英文论文
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文献类型
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Journal article (JA)
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题名
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Synthesis and biological evaluation of novel carboxylic acid DHA-alkanolamine derivatives as anti-inflammatory agents by targeting Nur77
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作者
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Fang, Hua; Wang, Xiumei; Li, Mengyu; Huang, Mengxian; Zhang, Yiping; Zhao, Taige; Sun, Cuiling; Xu, Min; Jin, Wenhui; Chen, Weizhu; Fang, Meijuan
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作者单位
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[Fang, Hua; Li, Mengyu; Huang, Mengxian; Zhang, Yiping; Jin, Wenhui; Chen, Weizhu] Minist Nat Resources, Inst Oceanog 3, Tech Innovat Ctr Utilizat Marine Biol Resources, Xiamen 361005, Peoples R China. [Wang, Xiumei; Zhao, Taige; Sun, Cuiling; Fang, Meijuan] Xiamen Univ, Sch Pharmaceut Sci, Fujian Prov Key Lab Innovat Drug Target Res, Xiamen 361102, Peoples R China. [Wang, Xiumei; Zhao, Taige; Sun, Cuiling; Fang, Meijuan] Xiamen Univ, Sch Pharmaceut Sci, State Key Lab Cellular Stress Biol, Xiamen 361102, Peoples R China. [Fang, Hua; Zhang, Yiping; Xu, Min; Jin, Wenhui; Chen, Weizhu] Xiamen Ocean Vocat Coll, Xiamen 361102, Peoples R China. [Fang, Hua; Huang, Mengxian] Zhejiang Wanli Univ, Coll Biol & Environm, Ningbo 315100, Peoples R China.
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通讯作者地址
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Minist Nat Resources, Inst Oceanog 3, Tech Innovat Ctr Utilizat Marine Biol Resources, Xiamen 361005, Peoples R China.; Xiamen Univ, Sch Pharmaceut Sci, Fujian Prov Key Lab Innovat Drug Target Res, Xiamen 361102, Peoples R China.; Xiamen Univ, Sch Pharmaceut Sci, State Key Lab Cellular Stress Biol, Xiamen 361102, Peoples R China.
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Email
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hfang@tio.org.cn
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ResearchID
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ORCID
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期刊名称
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Journal of Molecular Structure
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出版社
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ELSEVIER
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ISSN
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0022-2860
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出版信息
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2025-02-05, 1321 ():.
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JCR
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影响因子
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ISBN
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基金
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Xiamen Marine and Fishery Development Special Fund, Fujian [23CZP009HJ11]; Xiamen and Zhoushan Science and Technology Plan Project [2023N0035, 3502Z20227107, 2023C13017]
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会议名称
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会议地点
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会议开始日期
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会议结束日期
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关键词
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Alkanolamines; Fatty acid methyl ester; Polyunsaturated fatty acids; Salicylic acid
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摘要
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In this study, twenty-five novel carboxylic acid DHA-alkanolamine derivatives were synthesized by the reaction of cis-docosa-4,7,10,13,16,19-hexaenoic acid-alkanolamine (DHA-AA) with various carboxylic acids, including Naproxen (S1), Ibuprofen (S2), Ferulic acid (S3), Mefenamic acid (S4), and Aspirin (S5). Their molecular structures were characterized using 1H/13C NMR and HRMS techniques. To evaluate the anti-inflammatory activities of synthesized compounds, RAW264.7 macrophage cells pretreated with or without these compounds, were stimulated by LPS, and the levels of pro-inflammatory cytokines (NO, TNF-alpha, IL-1(3, and IL-6) were then measured by ELISA, qPCR, and Western Blot. The cell-based assays showed that compound 11 had marked anti-inflammatory activity. In addition, the molecular docking study and SPR assay demonstrated that compound 11 exhibited good Nur77-binding affinity (KD = 3.61 x 10-6 M). Moreover, compound 11 was found to inhibit NF-kappa B activation in a Nur77-dependent manner. Notably, compound 11 could attenuate LPS-induced inflammation in the mouse acute lung injury (ALI) model. In conclusion, these derivatives are potential Nur77-targeting anti-inflammatory agents against versatile inflammatory and autoimmune disorders.
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一级学科
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Chemistry, Physical
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WOS入藏号
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WOS:001303134700001
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EI收录号
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20243516949513
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DOI
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10.1016/j.molstruc.2024.139738
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ESI
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收录于
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SCIE, EI
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