 0/Phosphodiesterase Inhibitors; 163222-33-1/ezetimibe; EC 3.1.4.12/Sphingomyelin Phosphodiesterase |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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