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4-苯基硒基-7-氯喹啉,一种含硒的新型喹啉衍生物,具有潜在的抗伤害感受和抗炎作用。

4-Phenylselenyl-7-chloroquinoline, a new quinoline derivative containing selenium, has potential antinociceptive and anti-inflammatory actions.

作者信息

Pinz Mikaela, Reis Angélica S, Duarte Vanessa, da Rocha Márcia J, Goldani Bruna S, Alves Diego, Savegnago Lucielli, Luchese Cristiane, Wilhelm Ethel A

机构信息

Grupo de Pesquisa em Neurobiotecnologia - GPN, CCQFA/CDTec, Universidade Federal de Pelotas, UFPel, Pelotas, RS, Brazil.

Laboratório de Síntese Orgânica Limpa - LASOL - CCQFA - Universidade Federal de Pelotas, UFPel, P.O. Box 354, 96010-900 Pelotas, RS, Brazil.

出版信息

Eur J Pharmacol. 2016 Jun 5;780:122-8. doi: 10.1016/j.ejphar.2016.03.039. Epub 2016 Mar 25.

DOI:10.1016/j.ejphar.2016.03.039
PMID:27020552
Abstract

The development of new drugs to treat painful and inflammatory clinical conditions continues to be of great interest. The present study evaluated the antinociceptive and anti-inflammatory effects of 4-phenylselenyl-7-chloroquinoline (4-PSQ). Mice were orally (p.o.) pretreated with 4-PSQ (0.1-25mg/kg), meloxicam (25mg/kg, a reference drug) or vehicle, 30min prior to the acetic acid, formalin, hot-plate and open-field tests. 4-PSQ reduced abdominal writhing induced by acetic acid and it caused an increase in latency time in the hot-plate test. 4-PSQ inhibited early and late phases of nociception and reduced the paw edema caused by formalin. Locomotor and exploratory activities in the open field test were not altered by treatments. In addition, a time-response curve was carried out by administration of 4-PSQ (25mg/kg; p.o.) at different times before the acetic acid injection. The antinociceptive effect in inhibiting acetic acid-induced abdominal writhing of 4-PSQ started at 0.5h and remained significant up to 4h after administration. Indeed, the anti-inflammatory and antioxidant properties of 4-PSQ were investigated. 4-PSQ diminished the edema formation and decreased the myeloperoxidase activity and reactive species levels induced by croton oil in the ear tissue. 4-PSQ partially protected against the decrease of the 2,2'-Azinobis-3-ethylbenzothiazoline 6-sulfonic acid (ABTS) and 2,2-diphenyl-1-picrylhydrazyl (DPPH) levels induced by croton oil. Meloxicam presented similar results for 4-PSQ in tests evaluated. These results demonstrated that 4-PSQ exerts acute anti-inflammatory and antinociceptive actions, suggesting that it may represent an alternative in the development of future new therapeutic strategies.

摘要

开发用于治疗疼痛和炎症性临床病症的新药一直备受关注。本研究评估了4-苯基硒基-7-氯喹啉(4-PSQ)的抗伤害感受和抗炎作用。在进行醋酸、福尔马林、热板和旷场试验前30分钟,给小鼠口服(p.o.)4-PSQ(0.1 - 25mg/kg)、美洛昔康(25mg/kg,一种参比药物)或赋形剂。4-PSQ减少了醋酸诱导的腹部扭体反应,并使热板试验中的潜伏期延长。4-PSQ抑制了伤害感受的早期和晚期阶段,并减轻了福尔马林引起的爪部水肿。处理并未改变旷场试验中的运动和探索活动。此外,在醋酸注射前不同时间给予4-PSQ(25mg/kg;p.o.)绘制了时间-反应曲线。4-PSQ抑制醋酸诱导的腹部扭体反应的抗伤害感受作用在给药后0.5小时开始,直至4小时仍具有显著意义。实际上,对4-PSQ的抗炎和抗氧化特性进行了研究。4-PSQ减少了巴豆油诱导的耳部组织水肿形成,并降低了髓过氧化物酶活性和活性物质水平。4-PSQ部分保护了巴豆油诱导的2,2'-联氮双(3-乙基苯并噻唑啉-6-磺酸)(ABTS)和2,2-二苯基-1-苦基肼(DPPH)水平的降低。在评估的试验中,美洛昔康呈现出与4-PSQ相似的结果。这些结果表明,4-PSQ具有急性抗炎和抗伤害感受作用,提示它可能代表未来新治疗策略开发中的一种选择。

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