Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism
Ursolic acid is a PPAR-α agonist that regulates hepatic lipid metabolism
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DOI：
10.1016/j.bmcl.2011.07.095
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发表时间：
2011-10-01
影响因子：
2.7
通讯作者：
Lee, Sung-Joon
中科院分区：
文献类型：
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作者：
Jia, Yaoyao;Bhuiyan, Muhammad Javidul Haque;Lee, Sung-Joon
在这项研究中，我们证实了熊果酸，一种植物三萜类，激活过氧化物酶体增殖物激活受体（PPAR）-α在体外。表面等离子体共振和时间分辨荧光共振能量转移分析未显示熊果酸与PPAR-alpha的配体结合结构域直接结合;然而，熊果酸增强PPAR-alpha与PPAR-alpha响应基因中过氧化物酶体增殖物响应元件的结合，改变脂质代谢中关键基因的表达，显著降低肝细胞内甘油三酯和胆固醇浓度。因此，熊果酸是一种PPAR-alpha激动剂，可调节脂质代谢基因的表达，但不是PPAR-alpha的直接配体。(C)2011爱思唯尔有限公司保留所有权利。
In this study, we confirmed that ursolic acid, a plant triterpenoid, activates peroxisome proliferator-activated receptor (PPAR)-alpha in vitro. Surface plasmon resonance and time-resolved fluorescence resonance energy transfer analyses do not show direct binding of ursolic acid to the ligand-binding domain of PPAR-alpha; however, ursolic acid enhances the binding of PPAR-alpha to the peroxisome proliferator response element in PPAR-alpha-responsive genes, alters the expression of key genes in lipid metabolism, significantly reducing intracellular triglyceride and cholesterol concentrations in hepatocytes. Thus, ursolic acid is a PPAR-alpha agonist that regulates the expression of lipid metabolism genes, but it is not a direct ligand of PPAR-alpha. (C) 2011 Elsevier Ltd. All rights reserved.