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题名: Inhibition of 11 beta-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui
作者: Guo, Jie1, 2, 3, 4; Zhou, Li-Yan2, 3, 4; He, Hong-Ping1; Leng, Ying; Yang, Zhen2, 3, 4; null(郝小江)1
刊名: MOLECULES
关键词: tetracyclic triterpenoids ; Euphorbia kansui ; inhibition of 11 beta-HSD1 ; docking
英文摘要: The roots of Euphorbia kansui are considered an important traditional folk medicine. In this study the ethanol extracts of E. kansui were investigated. A new tetracyclic triterpenoid, euphane-3 beta,20-dihydroxy-24-ene, in addition to five known triterpenoids with euphane skeletons were isolated. Their structures were elucidated on the basis of physical and spectral techniques (1D-, 2D-NMR and MS, respectively). Furthermore, these compounds 1-6 exhibited strong inhibitory activity against human 11 beta-hydroxysteroid dehydrogenase type 1 (11 beta-HSD1), with IC50 values of 34.86 nM, 1.115 mu M, 16.08 nM, 2.815 nM, 26.47 nM, 15.99 nM, and 41.86 nM, respectively. The docking results show that the ring part of compounds can insert into the hydrophobic core of h11 beta-HSD1 and the alkane chain orientates toward the outside. The results presented herein provide a scientific explanation for the usage of the E. kansui in clinical treatment of diabetes.
出版日期: 2012-10-01
卷号: 17, 期号:10, 页码:11826-11838
语种: 英语
收录类别: SCI
学科分类: Chemistry, Organic
ISSN号: 1420-3049
Citation statistics:
内容类型: 期刊论文
URI标识: http://ir.kib.ac.cn/handle/151853/15942
Appears in Collections:植物化学与西部植物资源持续利用国家重点实验室_期刊论文

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作者单位: 1.Chinese Acad Sci, State Key Lab Phytochem & Plant Resources W China, Kunming Inst Bot, Kunming 650204, Yunnan, Peoples R China
2.Peking Univ, Shenzhen Grad Sch, Sch Chem Biol & Biotechnol, Lab Chem Genom, Shenzhen 518055, Guangdong, Peoples R China
3.Peking Univ, Coll Chem, Beijing Natl Lab Mol Sci, Beijing 100871, Peoples R China
4.Peking Univ, Minist Educ, Key Lab Bioorgan Chem & Mol Engn, Beijing 100871, Peoples R China

Recommended Citation:
Guo, Jie; Zhou, Li-Yan; He, Hong-Ping; Leng, Ying; Yang, Zhen; Hao, Xiao-Jiang.Inhibition of 11 beta-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui,MOLECULES,2012,17(10):11826-11838
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