title: The Flavone Luteolin Inhibits Liver X Receptor Activation.
abstract: Luteolin is a dietary flavonoid with medicinal properties including antioxidant, antimicrobial, anticancer, antiallergic, and anti-inflammatory. However, the effect of luteolin on liver X receptors (LXRs), oxysterol sensors that regulate cholesterol homeostasis, lipogenesis, and inflammation, has yet to be studied. To unveil the potential of luteolin as an LXRα/β modulator, we investigated by real-time RT-PCR the expression of LXR-target genes, namely, sterol regulatory element binding protein 1c (SREBP-1c) in hepatocytes and ATP-binding cassette transporter (ABC)A1 in macrophages. The lipid content of hepatocytes was evaluated by Oil Red staining. The results demonstrated, for the first time, that luteolin abrogated the LXRα/β agonist-induced LXRα/β transcriptional activity and, consequently, inhibited SREBP-1c expression, lipid accumulation, and ABCA1 expression. Therefore, luteolin could abrogate hypertriglyceridemia associated with LXR activation, thus presenting putative therapeutic effects in diseases associated with deregulated lipid metabolism, such as hepatic steatosis, cardiovascular diseases, and diabetes.
authors.affiliation: Center for Neurosciences and Cell Biology, University of Coimbra , 3000-214 Coimbra, Portugal.|Center for Pharmaceutical Studies, Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
authors.forename: Vera
authors.initials: V
authors.lastname: Francisco
authors.affiliation: Center for Neurosciences and Cell Biology, University of Coimbra , 3000-214 Coimbra, Portugal.|Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
authors.forename: Artur
authors.initials: A
authors.lastname: Figueirinha
authors.affiliation: Center for Neurosciences and Cell Biology, University of Coimbra , 3000-214 Coimbra, Portugal.|Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
authors.forename: Gustavo
authors.initials: G
authors.lastname: Costa
authors.affiliation: Center for Neurosciences and Cell Biology, University of Coimbra , 3000-214 Coimbra, Portugal.|Center for Pharmaceutical Studies, Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
authors.forename: Joana
authors.initials: J
authors.lastname: Liberal
authors.affiliation: Center for Pharmaceutical Studies, Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
authors.forename: Isabel
authors.initials: I
authors.lastname: Ferreira
authors.affiliation: Center for Neurosciences and Cell Biology, University of Coimbra , 3000-214 Coimbra, Portugal.|Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
authors.forename: Maria C
authors.initials: MC
authors.lastname: Lopes
authors.affiliation: Instituto de Biología y Genética Molecular, Universidad de Valladolid-CSIC , C/Sanz y Forés 3, 47003 Valladolid, Spain.
authors.forename: Carmen
authors.initials: C
authors.lastname: García-Rodríguez
authors.affiliation: Center for Neurosciences and Cell Biology, University of Coimbra , 3000-214 Coimbra, Portugal.|Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
authors.forename: Maria T
authors.initials: MT
authors.lastname: Cruz
authors.affiliation: Center for Neurosciences and Cell Biology, University of Coimbra , 3000-214 Coimbra, Portugal.|Center for Pharmaceutical Studies, Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.|Faculty of Pharmacy, University of Coimbra , Pólo das Ciências da Saúde, Azinhaga de Santa Comba, 3000-548 Coimbra, Portugal.
authors.forename: Maria T
authors.initials: MT
authors.lastname: Batista
mesh_terms: D000975:Antioxidants / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D047309:Flavones / Q000494:pharmacology*; D056945:Hep G2 Cells; D022781:Hepatocytes / Q000187:drug effects; D006801:Humans; D050356:Lipid Metabolism; D008099:Liver / Q000187:drug effects; D000071518:Liver X Receptors / Q000037:antagonists & inhibitors*; D047311:Luteolin / Q000737:chemistry / Q000494:pharmacology*; D015394:Molecular Structure; D016133:Polymerase Chain Reaction; D051780:Sterol Regulatory Element Binding Protein 1 / Q000187:drug effects
chemical_list: D000975:Antioxidants; D047309:Flavones; D000071518:Liver X Receptors; D051780:Sterol Regulatory Element Binding Protein 1; D047311:Luteolin