丹皮酚的孪药合成及降解动力学和抗炎活性研究  

Synthesis of Twin Drugs of Paeonol and Study on Their Degradation Dynamics Properties and Anti-inflammatory Activities

作　　者：陈莉敏[1] 姜玉才 彭永练 

机构地区：[1]福建医科大学药学院,福州350004

出　　处：《中国药学杂志》2016年第1期61-64,共4页Chinese Pharmaceutical Journal

基　　金：福建省自然科学基金资助项目(2015J01679)

摘　　要：目的合成丹皮酚及其类似物与萘普生的酯化产物,并研究其抗炎活性。方法将萘普生分别与丹皮酚、2-羟基-5-甲氧基-苯乙酮、3-羟基苯乙酮、2-羟基苯乙酮和3-甲氧基苯酚通过酯化反应合成系列化合物。用HPLC考察目标化合物在不同pH缓冲液中的降解情况,用二甲苯致小鼠耳肿胀模型对其进行抗炎活性筛选。结果合成了5个目标化合物,经MS和1H-NMR确证其结构。HPLC证明其在体内稳定。小鼠实验表明,目标化合物具有较强的抗炎作用。结论目标化合物在胃肠道pH值中稳定,抗炎活性较强,值得进一步研究。OBJECTIVE To synthesize the ester condensation products of paeonol by coupling paeonol or its analogues with naproxen and investigate the anti-inflammatory activities of the products. METHODS Five compounds were synthesized by conden- sing paeonol or its analogues with naproxen by DCC method. An HPLC method was established for determination of the content of the target products, and their degradation dynamics under pH 1.2, 5.0 and 7.4 buffer conditions at 37 ~C was studied. The anti-inflamma- tory activities of the compounds were evaluated in xylene-indueed mouse ear swelling model. RESULTS Five new compounds were synthesized and confirmed by MS and J H-NMR. Degradation kinetic experiments showed that these compounds were stable in buffers of different pHs. All the compounds showed anti-inflammatory activities. CONCLUSION All the compounds are stable and exhibit po- tent anti-inflammatory activities.

关 键 词：丹皮酚 萘普生 合成 高效液相色谱法 抗炎 

分 类 号：R914[医药卫生—药物化学]