Document Detail


Fenofibrate increases very low density lipoprotein triglyceride production despite reducing plasma triglyceride levels in APOE*3-Leiden.CETP mice.
MedLine Citation:
PMID:  20501652     Owner:  NLM     Status:  MEDLINE    
Abstract/OtherAbstract:
The peroxisome proliferator-activated receptor alpha (PPARalpha) activator fenofibrate efficiently decreases plasma triglycerides (TG), which is generally attributed to enhanced very low density lipoprotein (VLDL)-TG clearance and decreased VLDL-TG production. However, because data on the effect of fenofibrate on VLDL production are controversial, we aimed to investigate in (more) detail the mechanism underlying the TG-lowering effect by studying VLDL-TG production and clearance using APOE*3-Leiden.CETP mice, a unique mouse model for human-like lipoprotein metabolism. Male mice were fed a Western-type diet for 4 weeks, followed by the same diet without or with fenofibrate (30 mg/kg bodyweight/day) for 4 weeks. Fenofibrate strongly lowered plasma cholesterol (-38%) and TG (-60%) caused by reduction of VLDL. Fenofibrate markedly accelerated VLDL-TG clearance, as judged from a reduced plasma half-life of glycerol tri[(3)H]oleate-labeled VLDL-like emulsion particles (-68%). This was associated with an increased post-heparin lipoprotein lipase (LPL) activity (+110%) and an increased uptake of VLDL-derived fatty acids by skeletal muscle, white adipose tissue, and liver. Concomitantly, fenofibrate markedly increased the VLDL-TG production rate (+73%) but not the VLDL-apolipoprotein B (apoB) production rate. Kinetic studies using [(3)H]palmitic acid showed that fenofibrate increased VLDL-TG production by equally increasing incorporation of re-esterified plasma fatty acids and liver TG into VLDL, which was supported by hepatic gene expression profiling data. We conclude that fenofibrate decreases plasma TG by enhancing LPL-mediated VLDL-TG clearance, which results in a compensatory increase in VLDL-TG production by the liver.
Authors:
Silvia Bijland; Elsbet J Pieterman; Annemarie C E Maas; José W A van der Hoorn; Marjan J van Erk; Jan B van Klinken; Louis M Havekes; Ko Willems van Dijk; Hans M G Princen; Patrick C N Rensen
Publication Detail:
Type:  Journal Article; Research Support, Non-U.S. Gov't     Date:  2010-05-25
Journal Detail:
Title:  The Journal of biological chemistry     Volume:  285     ISSN:  1083-351X     ISO Abbreviation:  J. Biol. Chem.     Publication Date:  2010 Aug 
Date Detail:
Created Date:  2010-08-09     Completed Date:  2010-08-30     Revised Date:  2011-08-25    
Medline Journal Info:
Nlm Unique ID:  2985121R     Medline TA:  J Biol Chem     Country:  United States    
Other Details:
Languages:  eng     Pagination:  25168-75     Citation Subset:  IM    
Affiliation:
Department of Human Genetics, Leiden University Medical Center, 2300 RC Leiden, The Netherlands.
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MeSH Terms
Descriptor/Qualifier:
Animals
Apolipoproteins B / metabolism
Fenofibrate / pharmacology*
Humans
Lipid Metabolism / drug effects
Lipoproteins, HDL / metabolism
Lipoproteins, VLDL / metabolism*
Liver / drug effects,  metabolism
Male
Mice
Mice, Transgenic
Triglycerides / blood*,  metabolism
Chemical
Reg. No./Substance:
0/Apolipoproteins B; 0/Lipoproteins, HDL; 0/Lipoproteins, VLDL; 0/Triglycerides; 0/very low density lipoprotein triglyceride; 49562-28-9/Fenofibrate
Comments/Corrections

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