类丹皮酚的结构修饰与在模拟体液中的稳定性考察和抗炎活性研究  

Structural modifications of paeonol and its analogs,and their stability in the simulated body fluids and anti-inflammatory activity

作　　者：胡丁旺 方权辉 彭永练 林友文[2] 陈莉敏[2] HU Ding-wang;FANG Quan-hui;PENG Yong-lian;LIN You-wen;CHEN Li-min(Department of Anatomy and Histology and Embryology,Fujian Medical University,Fuzhou 350004,Chian;Faculty of Pharmacy,Fujian Medical University,Fuzhou 350004,China;Jiangxi Province Skin Discase Specialiaed Hospital,Nanchang 330009,China)

机构地区：[1]福建医科大学基础医学院人体解剖与组织胚胎学系,福建福州350004 [2]福建医科大学药学院,福建福州350004 [3]江西省皮肤病专科医院,江西南昌330009

出　　处：《化学研究与应用》2019年第2期219-224,共6页Chemical Research and Application

基　　金：福建省自然科学基金项目(2015J01679)资助

摘　　要：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2,4-二羟基苯乙酮先与1,4-二溴丁烷合成缩合物,再与酮洛芬合成系列目标化合物。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。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。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。Paeonol,2-hydroxy-5-methoxyacetophenone,2-hydroxy-5-methoxyacetophenone,2-hydroxyacetophenone,3-hydroxyacetophenone,2,4-dihydroxyacetophenone were condensated with 1,4-dibromobutane,then reacted with ketoprofen to yield series of target products.The HPLC method was established for determination of the content of the target products.Their degradation dynamics was assessed under pH 1.2,5.0 and 7.4 buffer conditions at 37℃.The anti-inflammatory activities of the compounds were evaluated in xylene-induced mouse ear swelling model.Five new compounds were synthesized and confirmed by MS and 1H-NMR.Degradation kinetic experiments showed that these compounds were stable in buffers of different pHs.All the compounds showed anti-inflammatory activities.All the compounds were stable and exhibited potent anti-inflammatory activities.

关 键 词：丹皮酚 酮洛芬 合成 高效液相色谱法 抗炎活性 

分 类 号：O625.4[理学—有机化学]