Synthesis and their inhibitory activities of neuroinflammation of dehydroepiandrosterone derivatives
文献类型：期刊论文
| 作者 | Wang Youfu1; Wang Rong1; Wang Junliang1; Feng Huijin2 ; Yang Yaxi2; Li Yuanchao2
|
| 刊名 | Chinese Journal of Medicinal Chemistry
 |
| 出版日期 | 2016 |
| 卷号 | 26期号:5页码:353-360 |
| 关键词 | dehydroepiandrosterone neuroinflammation nitric monoxide(NO) amino acid |
| ISSN号 | 1005-0108 |
| 其他题名 | 去氢表雄酮衍生物的合成及其抑制神经炎症活性研究 |
| 文献子类 | Article |
| 英文摘要 | Glial activation mediated neuroinflammation plays a pivotal role in the process of several neuroinflammatory diseases including stroke,Alzheimer' s diseases,Parkinson' s diseases,multiple sclerosis and ischemia. Inhibition of microglial activation may ameliorate neuronal degeneration under the inflammatory conditions. In the present study,a series of dehydroepiandrosterone derivatives were designed and synthesized. The anti-inflammatory effects of these compounds were evaluated using LPS-stimulated BV-2 microglia cells. Those derivatives were prepared from readily available dehydroepiandrosterone and its downstream product 15beta,16beta-cyclopropane-dehydroepiandrosterone incorporating amino acid methyl esters at C-3 hydroxyl group,and oxidation at C-4 or C-7 position. Among all the 16 compounds, several analogs exhibited potent inhibitory activities on nitric oxide production(inhibition rate > 75%) with no or weak cell toxi city at 20 mumol·L~(- 1). The related SARs and function mechanism is worth further research and discussion. |
| WOS研究方向 | Pharmacology & Pharmacy (provided by Clarivate Analytics) |
| 语种 | 中文 |
| CSCD记录号 | CSCD:5834451 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/269230]  |
| 专题 | 药物化学研究室 |
| 通讯作者 | Yang Yaxi |
| 作者单位 | 1.Zhejiang Shenzhou Pharmaceutical Co.,Ltd., Xianju, 317300.; 2.Shanghai Institute of Materia Medica,Chinese Academy of Sciences, Shanghai 201203, China. |
| 推荐引用方式 GB/T 7714 | Wang Youfu,Wang Rong,Wang Junliang,et al. Synthesis and their inhibitory activities of neuroinflammation of dehydroepiandrosterone derivatives[J]. Chinese Journal of Medicinal Chemistry,2016,26(5):353-360. |
| APA | Wang Youfu,Wang Rong,Wang Junliang,Feng Huijin,Yang Yaxi,&Li Yuanchao.(2016).Synthesis and their inhibitory activities of neuroinflammation of dehydroepiandrosterone derivatives.Chinese Journal of Medicinal Chemistry,26(5),353-360. |
| MLA | Wang Youfu,et al."Synthesis and their inhibitory activities of neuroinflammation of dehydroepiandrosterone derivatives".Chinese Journal of Medicinal Chemistry 26.5(2016):353-360. |
入库方式： OAI收割
来源：上海药物研究所
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