Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea
Anti-hyperglycemic activity of a TGR5 agonist isolated from Olea europaea
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DOI：
10.1016/j.bbrc.2007.06.130
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发表时间：
2007-11-03
影响因子：
3.1
通讯作者：
Saladin, Regis
中科院分区：
文献类型：
--
作者：
Sato, Hiroyuki;Genet, Cedric;Saladin, Regis
橄榄树（Olea europeaea）叶因其对代谢的作用而众所周知，特别是作为传统的抗糖尿病和抗高血压草药。这些性质到目前为止只归因于橄榄苦苷，橄榄叶的主要开环环烯醚萜。在这里，我们描述了另一种成分的分离和鉴定，这种植物的抗糖尿病作用，即油酸。我们发现，这种三萜是TGR 5的激动剂，TGR 5是由胆汁酸激活的G蛋白偶联受体的成员，并介导它们的各种细胞和生理效应。油酸可降低高脂饮食喂养小鼠的血清葡萄糖和胰岛素水平，并增强葡萄糖耐量。我们的数据表明橄榄苦苷和油酸都参与了橄榄叶的抗糖尿病作用，并进一步强调了TGR 5激动剂改善代谢紊乱的潜在作用。(c)2007爱思唯尔公司All rights reserved.
Olive tree (Olea europeaea) leaves are well known for their effect on metabolism in particular as a traditional anti-diabetic and antihypertensive herbal drug. These properties are until now only attributed to oleuropein, the major secoiridoid of olive leaves. Here we describe the isolation and the identification of another constituent implicated in the anti-diabetic effect of this plant, i.e. oleanolic acid. We show that this triterpene is an agonist for TGR5, a member of G-protein coupled receptor activated by bile acids and which mediates some of their various cellular and physiological effect. Oleanolic acid lowers serum glucose and insulin levels in mice fed with a high fat diet and it enhances glucose tolerance. Our data suggest that both oleuropein and oleanolic acid are involved in the anti-diabetic effect of olive leaves and further emphasize the potential role of TGR5 agonists to improve metabolic disorders. (c) 2007 Elsevier Inc. All rights reserved.