Excessive oxidation can lead to inflammation and affect health. Studies have shown that ursolic acid (UA) and gallic acid are widely employed in medicine and cosmetics owing to their obvious antioxidant and anti-inflammatory properties. In this study, a series of 16 novel UA hybrids tethered 1,2,3-triazole to the modified gallate moieties were synthesized via CuAAC 1,3-cycloaddition reactions. , all derivatives were proved to be effective in antioxidation and anti-inflammation activities. Interestingly, compound significantly inhibited the expression of pro-inflammatory cytokines including mRNA of inducible nitric oxide synthase (iNOS) ( < 0.05) and cyclooxygenase-2 (COX-2) ( < 0.01) in lipopolysaccharide (LPS)-induced RAW264.7 cells in a dose-dependent manner. The inhibitory effect of compound on pro-inflammatory cytokines was closely associated with suppression of the LPS-activated PIK/Akt signal pathway. Compound 20 significantly alleviated inflammation in the gastrointestinal tract of zebrafish . In addition, compound showed good biosafety in cytotoxicity evaluation. This study provides a novel reference for the development of treatments for health problems related to anti-oxidation and anti-inflammation properties.

中文翻译：

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新型熊果酸-没食子酸酯杂化物的1,2,3-三唑键合成及其抗氧化和抗炎活性研究

过度氧化会导致炎症并影响健康。研究表明，熊果酸（UA）和没食子酸因其明显的抗氧化和抗炎特性而广泛应用于医药和化妆品中。在本研究中，通过 CuAAC 1,3-环加成反应合成了一系列 16 个新型 UA 杂化物，将 1,2,3-三唑连接到修饰的没食子酸酯部分。 ，所有衍生物均被证明具有有效的抗氧化和抗炎活性。有趣的是，该化合物显着抑制脂多糖 (LPS) 诱导的 RAW264.7 细胞中促炎细胞因子的表达，包括诱导型一氧化氮合酶 (iNOS) (< 0.05) 和环氧合酶-2 (COX-2) (< 0.01) 的 mRNA以剂量依赖性方式。化合物对促炎细胞因子的抑制作用与 LPS 激活的 PIK/Akt 信号通路的抑制密切相关。化合物20显着减轻斑马鱼胃肠道的炎症。此外，化合物在细胞毒性评价中表现出良好的生物安全性。这项研究为开发与抗氧化和抗炎特性相关的健康问题的治疗方法提供了新的参考。