Synthesis of 5 alpha-cholestan-6-one derivatives and their inhibitory activities of NO production in activated microglia: Discovery of a novel neuroinflammation inhibitor
文献类型：期刊论文
| 作者 | Yang, Ya-Xi2 ; Zheng, Long-Tai3; Shi, Jing-Jing2; Gao, Bo3; Chen, Yan-Ke3; Yang, Hui-Chi3; Chen, Hong-Li1; Li, Yuan-Chao2; Zhen, Xue-Chu3
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2014-02-15 |
| 卷号 | 24期号:4页码:1222-1227 |
| ISSN号 | 0960-894X |
| 关键词 | Neuroinflammation Microglia Focal cerebral ischemia 5 alpha-Cholestan-6-one Nitric oxide |
| DOI | 10.1016/j.bmcl.2013.12.055 |
| 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 number of 5 alpha-cholestan-6-one derivatives were prepared and the anti-inflammatory effects of these compounds were evaluated in LPS-stimulated BV-2 microglia cells. Those derivatives were synthesized from readily available hyodeoxycholic acid (1). Among the tested compounds, several analogs (16-18, 25, 35, 38) exhibited potent inhibitory activities on nitric oxide production with no or weak cell toxicity. Compound 16 also significantly suppressed the expression of TNF-alpha, interleukin (IL)-1 beta, cyclooxygenase (COX-2) as well as inducible nitric oxide synthase (iNOS) in LPS-stimulated BV-2 microglia cells. In addition, compound 16 markedly reduced infarction volume in a focal ischemic mice model. (C) 2013 Elsevier Ltd. All rights reserved. |
| WOS关键词 | NITRIC-OXIDE SYNTHASE ; DRUG ABSORPTION MODIFIERS ; FACTOR-ALPHA GENE ; ALZHEIMERS-DISEASE ; BRAIN-DAMAGE ; EXPRESSION ; INFLAMMATION ; ACID ; CNS ; LIPOPOLYSACCHARIDE |
| 资助项目 | National Science Foundation of China[21102167] ; National Science Foundation of China[81130023] ; National Science Foundation of China[81371278] ; National Science Foundation of China[81372688] ; National Basic Research Plan (973) of the Ministry of Science and Technology of China[2009CB522000] ; National Basic Research Plan (973) of the Ministry of Science and Technology of China[2011CB5C4403] ; Priority Academic Program Development of Jiangsu Higher Education Institutes (PAPD)[00000000] ; Jiangsu Science and Technology Commission[BY2011131] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| WOS记录号 | WOS:000331196600042 |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/277184]  |
| 专题 | 药物化学研究室 药理学第二研究室 |
| 通讯作者 | Chen, Hong-Li |
| 作者单位 | 1.Chinese Acad Sci, Shanghai Inst Organ Chem, Shanghai 200032, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China; 3.Soochow Univ, Coll Pharmaceut Sci, Dept Pharmacol, Jiansu Key Lab Translat Res Neuropsychodis, Suzhou 215123, Peoples R China; |
| 推荐引用方式 GB/T 7714 | Yang, Ya-Xi,Zheng, Long-Tai,Shi, Jing-Jing,et al. Synthesis of 5 alpha-cholestan-6-one derivatives and their inhibitory activities of NO production in activated microglia: Discovery of a novel neuroinflammation inhibitor[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2014,24(4):1222-1227. |
| APA | Yang, Ya-Xi.,Zheng, Long-Tai.,Shi, Jing-Jing.,Gao, Bo.,Chen, Yan-Ke.,...&Zhen, Xue-Chu.(2014).Synthesis of 5 alpha-cholestan-6-one derivatives and their inhibitory activities of NO production in activated microglia: Discovery of a novel neuroinflammation inhibitor.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,24(4),1222-1227. |
| MLA | Yang, Ya-Xi,et al."Synthesis of 5 alpha-cholestan-6-one derivatives and their inhibitory activities of NO production in activated microglia: Discovery of a novel neuroinflammation inhibitor".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 24.4(2014):1222-1227. |
入库方式： OAI收割
来源：上海药物研究所
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