Design, synthesis and in vitro biological evaluation of marine phidianidine derivatives as potential anti-inflammatory agents
文献类型：期刊论文
| 作者 | Xu, Quan1,2,4; Zhao, Ning3; Liu, Jin4; Song, Jin-Qian3; Huang, Li-Hua3; Wang, Hong1,2; Li, Xu-Wen4,5,6 ; Pang, Tao3,4; Guo, Yue-Wei1,2,4,5,6
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY
 |
| 出版日期 | 2022-10-01 |
| 卷号 | 71页码:116936 |
| 关键词 | Indole alkaloids Marine natural products Phidianidines Anti-inflammatory activities Molecular docking |
| ISSN号 | 0968-0896 |
| DOI | 10.1016/j.bmc.2022.116936 |
| 文献子类 | Article |
| 英文摘要 | Phidianidines A and B are novel marine indole alkaloids with various biological activities. Based on their po-tential anti-inflammatory properties, a series of phidianidine derivatives were designed, synthesized, and tested for their effects on IL-17A production in PMA/ionomycin-stimulated T-cell-lymphoma EL-4 cells. Compounds 9a and 22c exhibited excellent anti-inflammatory activity and low toxicity, with IC50 values of 7.7 mu M and 5.3 mu M for IL-17A production in PMA/ionomycin-stimulated EL-4 cells, respectively. Further mechanistic study showed that 9a could decrease the STAT3 phosphorylation at Y705 to inhibit IL-17A production in EL-4 cells, indicating its ability of preventing the differentiation of Th17 cells and their possible function. This research may give an insight for the discovery of marine indole alkaloid derived anti-inflammatory drug leads for the treatment of T cell-mediated diseases. |
| WOS关键词 | TNF-ALPHA ; INHIBITORS ; 1,2,4-OXADIAZOLES |
| WOS研究方向 | Biochemistry & Molecular Biology ; Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000969216700005 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/309299]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Li, Xu-Wen; Pang, Tao; Guo, Yue-Wei |
| 作者单位 | 1.Zhejiang Univ Technol, Collaborat Innovat Ctr Yangtze River Delta Reg Gre, Hangzhou 310014, Zhejiang, Peoples R China; 2.Zhejiang Univ Technol, Coll Pharmaceut Sci, Hangzhou 310014, Zhejiang, Peoples R China; 3.China Pharmaceut Univ, New Drug Screening Ctr, State Key Lab Nat Med, Nanjing 210009, Peoples R China; 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, 555 Zu Chong Zhi Rd,Zhangjiang Hitech Pk, Shanghai 201203, Peoples R China; 5.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai 264117, Shandong, Peoples R China; 6.Pilot Natl Lab Marine Sci & Technol Qingdao, Open Studio Druggabil Res Marine Nat Prod, 1 Wenhai Rd, Qingdao 266237, Peoples R China |
| 推荐引用方式 GB/T 7714 | Xu, Quan,Zhao, Ning,Liu, Jin,et al. Design, synthesis and in vitro biological evaluation of marine phidianidine derivatives as potential anti-inflammatory agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY,2022,71:116936. |
| APA | Xu, Quan.,Zhao, Ning.,Liu, Jin.,Song, Jin-Qian.,Huang, Li-Hua.,...&Guo, Yue-Wei.(2022).Design, synthesis and in vitro biological evaluation of marine phidianidine derivatives as potential anti-inflammatory agents.BIOORGANIC & MEDICINAL CHEMISTRY,71,116936. |
| MLA | Xu, Quan,et al."Design, synthesis and in vitro biological evaluation of marine phidianidine derivatives as potential anti-inflammatory agents".BIOORGANIC & MEDICINAL CHEMISTRY 71(2022):116936. |
入库方式： OAI收割
来源：上海药物研究所
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