Discovery of novel Bis-amide analogue ST12 for the treatment of inflammatory bowel diseases (IBD) by inhibiting NLRP3 inflammasome activation
文献类型：期刊论文
| 作者 | Sun, Zhiqiang2; Zang, Qinru2; Xu, Chenglong2; Zhang, Xuewen2; Kang, Zhenghui3; Yang, Yushe4 ; Li, Ling1; Chen, Jianjun2
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| 刊名 | BIOORGANIC CHEMISTRY
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| 出版日期 | 2025-06-01 |
| 卷号 | 159页码:14 |
| 关键词 | Anti-inflammatory agents Nitric oxide (NO) NLRP3 inflammasome Inflammatory bowel diseases (IBD) |
| ISSN号 | 0045-2068 |
| DOI | 10.1016/j.bioorg.2025.108402 |
| 英文摘要 | Herein, we designed and synthesized a series of novel bis-amide small molecule anti-inflammatory agents, among them, compound ST12 showed most potent anti-inflammatory activity. ST12 effectively inhibited the production of nitric oxide (NO) (inhibition rate of 52.67 +/- 0.03 % at 10 mu M) and downregulated the mRNA levels of proinflammatory cytokines iNOS, IL-6, IL-1(3 and TNF-alpha in lipopolysaccharide (LPS) induced RAW264.7 cells. Furthermore, mechanism studies suggest that compound ST12 exerted anti-inflammatory effects by inhibiting the activation of the NLRP3 inflammasome. Importantly, ST12 effectively ameliorated DSS-induced colitis in vivo. Taken together, ST12 is worthy of further investigation as a small molecule anti-inflammatory agent for treatment of inflammatory bowel diseases (IBD). |
| WOS关键词 | PATHOGENESIS ; MECHANISMS |
| 资助项目 | Guangdong Basic and Applied Basic Research Foundation[2023A1515012967] ; Shenzhen Science and Technology Program[RCBS20231211090536059] |
| WOS研究方向 | Biochemistry & Molecular Biology ; Chemistry |
| 语种 | 英语 |
| WOS记录号 | WOS:001458150800001 |
| 出版者 | ACADEMIC PRESS INC ELSEVIER SCIENCE |
| 源URL | [http://119.78.100.183/handle/2S10ELR8/316917]  |
| 专题 | 新药研究国家重点实验室 |
| 通讯作者 | Kang, Zhenghui; Yang, Yushe; Li, Ling; Chen, Jianjun |
| 作者单位 | 1.Sun Yat Sen Univ, Affiliated Hosp 8, 3025 Shennan Middle Rd, Shenzhen 518000, Peoples R China 2.Southern Med Univ, Sch Pharmaceut Sci, Guangdong Prov Key Lab New Drug Screening, NMPA Key Lab Res & Evaluat Drug Metab, Guangzhou 510515, Peoples R China 3.Chinese Acad Sci, Zhongshan Inst Drug Discovery, Shanghai Inst Mat Med, Zhongshan 528400, Peoples R China 4.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China |
| 推荐引用方式 GB/T 7714 | Sun, Zhiqiang,Zang, Qinru,Xu, Chenglong,et al. Discovery of novel Bis-amide analogue ST12 for the treatment of inflammatory bowel diseases (IBD) by inhibiting NLRP3 inflammasome activation[J]. BIOORGANIC CHEMISTRY,2025,159:14. |
| APA | Sun, Zhiqiang.,Zang, Qinru.,Xu, Chenglong.,Zhang, Xuewen.,Kang, Zhenghui.,...&Chen, Jianjun.(2025).Discovery of novel Bis-amide analogue ST12 for the treatment of inflammatory bowel diseases (IBD) by inhibiting NLRP3 inflammasome activation.BIOORGANIC CHEMISTRY,159,14. |
| MLA | Sun, Zhiqiang,et al."Discovery of novel Bis-amide analogue ST12 for the treatment of inflammatory bowel diseases (IBD) by inhibiting NLRP3 inflammasome activation".BIOORGANIC CHEMISTRY 159(2025):14. |
入库方式： OAI收割
来源：上海药物研究所
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