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一种合成喹啉(托莫昔罗与萘普生的杂合物)对小鼠急性疼痛和炎症的药理作用:行为学与对接研究

Pharmacological effects of a synthetic quinoline, a hybrid of tomoxiprole and naproxen, against acute pain and inflammation in mice: a behavioral and docking study.

作者信息

Hosseinzadeh Hossein, Mazaheri Fatemeh, Ghodsi Razieh

机构信息

Pharmaceutical Research Center, Mashhad University of Medical Sciences, Mashhad, Iran.

Department of Pharmacodynamics and Toxicology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran.

出版信息

Iran J Basic Med Sci. 2017 Apr;20(4):446-450. doi: 10.22038/IJBMS.2017.8588.

Abstract

OBJECTIVES

In the present study, we investigated the potential anti-nociceptive activity and acute anti-inflammatory effect of a synthetic quinoline compound (2-(4-Methoxyphenyl)benzo[h]quinoline-4-carboxylic acid, QC), possessing structural elements of both naproxen and tomoxiprole drugs.

MATERIALS AND METHODS

The anti-nociceptive activity of QC was evaluated using chemical- and thermal-induced nociception models and its acute anti-inflammatory effect was evaluated by xylene-induced ear edema test in mice.

RESULTS

QC displayed a dose dependent effect in both acute anti-nociceptive tests (writhing and hot plate). This compound at dose of 6.562 mg/kg showed a high anti-nociceptive effect near equal to diclofenac 5 mg/kg. It also showed high anti-inflammatory effects (less than 6.562 mg/kg) comparable to those of reference drugs diclofenac (5 mg/kg) and celecoxib (100 mg/kg). Docking study showed that this quinoline derivative could inhibit COX-2 enzyme strongly.

CONCLUSION

QC showed high anti-nociceptive and anti-inflammatory effects comparable to reference drugs and can exert its anti-nociceptive and anti-inflammatory activities through COX-2 inhibition.

摘要

目的

在本研究中,我们研究了一种合成喹啉化合物(2-(4-甲氧基苯基)苯并[h]喹啉-4-羧酸,QC)的潜在抗伤害感受活性和急性抗炎作用,该化合物兼具萘普生和托莫昔罗药物的结构元素。

材料与方法

使用化学和热诱导的伤害感受模型评估QC的抗伤害感受活性,并通过二甲苯诱导的小鼠耳肿胀试验评估其急性抗炎作用。

结果

QC在两种急性抗伤害感受试验(扭体和热板)中均表现出剂量依赖性效应。该化合物在6.562 mg/kg剂量下显示出高抗伤害感受作用,几乎等同于5 mg/kg双氯芬酸。它还显示出高抗炎作用(剂量小于6.562 mg/kg),与参考药物双氯芬酸(5 mg/kg)和塞来昔布(100 mg/kg)相当。对接研究表明,这种喹啉衍生物可强烈抑制COX-2酶。

结论

QC显示出与参考药物相当的高抗伤害感受和抗炎作用,并且可通过抑制COX-2发挥其抗伤害感受和抗炎活性。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/433a/5425928/e40344e35e35/IJBMS-20-446-g001.jpg

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