文献类型：期刊文献

英文题名：Synthesis of novel ursolic acid-gallate hybrids via 1,2,3-triazole linkage and its anti-oxidant and anti-inflammatory activity study

作者：Qi, Zhiwen[1] Xie, Pujun[1] Wang, Zhihong[4] Zhou, Hao[1] Tao, Ran[1] Popov, Sergey A.[2] Yang, Guliang[3] Shults, Elvira E.[2] Wang, Chengzhang[1]

第一作者：齐志文

通信作者：Wang, CZ[1]

机构：[1]Chinese Acad Forest, Inst Chem Ind Forest Prod, Nanjing 210042, Jiangsu, Peoples R China;[2]Novosibirsk Inst Organ Chem, Acad Lavrentyev Ave 9, Novosibirsk 630090, Russia;[3]Cent South Univ Forestry & Technol, Food Sci & Engn Coll, Natl Engn Lab Rice & By Prod Proc, Changsha 410004, Hunan, Peoples R China;[4]Guangdong Acad Forestry, Guangdong Prov Key Lab Silviculture Protect & Util, Guangzhou 510520, Peoples R China

年份：2024

卷号：17

期号：5

外文期刊名：ARABIAN JOURNAL OF CHEMISTRY

收录：;EI(收录号：20241515876870);Scopus(收录号：2-s2.0-85189676255);WOS:【SCI-EXPANDED(收录号:WOS:001225600900001)】；

基金：We thank the National Key Research and Development Program of China (2022YFD2200604-3) , National Natural Science Foundation of China (32101472; 32271820) , Hunan Natural Science Foundation Project (2021JJ31154) , and Russian Science Foundation (grant #23-73-00077) for financial support. Authors would like to acknowledge the Multi-Access Chemical Research Center SB RAS for spectral and analytical measurements.

语种：英文

外文关键词：Ursolic acid; Gallic acid; Hybrids; Structure -activity relationships; Anti-inflammatory mechanism

摘要：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 antiinflammatory properties. In this study, a series of 16 novel UA hybrids tethered via 1,2,3-triazole to the modified gallate moieties were synthesized via CuAAC 1,3-cycloaddition reactions. In vitro, all derivatives were proved to be effective in antioxidation and anti-inflammation activities. Interestingly, compound 20 significantly inhibited the expression of pro-inflammatory cytokines including mRNA of inducible nitric oxide synthase (iNOS) (p < 0.05) and cyclooxygenase-2 (COX-2) (p < 0.01) in lipopolysaccharide (LPS)-induced RAW264.7 cells in a dose-dependent manner. The inhibitory effect of compound 20 on pro-inflammatory cytokines was closely associated with suppression of the LPS-activated PI3K/Akt signal pathway. Compound 20 significantly alleviated inflammation in the gastrointestinal tract of zebrafish in vivo. In addition, compound 20 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.