Design, synthesis and bioactivity evaluation of cinnamic acid derivatives as potential anti-inflammatory agents against LPS-induced acute lung injury

被引:0
|
作者
Chen, Pengqin [3 ]
Chen, Pan [2 ]
Wang, Xiemin [1 ]
机构
[1] Zhejiang Chinese Med Univ, Dermatol, Affiliated Hosp 3, Hangzhou, Zhejiang, Peoples R China
[2] Wenzhou Med Univ, Dept Cardiol, Affiliated Hosp 1, Wenzhou 325035, Peoples R China
[3] Zhejiang Univ, Affiliated Hosp 1, Sch Med, Dept Clin Pharm, Hangzhou 310000, Zhejiang, Peoples R China
关键词
Acute lung injury; Cinnamic acid derivatives; Anti-inflammatory; NATURAL-PRODUCTS;
D O I
10.1016/j.bmcl.2024.130036
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Acute lung injury (ALI), a common critical disease in clinical practice, has a mortality rate as high as 30-40 %, yet currently, no effective treatment methods are available. Research on ALI indicated that inhibition of over- expressed inflammatory factors might be a potential treatment for ALI. In this study, a series of cinnamic acid derivatives were obtained by introducing diverse aminothiazole fragments into the natural product cinnamic acid. Among these derivatives, compound 22 displayed excellent activity of inhibiting the release of IL-6 in J774A.1 cells. Moreover, it also ameliorated the LPS-induced ALI in mouse model by suppressing cytokine expression, reducing lung edema and macrophage infiltration. These findings indicated that compound 22 might provide a new lead structure for the development of drugs for ALI.
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页数:6
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