Crilvastatin, a new 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, inhibits cholesterol absorption in genetically hypercholesterolemic rats
Crilvastatin is a new drug from the pyrrolidone family, which acts as a non-competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. The long-term effects of oral crilvastatin treatment (200 mg per day per kg body weight for 4 and 10 weeks) were investigated on in vivo cholesterogen...
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| Veröffentlicht in: | European journal of pharmacology 1995-11, Vol.286 (2), p.131-136 |
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| creator | Hajri, Tahar Férézou, Jacqueline Laruelle, Claude Lutton, Claude |
| description | Crilvastatin is a new drug from the pyrrolidone family, which acts as a non-competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. The long-term effects of oral crilvastatin treatment (200 mg per day per kg body weight for 4 and 10 weeks) were investigated on in vivo cholesterogenesis in male adult normocholesterolemic (SW) and genetically hypercholesterolemic (RICO) rats. In both strains of rats, the treatment had no effect on the plasma cholesterol level, but efficiently inhibited cholesterol synthesis in liver and intestine, as shown by the decreased incorporation of exogenous [
14C]acetate into hepatic (3.5-fold in SW, 1.7-fold in RICO rats) and intestinal (2.5-fold in SW, 3.3-fold in RICO rats) sterols. In RICO rats in which the dietary cholesterol absorption coefficient was two-fold lower in treated (38%) than in untreated (78%) rats, this drug reduced intestinal cholesterol absorption. As a result, the total plasma cholesterol input (absorption + synthesis), measured by isotope analysis in RICO rats, was markedly lower in treated (11.3 mg per day) than in untreated animals (28.8 mg per day). |
| doi_str_mv | 10.1016/0014-2999(95)00437-P |
| format | Article |
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14C]acetate into hepatic (3.5-fold in SW, 1.7-fold in RICO rats) and intestinal (2.5-fold in SW, 3.3-fold in RICO rats) sterols. In RICO rats in which the dietary cholesterol absorption coefficient was two-fold lower in treated (38%) than in untreated (78%) rats, this drug reduced intestinal cholesterol absorption. As a result, the total plasma cholesterol input (absorption + synthesis), measured by isotope analysis in RICO rats, was markedly lower in treated (11.3 mg per day) than in untreated animals (28.8 mg per day).</description><identifier>ISSN: 0014-2999</identifier><identifier>EISSN: 1879-0712</identifier><identifier>DOI: 10.1016/0014-2999(95)00437-P</identifier><identifier>PMID: 8605949</identifier><identifier>CODEN: EJPHAZ</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Absorption ; Animals ; Anticholesteremic Agents - pharmacology ; Biological and medical sciences ; Cholesterol - metabolism ; Cholesterol synthesis ; Dual isotope blood ratio method ; Enzyme Inhibitors - pharmacology ; General and cellular metabolism. Vitamins ; Hydroxymethylglutaryl-CoA Reductase Inhibitors ; Hypercholesterolemia - drug therapy ; Hypercholesterolemia - metabolism ; Hypocholesterolemic drug ; Intestine ; Liver ; Male ; Medical sciences ; Occupancy principle ; Pharmacology. Drug treatments ; Proline - analogs & derivatives ; Proline - pharmacology ; Proline - therapeutic use ; Rats ; RICO rat</subject><ispartof>European journal of pharmacology, 1995-11, Vol.286 (2), p.131-136</ispartof><rights>1995</rights><rights>1996 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c386t-94edcbc8188423290e10d33d1091ffa1b14101a627204a546b33e77f8e78f22c3</citedby><cites>FETCH-LOGICAL-c386t-94edcbc8188423290e10d33d1091ffa1b14101a627204a546b33e77f8e78f22c3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/001429999500437P$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=2912227$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8605949$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Hajri, Tahar</creatorcontrib><creatorcontrib>Férézou, Jacqueline</creatorcontrib><creatorcontrib>Laruelle, Claude</creatorcontrib><creatorcontrib>Lutton, Claude</creatorcontrib><title>Crilvastatin, a