Inhibition of 11 beta-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui
Guo, Jie1,2,3,4; Zhou, Li-Yan2,3,4; He, Hong-Ping1; Leng, Ying; Yang, Zhen2,3,4; Hao, Xiao-Jiang1
2012-10-01
发表期刊MOLECULES
ISSN1420-3049
卷号17期号:10页码:11826-11838
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.
关键词Tetracyclic Triterpenoids Euphorbia Kansui Inhibition Of 11 Beta-hsd1 Docking
收录类别SCI
语种英语
引用统计
文献类型期刊论文
条目标识符http://ir.kib.ac.cn/handle/151853/15942
专题植物化学与西部植物资源持续利用国家重点实验室
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
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Guo, Jie,Zhou, Li-Yan,He, Hong-Ping,et al. Inhibition of 11 beta-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui[J]. MOLECULES,2012,17(10):11826-11838.
APA Guo, Jie,Zhou, Li-Yan,He, Hong-Ping,Leng, Ying,Yang, Zhen,&Hao, Xiao-Jiang.(2012).Inhibition of 11 beta-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui.MOLECULES,17(10),11826-11838.
MLA Guo, Jie,et al."Inhibition of 11 beta-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui".MOLECULES 17.10(2012):11826-11838.
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