Nitric oxide production inhibition and mechanism of phenanthrene analogs in lipopolysaccharide-stimulated RAW264.7 macrophages
文献类型:期刊论文
作者 | Yuan, XH (reprint author), Southwest Univ Sci & Technol, Sch Life Sci & Engn, Mianyang, Peoples R China.; Chen, LQ; Shen, XF; Hu, BY; Lin, Y; Igbe, I; Zhang, CG; Zhang, GL; Yuan, XH; Wang, F |
刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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出版日期 | 2016 |
卷号 | 26期号:10页码:2521-2525 |
关键词 | Phenanthrene Anti-inflammatory Activity P38 Ijba Macrophage |
DOI | 10.1016/j.bmcl.2016.03.088 |
产权排序 | 2 |
文献子类 | Article |
英文摘要 | Natural phenanthrene derivatives are considered to be important resource for the anti-inflammatory therapeutics, but their structure-activity relationship and mechanisms are still unknown. In this study we evaluated 20 synthesized phenanthrene analogs in lipopolysaccharide (LPS)-stimulated RAW264.7 macrophages. Compounds 10, 11 and 17 were found to inhibit the production of nitric oxide (NO) with IC50 values of 37.26 mu M, 5.05 mu M and 20.31 mu M, respectively. Compound 11 decreased LPS-induced expression of inducible NO synthase (iNOS), inhibited phosphorylation of p38 mitogen-activated protein kinase (MAPK) and serine/threonine kinase Akt. It also suppressed the phosphorylation and degradation of inhibitory kappa B-alpha (I kappa B alpha). Data obtained suggest that compound 11 exerts anti-inflammatory effects by inhibiting p38 MAPK and nuclear factor kappa B (NF-kappa B) pathways, which warrants further investigation as a new anti-inflammatory pharmaceutical tool. (C) 2016 Elsevier Ltd. All rights reserved. |
学科主题 | Pharmacology & Pharmacy ; Chemistry |
资助项目 | 天然药物和临床转化实验室 |
语种 | 英语 |
资助机构 | National Natural Science Foundation of China [91413108, 21272189, 21561142003] ; National Natural Science Foundation of China [91413108, 21272189, 21561142003] ; Sichuan Youth Science & Technology Foundation [2014JQ0028] ; Sichuan Youth Science & Technology Foundation [2014JQ0028] ; West Light Foundation of the Chinese Academy of Sciences ; West Light Foundation of the Chinese Academy of Sciences ; National Natural Science Foundation of China [91413108, 21272189, 21561142003] ; National Natural Science Foundation of China [91413108, 21272189, 21561142003] ; Sichuan Youth Science & Technology Foundation [2014JQ0028] ; Sichuan Youth Science & Technology Foundation [2014JQ0028] ; West Light Foundation of the Chinese Academy of Sciences ; West Light Foundation of the Chinese Academy of Sciences |
源URL | [http://210.75.237.14/handle/351003/28194] ![]() |
专题 | 成都生物研究所_天然产物研究 |
通讯作者 | Yuan, XH (reprint author), Southwest Univ Sci & Technol, Sch Life Sci & Engn, Mianyang, Peoples R China.; Wang, F (reprint author), Chinese Acad Sci, Chengdu Inst Biol, Key Lab Nat Med & Clin Translat, Chengdu, Peoples R China. |
推荐引用方式 GB/T 7714 | Yuan, XH ,Chen, LQ,Shen, XF,et al. Nitric oxide production inhibition and mechanism of phenanthrene analogs in lipopolysaccharide-stimulated RAW264.7 macrophages[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2016,26(10):2521-2525. |
APA | Yuan, XH .,Chen, LQ.,Shen, XF.,Hu, BY.,Lin, Y.,...&Wang, F .(2016).Nitric oxide production inhibition and mechanism of phenanthrene analogs in lipopolysaccharide-stimulated RAW264.7 macrophages.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,26(10),2521-2525. |
MLA | Yuan, XH ,et al."Nitric oxide production inhibition and mechanism of phenanthrene analogs in lipopolysaccharide-stimulated RAW264.7 macrophages".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 26.10(2016):2521-2525. |
入库方式: OAI收割
来源:成都生物研究所
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