Jatrophane diterpenoids from Euphorbia helioscopia and their lipid-lowering activities
文献类型：期刊论文
| 作者 | Li, Jun2,3 ; Li, Hui-hui1,3; Wang, Wen-qiong2; Song, Wei-bin2; Wang, Yi-ping1; Xuan, Li-jiang2
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| 刊名 | FITOTERAPIA
 |
| 出版日期 | 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. |
| WOS关键词 | RECEPTOR MESSENGER-RNA ; MULTIDRUG-RESISTANCE ; MODULATORS ; LDL ; ATHEROSCLEROSIS ; HYPERLIPIDEMIA ; STABILIZATION ; AGENTS ; CELLS |
| 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研究方向 | Pharmacology & Pharmacy |
| 语种 | 英语 |
| WOS记录号 | WOS:000437076200017 |
| 出版者 | ELSEVIER SCIENCE BV |
| 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. |
入库方式： OAI收割
来源：上海药物研究所
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