| 新型阿魏酸衍生物的合成及药理活性研究 |
| |
| 引用本文： | 毛近隆,林翠霞,周洪雷,冉祥凯,孙蓉.新型阿魏酸衍生物的合成及药理活性研究[J].山东中医药大学学报,2014(3):260-262,269. |
| |
| 作者姓名： | 毛近隆 林翠霞 周洪雷 冉祥凯 孙蓉 |
| |
| 作者单位： | [1]山东中医药大学药学院,山东济南250355 [2]山东中医药大学护理学院,山东济南250355 [3]山东大学化学与化工学院,山东济南250014 [4]山东省中医药研究院药理研究室,山东济南250014 |
| |
| 基金项目： | 国家科技部十一五支撑计划重点项目（编号：2008BA151802）.国家重大新药创制重大专项课题（编号：2009ZX09502-015） |
| |
| 摘 要： | 目的:NSAIDs药物抑制COX-2的同时,也使心血管风险加大,以中药活性成分为先导化合物设计药物分子,以提高其心血管安全性。方法:以阿魏酸的核心结构为先导化合物,设计合成新型阿魏酸衍生物,并进行初步的抗炎活性和心肌毒性实验。结果:代表性化合物CMY和CMZ具有显著的抗炎活性,二甲苯致鼠耳肿胀抑制率分别为45.29%和24.11%,且其心肌毒性未观察到。结论:NSAIDs药物抑制COX-2的同时,保持了PGI2与TXA2的相对平衡,促进了内源性NO的表达,有利于提高其心血管安全性。
|
| 关 键 词： | 阿魏酸 4-羟基苯丙烯酸 非甾体抗炎药物 环氧合酶 心血管安全性 |
Synthesis and Pharmacological Activity of the New Derivatives of Ferulic Acid |
| |
| MAO Jinlong,LIN Cuixia,ZHOU Honglei,RAN Xiangkai,SUN Rong.Synthesis and Pharmacological Activity of the New Derivatives of Ferulic Acid[J].Journal of Shandong University of Traditional Chinese Medicine,2014(3):260-262,269. |
| |
| Authors: | MAO Jinlong LIN Cuixia ZHOU Honglei RAN Xiangkai SUN Rong |
| |
| Institution: | 1.College of Pharmacy,Shandong University of Traditional Chinese Medicine,Jinan 250355,China;2.College of Nursing,Shandong University of Traditional Chinese Medicine,Jinan 250355,China;3.College of Chemistry and Chemical Engineering,Shandong University,Jinan 250014,China;4.Division of Pharmacology,Shandong Academy of Chinese Medicine,Jinan 250014,China) |
| |
| Abstract: | Objective-NSAIDs can increase the cardiovascular risk due to inhibition of COX-2,new drug structrue was designed to improve their cardiovascular safety on the basis of traditional Chinese medicine active ingredients. Methods：New ferulic acid derivatives were designed and synthesized based on the core structure of ferulic acid,and conducted a preliminary anti-inflammatory activity and cardiac toxicity. Results： The tested compound CMY and CMZ have significant anti-inflammatory activity with suppression rates of 45.29% and 24.11% in xylene induced served. Conclusion：When NSAIDs take TXA2,increases the release of NO,and ear edema model respectively,and the cardiac toxicity was not ob- effect of COX-2 inhibition,it keeps a balance between PGI2 and helps to improve cardiovascular safety |
| |
| Keywords: | ferulic acid 4-Hydroxycinnamic acid NSAIDs COX cardiovascular safety |
| 本文献已被 CNKI 维普 等数据库收录！ |
|
