Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation
文献类型：期刊论文
| 作者 | Ajiaikebaier, D (Ajiaikebaier, Dilidaer) 1 , 3; Li, ZP (Li, Zuopeng) 2; Lin, TC (Lin, TzuChun) 1; Sun, XY (Sun, Xinyu) 1; Wang, BL (Wang, Bianlin) 2; Li, JY (Li, Jingya) 1 , 3 |
| 刊名 | BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
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| 出版日期 | 2021 |
| 卷号 | 42期号:6页码:1-5 |
| 关键词 | Pyranochalcone derivativesNF-kappa B inhibitorAnti-inflammatoryInflammatory factor |
| ISSN号 | 0960-894X |
| DOI | 10.1016/j.bmcl.2021.128042 |
| 英文摘要 | In an effort to identify novel inhibitors of nuclear factor kappa B (NF-kappa B), twenty five pyranochalcone derivatives were synthesized and evaluated for their in vitro activities against TNF-alpha induced NF-kappa B inhibition in HEK293T cells. Among all of these derivatives, several displaying the same acrylate moiety on the B ring exhibited potent inhibition, with IC50 values ranging from 0.29 to 10.46 mu M. A functional study of the most potent of these compounds, designated 6b, revealed that it significantly suppressed the transcriptional expression of inflammatory factor IL-10 in lipopolysaccharide-induced RAW 264.7 macrophages, and also mildly inhibited CCL2, IL6 and TNF-alpha. In addition, compound 6b was found to inhibit IL-10 released in LPS-induced BMDM cells. This study demonstrates that the inhibitory effect of 6b on LPS-stimulated inflammatory mediator production in the mouse macrophage cell line RAW 264.7 correlates with the suppression of the NF-kappa B and MAPK signaling pathways. |
| WOS记录号 | WOS:000655255700003 |
| 源URL | [http://ir.xjipc.cas.cn/handle/365002/7861]  |
| 专题 | 新疆理化技术研究所_省部共建新疆特有药用资源利用重点实验室 |
| 作者单位 | 1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China 2.Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, Urumqi 830011, Peoples R China 3.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Ajiaikebaier, D ,Li, ZP ,Lin, TC ,et al. Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation[J]. BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,2021,42(6):1-5. |
| APA | Ajiaikebaier, D ,Li, ZP ,Lin, TC ,Sun, XY ,Wang, BL ,&Li, JY .(2021).Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation.BIOORGANIC & MEDICINAL CHEMISTRY LETTERS,42(6),1-5. |
| MLA | Ajiaikebaier, D ,et al."Synthesis of pyranochalcone derivatives and their inhibitory effect on NF-kappa B activation".BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 42.6(2021):1-5. |
入库方式： OAI收割
来源：新疆理化技术研究所
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