new 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, inhibits cholesterol absorption in genetically hypercholesterolemic rats</title><title>European journal of pharmacology</title><addtitle>Eur J Pharmacol</addtitle><description>Crilvastatin is a new drug from the pyrrolidone family, which acts as a non-competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. The long-term effects of oral crilvastatin treatment (200 mg per day per kg body weight for 4 and 10 weeks) were investigated on in vivo cholesterogenesis in male adult normocholesterolemic (SW) and genetically hypercholesterolemic (RICO) rats. In both strains of rats, the treatment had no effect on the plasma cholesterol level, but efficiently inhibited cholesterol synthesis in liver and intestine, as shown by the decreased incorporation of exogenous [
14C]acetate into hepatic (3.5-fold in SW, 1.7-fold in RICO rats) and intestinal (2.5-fold in SW, 3.3-fold in RICO rats) sterols. In RICO rats in which the dietary cholesterol absorption coefficient was two-fold lower in treated (38%) than in untreated (78%) rats, this drug reduced intestinal cholesterol absorption. As a result, the total plasma cholesterol input (absorption + synthesis), measured by isotope analysis in RICO rats, was markedly lower in treated (11.3 mg per day) than in untreated animals (28.8 mg per day).</description><subject>Absorption</subject><subject>Animals</subject><subject>Anticholesteremic Agents - pharmacology</subject><subject>Biological and medical sciences</subject><subject>Cholesterol - metabolism</subject><subject>Cholesterol synthesis</subject><subject>Dual isotope blood ratio method</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>General and cellular metabolism. Vitamins</subject><subject>Hydroxymethylglutaryl-CoA Reductase Inhibitors</subject><subject>Hypercholesterolemia - drug therapy</subject><subject>Hypercholesterolemia - metabolism</subject><subject>Hypocholesterolemic drug</subject><subject>Intestine</subject><subject>Liver</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Occupancy principle</subject><subject>Pharmacology. Drug treatments</subject><subject>Proline - analogs & derivatives</subject><subject>Proline - pharmacology</subject><subject>Proline - therapeutic use</subject><subject>Rats</subject><subject>RICO rat</subject><issn>0014-2999</issn><issn>1879-0712</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1995</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kU2LFDEQhoMo6-zoP1DIQWSFjeaje9K5LCyDX7DgHvQc0unq7Ui6Mybp1faP-HfNOOPgyVMK6qlK8bwIPWP0NaNs84ZSVhGulLpQ9StKKyHJ7QO0Yo1UhErGH6LVCXmMzlP6SimtFa_P0FmzKVWlVujXNjp_b1I22U2X2OAJvmNBhqWL4cdCBBkhD4u_83M2cfHEBph-LiPgaxyhm202CbCbBte6HOLl3zJhOwQPKUMMHps2hbjLLkylj-9gguys8X7Bw7KD-A8Ko7M4mpyeoEe98QmeHt81-vLu7eftB3Lz6f3H7fUNsaLZZKIq6GxrG9Y0FRdcUWC0E6JjVLG-N6xlVXFlNlxyWpm62rRCgJR9A7LpObdijV4e9u5i-DaXK_TokgXvzQRhTlrKRjAuRQGrA2hjSClCr3fRjcWJZlTv89B72XovW6ta_8lD35ax58f9cztCdxo6BlD6L459k4qSPprJunTCuGKcl-_X6OqAQXFx7yDqZB1MFjoXwWbdBff_O34DvkOqUQ</recordid><startdate>19951114</startdate><enddate>19951114</enddate><creator>Hajri, Tahar</creator><creator>Férézou, Jacqueline</creator><creator>Laruelle, Claude</creator><creator>Lutton, Claude</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>19951114</creationdate><title>Crilvastatin, a new 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, inhibits cholesterol absorption in genetically hypercholesterolemic rats</title><author>Hajri, Tahar ; Férézou, Jacqueline ; Laruelle, Claude ; Lutton, Claude</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c386t-94edcbc8188423290e10d33d1091ffa1b14101a627204a546b33e77f8e78f22c3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1995</creationdate><topic>Absorption</topic><topic>Animals</topic><topic>Anticholesteremic Agents - pharmacology</topic><topic>Biological and medical