Synthesis of aspirin eugenol ester and its biological activity

被引:54
作者
Li, Jian-yong [1 ]
Yu, Yuan-guang [1 ]
Wang, Qi-wen [1 ]
Zhang, Ji-yu [1 ]
Yang, Ya-jun [1 ]
Li, Bing [1 ]
Zhou, Xu-zheng [1 ]
Niu, Jian-rong [1 ]
Wei, Xiao-juan [1 ]
Liu, Xi-wang [1 ]
Liu, Zhi-qi [2 ]
机构
[1] Chinese Acad Agr Sci, Key Lab New Anim Drug Project Gansu Prov, Lanzhou Inst Anim Sci & Vet Pharmaceut, Key Lab Vet Pharmaceut Discovery,Agr Minist, Lanzhou 730050, Peoples R China
[2] Lanzhou Univ Technol, Acad Life Sci & Engn, Lanzhou 730050, Peoples R China
关键词
Aspirin eugenol ester (AEE); Synthesis; Toxicity; Anti-inflammation; Analgesic and antipyretic effects; IN-VIVO; ANTIINFLAMMATORY DRUGS; BIOSYNTHESIS; CYCLOOXYGENASE; INHIBITION; MECHANISM; VITRO;
D O I
10.1007/s00044-011-9609-1
中图分类号
R914 [药物化学];
学科分类号
100705 [微生物与生化药学];
摘要
Aspirin, as starting precursor, was reacted with SOCl2 to generate acyl chloride compound via esterifying eugenol to aspirin eugenol ester (AEE) with a yield of 65%. Tests of AEE for acute toxicity, anti-inflammatory, analgesic, and antipyretic effects were carried out in mice and rats. The results showed that toxicity of AEE was significantly reduced, about 50 and 3.7 times lower than aspirin and eugenol, respectively. Its strength of anti-inflammation, analgesia, and antipyresis was similar as aspirin and eugenol, but the effects lasted longer.
引用
收藏
页码:995 / 999
页数:5
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