Synthesis and Biological Evaluation of Isoaurone Derivatives as Anti-inflammatory Agents

被引：2

作者：

Bai, Xueqian ^{[1
]}

Ye, Chao ^{[1
]}

Liu, Zhe ^{[1
]}

Zhou, Zhijiang ^{[1
]}

Zhang, Tianyi ^{[1
]}

机构：

[1] Jilin Med Univ, Jilin 132013, Peoples R China

来源：

CHEMISTRY & BIODIVERSITY | 2025年 / 22卷 / 03期

关键词：

Isoaurone derivatives; COX-2; NO; Anti-inflammatory agents; ISOAUROSTATIN; INHIBITORS; DESIGN; DRUGS;

D O I：

10.1002/cbdv.202402073

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Twenty-eight isoaurone derivatives with 1,2,4-triazole moieties were synthesized using a fragment-based design strategy, and their anti-inflammatory activity was investigated. The anti-inflammatory effect of the most active derivative, 14e (41.82 %), was dose-dependent and higher than the values for celecoxib (31.82 %). Compound 14e was almost non-toxic and inhibited different concentrations of nitric oxide (NO). The western blotting results demonstrated that cyclooxygenase-2 (COX-2) expression was elevated when the macrophages were exclusively treated with LPS. However, compound 14e effectively suppressed the LPS-induced COX-2 upregulation. Subsequent investigation revealed that 14e is a promising compound capable of inhibiting the downstream signaling of COX-2. With the above interesting biological profile, molecular 14e could be a promising lead to develop novel anti-inflammatory agents.

引用

页数：9

共 30 条

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