Quercetin Enhances VDR Activity, Leading to Stimulation of Its Target Gene Expression in Caco-2 Cells
Quercetin Enhances VDR Activity, Leading to Stimulation of Its Target Gene Expression in Caco-2 Cells
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DOI：
10.3177/jnsv.56.326
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发表时间：
2010-10-01
影响因子：
1.6
通讯作者：
Sato, Ryuichiro
中科院分区：
文献类型：
--
作者：
Inoue, Jun;Choi, Jung-Min;Sato, Ryuichiro
维生素D受体（VDR）是一种调节钙稳态相关基因表达的核受体。VDR的激活被认为是骨质疏松症的一个有前途的药物靶点。使用VDR驱动的荧光素酶表达试验筛选天然存在的食品成分，我们确定槲皮素作为VDR激活剂。槲皮素还激活与VDR配体结合结构域融合的GAL 4 DNA结合结构域。而且。证实了槲皮素增加Caco-2细胞中VDR靶基因TRPV 6的mRNA水平。这些结果表明，槲皮素通过改变辅因子募集来增强VDR活性，从而刺激其靶基因，同时为槲皮素作为VDR激活剂提供新的功能。
Vitamin D receptor (VDR) is a nuclear receptor that regulates the expression of genes involved in calcium homeostasis. Activation of VDR is thought to be a promising drug target for osteoporosis. Using a VDR-driven luciferase expression assay for screening a naturally occurring food component, we identified quercetin as a VDR activator. Quercetin also activated the GAL4 DNA-binding domain fused to the VDR ligand-binding domain. Moreover. it was confirmed that quercetin increases the mRNA level of TRPV6, which is a VDR target gene, in Caco-2 cells. These results indicate that quercetin enhances VDR activity through the alteration of cofactor recruitment, thereby stimulating its target genes while providing a new function for quercetin as the VDR activator.