sciences</topic><topic>Cholesterol - metabolism</topic><topic>Cholesterol synthesis</topic><topic>Dual isotope blood ratio method</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>General and cellular metabolism. Vitamins</topic><topic>Hydroxymethylglutaryl-CoA Reductase Inhibitors</topic><topic>Hypercholesterolemia - drug therapy</topic><topic>Hypercholesterolemia - metabolism</topic><topic>Hypocholesterolemic drug</topic><topic>Intestine</topic><topic>Liver</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Occupancy principle</topic><topic>Pharmacology. Drug treatments</topic><topic>Proline - analogs & derivatives</topic><topic>Proline - pharmacology</topic><topic>Proline - therapeutic use</topic><topic>Rats</topic><topic>RICO rat</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Hajri, Tahar</creatorcontrib><creatorcontrib>Férézou, Jacqueline</creatorcontrib><creatorcontrib>Laruelle, Claude</creatorcontrib><creatorcontrib>Lutton, Claude</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>European journal of pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Hajri, Tahar</au><au>Férézou, Jacqueline</au><au>Laruelle, Claude</au><au>Lutton, Claude</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Crilvastatin, a new 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, inhibits cholesterol absorption in genetically hypercholesterolemic rats</atitle><jtitle>European journal of pharmacology</jtitle><addtitle>Eur J Pharmacol</addtitle><date>1995-11-14</date><risdate>1995</risdate><volume>286</volume><issue>2</issue><spage>131</spage><epage>136</epage><pages>131-136</pages><issn>0014-2999</issn><eissn>1879-0712</eissn><coden>EJPHAZ</coden><abstract>Crilvastatin is a new drug from the pyrrolidone family, which acts as a non-competitive inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A reductase. The long-term effects of oral crilvastatin treatment (200 mg per day per kg body weight for 4 and 10 weeks) were investigated on in vivo cholesterogenesis in male adult normocholesterolemic (SW) and genetically hypercholesterolemic (RICO) rats. In both strains of rats, the treatment had no effect on the plasma cholesterol level, but efficiently inhibited cholesterol synthesis in liver and intestine, as shown by the decreased incorporation of exogenous [
14C]acetate into hepatic (3.5-fold in SW, 1.7-fold in RICO rats) and intestinal (2.5-fold in SW, 3.3-fold in RICO rats) sterols. In RICO rats in which the dietary cholesterol absorption coefficient was two-fold lower in treated (38%) than in untreated (78%) rats, this drug reduced intestinal cholesterol absorption. As a result, the total plasma cholesterol input (absorption + synthesis), measured by isotope analysis in RICO rats, was markedly lower in treated (11.3 mg per day) than in untreated animals (28.8 mg per day).</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>8605949</pmid><doi>10.1016/0014-2999(95)00437-P</doi><tpages>6</tpages></addata></record> |
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| ispartof | European journal of pharmacology, 1995-11, Vol.286 (2), p.131-136 |
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| source | MEDLINE; Elsevier ScienceDirect Journals Complete |
| subjects | Absorption Animals Anticholesteremic Agents - pharmacology Biological and medical sciences Cholesterol - metabolism Cholesterol synthesis Dual isotope blood ratio method Enzyme Inhibitors - pharmacology General and cellular metabolism. Vitamins Hydroxymethylglutaryl-CoA Reductase Inhibitors Hypercholesterolemia - drug therapy Hypercholesterolemia - metabolism Hypocholesterolemic drug Intestine Liver Male Medical sciences Occupancy principle Pharmacology. Drug treatments Proline - analogs & derivatives Proline - pharmacology Proline - therapeutic use Rats RICO rat |
| title | Crilvastatin, a new 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitor, inhibits cholesterol absorption in genetically hypercholesterolemic rats |
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