Synthesis and biological evaluation of artemisinin derivatives as potential MS agents
文献类型：期刊论文
| 作者 | Zhang, Yan5,6; Lv, Jie4; Zhang, Suqing3; Yang, Hanxi1; Shen, Jingshan2,3 ; Du, Changsheng4; Jiang, Xiangrui2,3; Aisa, Haji A.2,5,6
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| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2022-05-15 |
| 卷号 | 64页码:5 |
| 关键词 | Artemisinin derivatives Multiple sclerosis Th1/Th17 IFN-?/IL-17A EAE |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2022.128682 |
| 通讯作者 | Du, Changsheng(duchangsheng@tongji.edu.cn) ; Jiang, Xiangrui(jiangxiangrui@simm.ac.cn) ; Aisa, Haji A.(haji@ms.xjb.ac.cn) |
| 英文摘要 | In this paper, a series of artemisinin derivatives were synthesized and evaluated. Studies have shown that IFN-gamma produced by Th1 CD4(+) T cells and IL-17A secreted by Th17 CD4(+) T cells played critical roles in the treatment of multiple sclerosis. We used different concentrations of artemisinin derivatives to inhibit Th1/Th17 differentiation in naive CD4(+) T cells and to characterize IFN-gamma / IL-17A in in vitro experiments. The preliminary screening results showed that ester compound 5 exhibited obvious inhibitory activities on Th1 and Th17 (IFN-gamma decreased from 41% to 3% and IL-17A decreased from 24% to 8% at the concentration of 10 nM to 10 mu M), and carbamate compounds also had obvious inhibitory activities against Th17 at high concentration. Moreover, we investigated the effect of compound 5 on myelin oligodendrocyte glycoprotein (MOG)-induced mice experimental autoimmune encephalomyelitis (EAE) model in vivo. 100 mg/kg compound 5 effectively reduced the disease severity of EAE compared with the vehicle group. This research revealed that compound 5 could be a promising avenue as potential MS inhibitor. |
| WOS关键词 | MULTIPLE-SCLEROSIS ; THERAPEUTIC-EFFICACY ; ARTESUNATE ; MODEL |
| 资助项目 | Shanghai Science and Technology Committee in China[19430750100] ; Strategic Priority Research Program of Chinese Academy of Sciences[XDA12040327] |
| WOS研究方向 | Pharmacology & Pharmacy ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:000791828500001 |
| 出版者 | PERGAMON-ELSEVIER SCIENCE LTD |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/301038]  |
| 专题 | 中国科学院上海药物研究所 |
| 通讯作者 | Du, Changsheng; Jiang, Xiangrui; Aisa, Haji A. |
| 作者单位 | 1.Zhengzhou Univ, Coll Chem, 100 Kexuedadao Rd, Zhengzhou 450001, Peoples R China 2.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 3.Shanghai Inst Mat Med, Chinese Acad Sci, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China 4.Tongji Univ, Sch Life Sci & Technol, Putuo Peoples Hosp, Shanghai Key Lab Signaling & Dis Res, Shanghai 200092, Peoples R China 5.Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Reg, Chinese Acad Sci, South Beijing Rd 40-1, Urumqi 830011, Peoples R China 6.Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Chinese Acad Sci, South Beijing Rd 40-1, Urumqi 830011, Peoples R China |
| 推荐引用方式 GB/T 7714 | Zhang, Yan,Lv, Jie,Zhang, Suqing,et al. Synthesis and biological evaluation of artemisinin derivatives as potential MS agents[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2022,64:5. |
| APA | Zhang, Yan.,Lv, Jie.,Zhang, Suqing.,Yang, Hanxi.,Shen, Jingshan.,...&Aisa, Haji A..(2022).Synthesis and biological evaluation of artemisinin derivatives as potential MS agents.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,64,5. |
| MLA | Zhang, Yan,et al."Synthesis and biological evaluation of artemisinin derivatives as potential MS agents".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 64(2022):5. |
入库方式： OAI收割
来源：上海药物研究所
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