Mechanisms of action in the liver of crilvastatin, a new hydroxymethylglutaryl-coenzyme A reductase inhibitor
Identifieur interne : 000151 ( France/Analysis ); précédent : 000150; suivant : 000152Mechanisms of action in the liver of crilvastatin, a new hydroxymethylglutaryl-coenzyme A reductase inhibitor
Auteurs : Thierry Clerc [France] ; Michel Jomier [France] ; Magali Chautan [France] ; Henry Portugal [France] ; Michèle Senft ; Anne-Marie Pauli [France] ; Claude Laruelle [France] ; Olivier Morel [France] ; Huguette Lafont [France] ; Françoise ChanussotSource :
- European Journal of Pharmacology [ 0014-2999 ] ; 1993.
Abstract
Crilvastatin is a drug from the pyrrolidone family that had been shown to induce non-competitive inhibition of rat hydroxymethylglutaryl-coenzyme A reductase activity in vitro. The aim of this study was to evaluate the activity of crilvastatin on the hepatic metabolism of cholesterol in rats. Crilvastatin increased low density lipoprotein (LDL)-cholesterol uptake by the liver more than high density lipoprotein (HDL) uptake, thus increasing by up 30% the clearance of excess plasma cholesterol. In normolipidemic rats, crilvastatin significantly enhanced acyl coenzyme A: cholesterol acyl transferase and cholesterol 7α-hydroxylase activity. In rats with a previous high cholesterolemia, crilvastatin also enhanced cholesterol 7α-hydroxylase activity and did not increase liver acyl coenzyme A: cholesterol acyl transferase activity. These findings suggest that a drug such as crilvastatin could have a hypocholesterolemic effect by a mechanism other than the sole inhibition of cholesterol synthesis, possibly by stimulating cholesterol and bile salt secretion via the biliary tract in previously hypercholesterolemic rats.
Url:
DOI: 10.1016/0014-2999(93)90820-8
Affiliations:
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The aim of this study was to evaluate the activity of crilvastatin on the hepatic metabolism of cholesterol in rats. Crilvastatin increased low density lipoprotein (LDL)-cholesterol uptake by the liver more than high density lipoprotein (HDL) uptake, thus increasing by up 30% the clearance of excess plasma cholesterol. In normolipidemic rats, crilvastatin significantly enhanced acyl coenzyme A: cholesterol acyl transferase and cholesterol 7α-hydroxylase activity. In rats with a previous high cholesterolemia, crilvastatin also enhanced cholesterol 7α-hydroxylase activity and did not increase liver acyl coenzyme A: cholesterol acyl transferase activity. These findings suggest that a drug such as crilvastatin could have a hypocholesterolemic effect by a mechanism other than the sole inhibition of cholesterol synthesis, possibly by stimulating cholesterol and bile salt secretion via the biliary tract in previously hypercholesterolemic rats.</div></front></TEI><affiliations><list><country><li>France</li></country><region><li>Provence-Alpes-Côte d'Azur</li></region><settlement><li>Carros</li><li>Marseille</li></settlement></list><tree><noCountry><name sortKey="Chanussot, Francoise" sort="Chanussot, Francoise" uniqKey="Chanussot F" first="Françoise" last="Chanussot">Françoise Chanussot</name><name sortKey="Senft, Michele" sort="Senft, Michele" uniqKey="Senft M" first="Michèle" last="Senft">Michèle Senft</name></noCountry><country name="France"><region name="Provence-Alpes-Côte d'Azur"><name sortKey="Clerc, Thierry" sort="Clerc, Thierry" uniqKey="Clerc T" first="Thierry" last="Clerc">Thierry Clerc</name></region><name sortKey="Chautan, Magali" sort="Chautan, Magali" uniqKey="Chautan M" first="Magali" last="Chautan">Magali Chautan</name><name sortKey="Jomier, Michel" sort="Jomier, Michel" uniqKey="Jomier M" first="Michel" last="Jomier">Michel Jomier</name><name sortKey="Lafont, Huguette" sort="Lafont, Huguette" uniqKey="Lafont H" first="Huguette" last="Lafont">Huguette Lafont</name><name sortKey="Laruelle, Claude" sort="Laruelle, Claude" uniqKey="Laruelle C" first="Claude" last="Laruelle">Claude Laruelle</name><name sortKey="Morel, Olivier" sort="Morel, Olivier" uniqKey="Morel O" first="Olivier" last="Morel">Olivier Morel</name><name sortKey="Pauli, Anne Marie" sort="Pauli, Anne Marie" uniqKey="Pauli A" first="Anne-Marie" last="Pauli">Anne-Marie Pauli</name><name sortKey="Portugal, Henry" sort="Portugal, Henry" uniqKey="Portugal H" first="Henry" last="Portugal">Henry Portugal</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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