Potential AMPK activators of cucurbitane triterpenoids from Siraitia grosvenorii Swingle
Potential AMPK activators of cucurbitane triterpenoids from Siraitia grosvenorii Swingle
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DOI：
10.1016/j.bmc.2011.08.030
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发表时间：
2011-10-01
影响因子：
3.5
通讯作者：
Hu, Li-hong
中科院分区：
文献类型：
--
作者：
Chen, Xu-bing;Zhuang, Jing-jing;Hu, Li-hong
腺苷酸活化蛋白激酶（AMPK）作为全身能量稳态调节的关键调控因子，在保护机体免受代谢性疾病侵害方面发挥着重要作用。近期，在几种用从罗汉果果实中分离出的粗罗汉果甜苷治疗的糖尿病啮齿动物模型中，观察到葡萄糖利用改善、脂质利用改善以及胰岛素敏感性提高，但该植物中负责抗糖尿病活性的精确活性化合物尚未明确确定。在我们目前的工作中，粗罗汉果甜苷经酸水解得到了5种新的葫芦烷型三萜类化合物（1 - 4，8）以及3种已知的化合物（5 - 7）。主要苷元罗汉果醇（7）以及化合物4和8在HepG2细胞系中被发现是有效的AMPK激活剂。这一结果表明，罗汉果甜苷苷元7和8对AMPK的激活被证明至少部分有助于罗汉果在体内的抗高血糖和抗高血脂特性。（C）2011爱思唯尔有限公司。保留所有权利。
AMP-activated kinase (AMPK) as a key controller in the regulation of whole-body energy homeostasis, plays an important role in protecting the body from metabolic diseases. Recently, improved glucose, lipid utility and increased insulin sensitivity were observed on several diabetic rodent models treated with crude mogrosides isolated from the fruit of Siraitia grosvenorii Swingle, but the precise active compounds responsible for the anti-diabetic activity of this plant have not been clearly identified. In our current work, acid hydrolysis of crude mogrosides provided five new cucurbitane triterpenoids (1-4, 8), along with three known ones (5-7). The main aglycone mogrol (7) and compounds 4 and 8 were found to be potent AMPK activators in the HepG2 cell line. This result suggested AMPK activation by the mogroside aglycones 7 and 8 was proved to contribute at least partially to the anti-hyperglycemic and anti-lipidemic properties in vivo of S. grosvenorii. (C) 2011 Elsevier Ltd. All rights reserved.