A novel compound N-1, N-5-(Z)-N-10-(E)-tri-p-coumaroylspermidine isolated from Carthamus tinctorius L. and acting by serotonin transporter inhibition
文献类型：期刊论文
| 作者 | Zhao, Gang2,3; Gai, Yue2; Chu, Wen-Jing2; Qin, Guo-Wei1; Guo, Li-He2,3 |
| 刊名 | EUROPEAN NEUROPSYCHOPHARMACOLOGY
 |
| 出版日期 | 2009-10 |
| 卷号 | 19期号:10页码:749-758 |
| 关键词 | Safflower N-1,N-5-(Z)-N-10-(E)-tri-p-coumaroylspermidine Serotonin transporter Reuptake Inhibitor |
| ISSN号 | 0924-977X |
| DOI | 10.1016/j.euroneuro.2009.06.009 |
| 文献子类 | Article |
| 英文摘要 | Safflower, the dry flower of Carthamus tinctorius L., has long been applied for empirically treating cerebral ischemia and depression in traditional Chinese medicine. Pathogenesis of major depression involves monoaminergic transmission. The present study assessed whether safflower or its isolate would be effective in functionally regulating monoamine transporter using in vitro screening cell lines. We discovered that safflower insoluble fraction significantly inhibited serotonin uptake in Chinese hamster ovary cells stably expressing serotonin transporter (i.e. S6 cells). This fraction went through an activity-guided isolation and an active ingredient was obtained, which was subsequently elucidated as a novel coumaroylspermidine analog N-1,N-5-(Z)-N-10-(E)-tri-p-coumaroylspermidine using NMR techniques. Pharmacologically, this compound potently and selectively inhibited serotonin uptake in S6 cells or in synaptosomes, with IC50 of 0.74 +/- 0.15 mu M for S6 cells or 1.07 +/- 0.23 mu M for synaptosomes and with a reversible competitive property for the 5HT-uptake inhibition. The potency of it for 5HT uptake was weaker than that of fluoxetine whereas efficacy generally similar for both. Animals treated with this testing compound showed a significant decrease in synaptosomal 5HT uptake capacity. Thus, N-1,N-5-(Z)N-10-(E)-tri-p-coumaroylspermidine is a novel serotonin transporter inhibitor, which could improve neuropsychological disorders through regulating serotoninergic transmission. (C) 2009 Elsevier B.V. and ECNP. All rights reserved. |
| WOS关键词 | HYDROXYSAFFLOR-YELLOW ; DOPAMINE TRANSPORTER ; MONOAMINE TRANSPORTERS ; LINOLENIC ACID ; RAT-BRAIN ; OIL CAKE ; IN-VITRO ; SAFFLOWER ; DERIVATIVES ; ANXIETY |
| 资助项目 | Shanghai Government[05DZ19339] ; Chinese Academy of Science[00000000] |
| WOS研究方向 | Neurosciences & Neurology ; Pharmacology & Pharmacy ; Psychiatry |
| 语种 | 英语 |
| WOS记录号 | WOS:000270312300009 |
| 出版者 | ELSEVIER SCIENCE BV |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/279114]  |
| 专题 | 天然药物化学研究室 |
| 通讯作者 | Guo, Li-He |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Mat Med, Shanghai 201203, Peoples R China 2.Cell Star Biotechnol Co Ltd, Shanghai 201203, Peoples R China; 3.Chinese Acad Sci, Shanghai Inst Biol Sci, Inst Biochem & Cell Biol, Shanghai 200031, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Zhao, Gang,Gai, Yue,Chu, Wen-Jing,et al. A novel compound N-1, N-5-(Z)-N-10-(E)-tri-p-coumaroylspermidine isolated from Carthamus tinctorius L. and acting by serotonin transporter inhibition[J]. EUROPEAN NEUROPSYCHOPHARMACOLOGY,2009,19(10):749-758. |
| APA | Zhao, Gang,Gai, Yue,Chu, Wen-Jing,Qin, Guo-Wei,&Guo, Li-He.(2009).A novel compound N-1, N-5-(Z)-N-10-(E)-tri-p-coumaroylspermidine isolated from Carthamus tinctorius L. and acting by serotonin transporter inhibition.EUROPEAN NEUROPSYCHOPHARMACOLOGY,19(10),749-758. |
| MLA | Zhao, Gang,et al."A novel compound N-1, N-5-(Z)-N-10-(E)-tri-p-coumaroylspermidine isolated from Carthamus tinctorius L. and acting by serotonin transporter inhibition".EUROPEAN NEUROPSYCHOPHARMACOLOGY 19.10(2009):749-758. |
入库方式： OAI收割
来源：上海药物研究所
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