Inhibition of 11 beta-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui

CORC > 昆明植物研究所 > 中国科学院昆明植物研究所 > 植物化学与西部植物资源持续利用国家重点实验室

	Inhibition of 11 beta-HSD1 by Tetracyclic Triterpenoids from Euphorbia kansui
	Guo, Jie 1,2,3,4; Zhou, Li-Yan 2,3,4; He, Hong-Ping 1; Leng, Ying ; Yang, Zhen 2,3,4; Hao, Xiao-Jiang1
刊名	MOLECULES
	2012-10-01
卷号	17 期号:10 页码:11826-11838
关键词	tetracyclic triterpenoids Euphorbia kansui inhibition of 11 beta-HSD1 docking
ISSN号	1420-3049
通讯作者	Hao, XJ (reprint author), Chinese Acad Sci, State Key Lab Phytochem & Plant Resources W China, Kunming Inst Bot, Kunming 650204, Yunnan, Peoples R China.,guojie@pkusz.edu.cn ; zhouly@pkusz.edu.cn ; hehongping@mail.kib.ac.cn ; yleng@mail.shcnc.ac.cn ; zyang@pku.edu.cn ; haoxj@mail.kib.ac.cn
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.
学科主题	Chemistry, Organic
类目[WOS]	Chemistry, Organic
研究领域[WOS]	Chemistry
关键词[WOS]	11-BETA-HYDROXYSTEROID DEHYDROGENASE TYPE-1 ; DITERPENOIDS ; EUPHANE
收录类别	SCI
语种	英语
WOS记录号	WOS:000310505400037
公开日期	2013-01-22
内容类型	期刊论文
源URL	[http://ir.kib.ac.cn/handle/151853/15942]
专题	昆明植物研究所_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
推荐引用方式 GB/T 7714	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.