Inhibition of cholesterol biosynthesis by Δ22-unsaturated phytosterols via competitive inhibition of sterol Δ24-reductase in mammalian cells
FERNÁNDEZ C, SUÁREZ Y, FERRUELO AJ, GÓMEZ-CORONADO D, LASUNCIÓN MA. Inhibition of cholesterol biosynthesis by Δ22-unsaturated phytosterols via competitive inhibition of sterol Δ24-reductase in mammalian cells. Biochemical Journal 2002, 366: 109-119. PMID: 12162789, PMCID: PMC1222779, DOI: 10.1042/bj20011777.Peer-Reviewed Original ResearchMeSH KeywordsAnimalsBinding, CompetitiveCaco-2 CellsCholesterolChromatography, High Pressure LiquidDose-Response Relationship, DrugHL-60 CellsHumansHypolipidemic AgentsKineticsMacrophagesMaleMiceMicrosomes, LiverModels, ChemicalOxidoreductasesPhytosterolsRatsRats, Sprague-DawleyStigmasterolTime FactorsTumor Cells, CulturedConceptsCholesterol biosynthesisCholesterol-lowering actionCholesterol-lowering agentsEffective hypocholesterolaemic agentHL-60 human cell linesRat liver microsomesIntestinal absorptionDietary phytosterolsLiver microsomesHypocholesterolaemic agentsLow intracellular concentrationsCaco-2Inhibition of sterolIncorporation of radioactivityHuman cell linesCell linesInhibitionSaturated side chainIntracellular concentrationCholesterolRelevant concentrationsRadioactivity incorporationPresent studyStrong inhibitionCompetitive inhibition