Dietary flavonoids activate the constitutive androstane receptor (CAR).
Dietary flavonoids activate the constitutive androstane receptor (CAR).
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DOI：
10.1021/jf903711q
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发表时间：
2010-02-24
影响因子：
6.1
通讯作者：
Abe K
中科院分区：
文献类型：
--
作者：
Yao R;Yasuoka A;Kamei A;Kitagawa Y;Tateishi N;Tsuruoka N;Kiso Y;Sueyoshi T;Negishi M;Misaka T;Abe K
组成型雄甾烷受体（CAR）被称为异种传感器，可调节参与异种物质排泄和能量代谢的基因。这项研究测试了多种多酚调节 CAR 活性的能力。 HepG2细胞用CAR表达质粒和含有人CYP2B6调节区的报告质粒转染，然后用类黄酮、儿茶素和其他生物活性多酚处理。荧光素酶测定表明，黄芩素（5,6,7-OH 黄酮）是人和小鼠 CAR 的有效激活剂。儿茶素没食子酸酯还可以激活人和小鼠的 CAR。用黄芩素和白杨素（5, 7-OH黄酮）处理野生型和CAR基因敲除小鼠，并通过实时PCR分析它们的肝脏mRNA。仅在喂食白杨素的野生型小鼠中观察到 cyp2b10 mRNA 含量显着增加。这些结果表明，膳食黄酮类化合物可调节 CAR 活性，从而加速解毒和能量代谢。
The constitutive androstane receptor (CAR) is known as a xeno-sensor that regulates genes involved in xenobiotic excretion and energy metabolism. This study tested a variety of polyphenols for their ability to modulate CAR activity. HepG2 cells were transfected with a CAR expression plasmid and a reporter plasmid containing the human CYP2B6 regulatory region and then treated with flavonoids, catechins and other bioactive polyphenols. Luciferase assays revealed that baicalein (5, 6, 7-OH flavone) was a potent activator of both human and mouse CAR. Catechin gallates also activated human and mouse CAR. Wild-type and CAR knockout mice were treated with baicalein and chrysin (5, 7-OH flavone), and their liver mRNA was analyzed by real-time PCR. A significant increase in cyp2b10 mRNA content was observed only in wild-type mice fed chrysin. These results suggest that dietary flavonoids regulate CAR activity and thereby accelerate both detoxification and energy metabolism.
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影响因子：
10.4
作者：
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通讯作者：
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影响因子：
5.3
作者：
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影响因子：
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作者：
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发表时间：
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影响因子：
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作者：
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通讯作者：
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影响因子：
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作者：
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