单酰甘油脂肪酶抑制剂的抗炎与镇痛作用  

Anti-inflammatory and analgesic effects of monoacylglycerol lipase inhibitor

作　　者：徐媛 牟建芮 叶香含 柯博文[3] 闫薇[4] 宋颢[1] XU Yuan;MOU Janrui;YE Xianghan;KE Bowen;YAN Wei;SONG Hao(Key Laboratory of Drug-Targeting and Drug Delivery System of the Education Ministry,West China School of Pharmacy,Sichuan University,Chengdu,Sichuan,610041 P.R.China;School of Pharmacy,Southwest Minzu University,Chengdu,Sichuan,610041 P.R.China;Laboratory of Anaesthesiology&Critical Care Medicine,West China Brain Research Center,West China Hospital,Sichuan University,Chengdu,Sichuan,610041 P.R.China;Department of Dermatology,West China Hospital,Sichuan University,Chengdu,Sichuan,610041 P.R.China)

机构地区：[1]四川大学华西药学院教育部药物靶向与给药系统重点实验室,四川成都610041 [2]西南民族大学药学院,四川成都610041 [3]四川大学华西医院转化神经科学中心麻醉与危重急救研究室,四川成都610041 [4]四川大学华西医院皮肤性病科,四川成都610041

出　　处：《华西药学杂志》2021年第3期254-257,共4页West China Journal of Pharmaceutical Sciences

基　　金：国家自然科学基金资助项目(批准号:81803142)。

摘　　要：目的研究单酰甘油脂肪酶抑制剂URB 602在大鼠足底切口引起的急性术后疼痛和冰醋酸导致小鼠急性内脏痛模型上的抗炎、镇痛作用。方法采用大鼠切口痛模型和0.6%冰乙酸致小鼠扭体模型研究URB 602的镇痛作用;运用HE染色方法观察URB 602对切口痛的抗炎作用。结果URB 602(5、2.5 mg·kg^(-1))两个剂量对小鼠内脏痛有显著的镇痛作用,抑制率分别为91.03%、56.06%;在大鼠切口痛模型中,URB 602(50、20、10 mg·kg^(-1))3个剂量在给药30 min后均有明显的镇痛活性,90 min后药效逐渐消失;URB 602可以明显减轻后爪肿胀度,从HE染色结果中可见:给药组的炎症浸润面积比明显减少。结论URB 602具有很好的抗炎、镇痛作用。OBJECTIVE To study anti-inflammatory and analgesic effects of MAGL inhibitor,URB 602,on acute postoperative pain caused by plantar incision and acute visceral pain model caused by acetic acid.METHODS Rat incision pain model and acetic acid-induced mouse writhing assay were used to identify the analgesic effect of URB 602.H&E staining was used to observe the anti-inflammatory effect of URB 602 on rat plantar incision.RESULTS 5 and 2.5 mg·kg^(-1)of URB 602 had a significant analgesic effect on visceral pain of mice,and the inhibition rates were 91.03%and 56.06%,respectively.In the rat incision pain model,50,20 and 10 mg·kg^(-1)of URB 602 showed potent analgesic activity after 30 minutes of administration,and the activity gradually disappeared after 90 minutes.The hind paw swelling of URB 602 groups were obviously alleviated.The area ratios of inflammation in the URB 602 groups were significantly reduced and were consistent with the H&E staining results.CONCLUSION URB 602 exhibits good anti-inflammatory and analgesic effects.

关 键 词：单酰甘油脂肪酶抑制剂 URB 602 足底切口 扭体反应 组织染色 足底肿胀 抗炎 镇痛 

分 类 号：R914[医药卫生—药物化学] R96[医药卫生—药学]