Jatrophane diterpenoids from Euphorbia helioscopia and their lipid-lowering activities

doi:10.1016/j.fitote.2018.05.007

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	Jatrophane diterpenoids from Euphorbia helioscopia and their lipid-lowering activities
	Li, Jun2,3 ; Li, Hui-hui 1,3; Wang, Wen-qiong 2; Song, Wei-bin 2; Wang, Yi-ping1 ; Xuan, Li-jiang2
刊名	FITOTERAPIA
	2018-07
卷号	128 页码:102-111
关键词	Euphorbia helioscopia Jatrophanes Hyperlipidemia Lipid-lowering LDL receptor
ISSN号	0367-326X
DOI	10.1016/j.fitote.2018.05.007
文献子类	Article
英文摘要	The phytochemical study of Euphorbia helioscopia led to the isolation of 33 jatrophane diterpenoids (1-33), of which six (1-6) were new. This small jatrophane library was established to screen for potential lipid modulators. LDL-Uptake screening assay demonstrated that most of them improved LDL-Uptake rate in HepG2 cells, with compounds 16, 21 and 26 exhibiting more outstanding effects. Further exploration found that these three compounds could increase LDLR protein level in HepG2 cells dose-dependently. SAR studies suggested that substituted patterns of C-9, steric hindrance between C-14 and C-15, and the long conjugated fragment from C-5 to the carbonyl (C-9) were essential for the activity. Moreover, compound 21, a relatively abundant chemical in E. helioscopia, showed remarkable lipid-lowering effect in vivo, which makes it a promising lead for development of new lipid-lowering agents.
资助项目	State Key Laboratory of Drug Research[SIMM1601ZZ-03] ; National Natural Science Foundation of China[81773863] ; National Natural Science Foundation of China[21702219]
WOS关键词	RECEPTOR MESSENGER-RNA ; MULTIDRUG-RESISTANCE ; MODULATORS ; LDL ; ATHEROSCLEROSIS ; HYPERLIPIDEMIA ; STABILIZATION ; AGENTS ; CELLS
WOS研究方向	Pharmacology & Pharmacy
语种	英语
出版者	ELSEVIER SCIENCE BV
WOS记录号	WOS:000437076200017
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/279684]
专题	药理学第一研究室中科院受体结构与功能重点实验室新药研究国家重点实验室上海中药现代化研究中心所领导
通讯作者	Wang, Yi-ping; Xuan, Li-jiang
作者单位	1.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China; 2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 501 Haike Rd, Shanghai 201203, Peoples R China; 3.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
推荐引用方式 GB/T 7714	Li, Jun,Li, Hui-hui,Wang, Wen-qiong,et al. Jatrophane diterpenoids from Euphorbia helioscopia and their lipid-lowering activities[J]. FITOTERAPIA,2018,128:102-111.
APA	Li, Jun,Li, Hui-hui,Wang, Wen-qiong,Song, Wei-bin,Wang, Yi-ping,&Xuan, Li-jiang.(2018).Jatrophane diterpenoids from Euphorbia helioscopia and their lipid-lowering activities.FITOTERAPIA,128,102-111.
MLA	Li, Jun,et al."Jatrophane diterpenoids from Euphorbia helioscopia and their lipid-lowering activities".FITOTERAPIA 128(2018):102-111.