The Flavone Luteolin Inhibits Liver X Receptor Activation

被引:38
作者
Francisco, Vera [1 ,2 ]
Figueirinha, Artur [1 ,3 ]
Costa, Gustavo [1 ,3 ]
Liberal, Joana [1 ,2 ]
Ferreira, Isabel [2 ]
Lopes, Maria C. [1 ,3 ]
Garcia-Rodriguez, Carmen [4 ]
Cruz, Maria T. [1 ,3 ]
Batista, Maria T. [1 ,2 ,3 ]
机构
[1] Univ Coimbra, Ctr Neurosci & Cell Biol, P-3000214 Coimbra, Portugal
[2] Univ Coimbra, Fac Pharm, Ctr Pharmaceut Studies, Polo Ciencias Saude, Azinhaga Santa Comba, P-3000548 Coimbra, Portugal
[3] Univ Coimbra, Fac Pharm, Polo Ciencias Saude, Azinhaga Santa Comba, P-3000548 Coimbra, Portugal
[4] Univ Valladolid, CSIC, Inst Biol & Genet Mol, C Sanz y Fores 3, Valladolid 47003, Spain
来源
JOURNAL OF NATURAL PRODUCTS | 2016年 / 79卷 / 05期
关键词
PHARMACOLOGICAL ACTIVATION; INFLAMMATION; CHOLESTEROL; MODULATION; CELLS; ATHEROSCLEROSIS; LIPOGENESIS; REGULATORS; PATHWAYS; DISEASE;
D O I
10.1021/acs.jnatprod.6b00146
中图分类号
Q94 [植物学];
学科分类号
071001 ;
摘要
Luteolin is a dietary flavonoid with medicinal properties including antioxidant, antimicrobial, anticancer, antiallergic, and antiinflammatory. 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 LXR alpha/beta modulator, we investigated by realtime RT-PCR the expression of LXR-target genes, namely, sterol regulatory element binding protein lc (SREBP-lc) 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 LXR alpha/beta agonist-induced LXR alpha/beta 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.
引用
收藏
页码:1423 / 1428
页数:6
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