老鼠生物碱 A羧酸衍生物抗炎镇痛活性的研究

摘要

Objective To study the anti-inflammatory and analgesic activity of the carboxylic acid derivatives of Ilicifolius alkaloids A (4-Hydroxy-2-benzoxazolone ,HBOA) ,and to find out novel derivatives of Ilicifolius alkaloids A with better efficacy.Methods The anti-inflammatory activities of the carboxylic acid derivatives were evaluated by the xylene-induced mice ear swelling model .The analgesic activities of the carboxylic acid derivatives were evaluated by the mouse aceticacid-induced stretching test and hot-plate test .Results Eight derivatives were observed to have anti-inflammatory activities in the xylene-induced mice ear swelling model .Compounds 2,3,4 and 8 exhibited equal anti-inflammatory activity and Compounds 1,5,6 and 7 showed lower activity in comparison with aspirin .Eight derivatives exhibited significant analgesic activities in the HAc-induced stretching test .However , none of them was observed to have analgesic activities in the hot-plate test.Among these 8 compounds, Compound 3 exhibited higher peripheral analgesic activities,and the others showed equal activities in comparison with aspirin .Conclusion Four derivatives (Compounds 2,3,4,8) are worthy of further research ,which possess superior anti-inflammatory and analgesia activities .%目的：研究老鼠簕生物碱A羧酸衍生物的抗炎镇痛活性，筛选具有良好抗炎、镇痛药理活性的老鼠簕生物碱A衍生物。方法采用二甲苯致小鼠耳肿胀模型评价羧酸衍生物的抗炎活性，采用醋酸诱导的小鼠扭体法和热板法评价羧酸衍生物的镇痛活性。结果二甲苯致小鼠耳肿胀实验显示，老鼠簕生物碱A羧酸8个化合物对小鼠耳肿胀均有抑制作用，其中化合物2、化合物3、化合物4、化合物8对小鼠耳肿胀的抑制作用与阿司匹林相当；化合物1、化合物5、化合物6、化合物7对小鼠耳肿胀的抑制作用比阿司匹林小。热板法镇痛实验显示，8个衍生物对热刺激引起的疼痛均无抑制作用。小鼠醋酸扭体实验显示，8个化合物对醋酸所致小鼠的扭体反应均有抑制作用，其中化合物3的外周镇痛作用比阿司匹林强，其他7个化合物发挥的外周镇痛作用与阿司匹林相当。结论化合物2、化合物3、化合物4和化合物8等4个羧酸衍生物具有较好的抗炎和镇痛活性，值得进一步研究。