HMG-CoA reductase activity in human liver microsomes: comparative inhibition by statins

The aim of this study was to compare a number of vastatins, HMG-CoA reductase inhibitors, in human liver microsomes.HMG-CoA reductase activity was four times lower than the activity in untreated rat liver microsomes.Vastatins could be classified in this in vitro assay in three classes both in human...

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Bibliographic Details
Published in:Experimental and toxicologic pathology : official journal of the Gesellschaft für Toxikologische Pathologie 2000-05, Vol.52 (2), p.145-148
Main Authors: Dansette, P.M., Jaoen, M., Pons, C.
Format: Article
Language:English
Subjects:
Animals
Atorvastatin Calcium
Biological and medical sciences
Fatty Acids, Monounsaturated - pharmacology
General and cellular metabolism. Vitamins
Heptanoic Acids - pharmacology
HMG-CoA reductase
Humans
Hydroxymethylglutaryl CoA Reductases - metabolism
Hydroxymethylglutaryl-CoA Reductase Inhibitors - pharmacology
Indoles - pharmacology
Liver microsomes
Lovastatin - pharmacology
Male
Medical sciences
Microsomes, Liver - enzymology
Pharmacology. Drug treatments
Pravastatin - pharmacology
Pyridines - pharmacology
Pyrroles - pharmacology
Rats
Rats, Sprague-Dawley
Simvastatin - pharmacology
Species Specificity
Vastatins
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Summary:The aim of this study was to compare a number of vastatins, HMG-CoA reductase inhibitors, in human liver microsomes.HMG-CoA reductase activity was four times lower than the activity in untreated rat liver microsomes.Vastatins could be classified in this in vitro assay in three classes both in human and rat microsomes: the first one including cerivastatin with an IC50 of 6 nM, the second one with atorvastatin and fluvastatin (IC50) between 40 and 100 nM) and the third one containing pravastatin, simvastatin and lovastatin (IC50 between 100 and 300 nM).
ISSN:0940-2993
1618-1433
DOI:10.1016/S0940-2993(00)80107-4