肉桂酸衍生物的设计、合成和生物活性评估，作为抗 LPS 诱导的急性肺损伤的潜在抗炎剂。

IF 2.5 4区医学 Q3 CHEMISTRY, MEDICINAL

Bioorganic & Medicinal Chemistry Letters Pub Date : 2024-11-21 DOI:10.1016/j.bmcl.2024.130036

Pengqin Chen, Pan Chen, Xiemin Wang

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引用次数: 0

摘要

急性肺损伤（ALI）是临床上常见的危重病，死亡率高达 30-40%，但目前还没有有效的治疗方法。对急性肺损伤的研究表明，抑制过度表达的炎症因子可能是治疗急性肺损伤的一种潜在方法。本研究通过在天然产物肉桂酸中引入不同的氨基噻唑片段，获得了一系列肉桂酸衍生物。在这些衍生物中，化合物 22 在抑制 J774A.1 细胞中 IL-6 的释放方面表现出卓越的活性。此外，它还通过抑制细胞因子的表达、减轻肺水肿和巨噬细胞浸润，改善了 LPS 诱导的小鼠 ALI 模型。这些研究结果表明，化合物 22 可为 ALI 药物的开发提供新的先导结构。

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

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 overexpressed 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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来源期刊

Bioorganic & Medicinal Chemistry Letters 医学-医药化学

CiteScore

5.70

自引率

3.70%

发文量

463

审稿时长

27 days

期刊介绍： Bioorganic & Medicinal Chemistry Letters presents preliminary experimental or theoretical research results of outstanding significance and timeliness on all aspects of science at the interface of chemistry and biology and on major advances in drug design and development. The journal publishes articles in the form of communications reporting experimental or theoretical results of special interest, and strives to provide maximum dissemination to a large, international audience.