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苦豆碱对小鼠化学诱导的神经性和炎性疼痛模型的镇痛活性。

The antinociceptive activity of harmicine on chemical-induced neurogenic and inflammatory pain models in mice.

机构信息

CPQBA, University of Campinas, PO Box 6171, 13083-970 Campinas-SP, Brazil.

出版信息

Pharmacol Biochem Behav. 2012 Jul;102(1):133-8. doi: 10.1016/j.pbb.2012.03.030. Epub 2012 Apr 6.

Abstract

Harmicine is a β-carboline alkaloid isolated and identified as a major active compound present in many plant species and marine invertebrates. This alkaloid exhibits a wide spectrum of pharmacological activities, including antispasmodic, antipyretic, and anticancer properties. This report described the antinociceptive properties of harmicine by means of chemical experimental models in order to evaluate the use for pain relief. The results demonstrating the potential analgesic properties of harmicine administered intraperitoneally were shown with the writhing test, reducing writhes around 60% (1 mg/kg), and in the formalin test, where harmicine was more effective toward neurogenic (reducing reaction time around 60%, 1 mg/kg) than inflammatory (68% reduction, 10 mg/kg) pain responses. Furthermore, these effects may operate via vanilloid receptors as revealed by the capsaicin test (41% reduction, with 3 mg/kg), as well as via peripheral glutamate receptors as shown by the glutamate test (50% reduction, with 1 mg/kg). Moreover, the opioid antagonist naloxone hydrochloride did not interfere in the antinociceptive properties of harmicine in the writhing test, revealing that this effect may not have a relationship with the opioid systems. Concluding, this report highlights harmicine as a new candidate to be used as analgesic in the future. Therefore, further studies are being undertaken in order to understand the exact mechanisms involved with the antinociceptive properties of harmicine.

摘要

哈尔明碱是一种β-咔啉生物碱,已被分离并鉴定为许多植物物种和海洋无脊椎动物中存在的主要活性化合物。该生物碱具有广泛的药理活性,包括抗痉挛、解热和抗癌特性。本报告通过化学实验模型描述了哈尔明碱的镇痛特性,以评估其用于缓解疼痛的用途。结果表明,哈尔明碱腹腔内给药具有潜在的镇痛作用,扭体试验中扭体减少约 60%(1mg/kg),在福尔马林试验中,哈尔明碱对神经源性疼痛(反应时间减少约 60%,1mg/kg)的作用比对炎症性疼痛(反应时间减少 68%,10mg/kg)更有效。此外,这些作用可能通过辣椒素试验(3mg/kg 时减少 41%)通过香草素受体起作用,也可能通过谷氨酸试验(1mg/kg 时减少 50%)通过外周谷氨酸受体起作用。此外,阿片受体拮抗剂盐酸纳洛酮在扭体试验中并未干扰哈尔明碱的镇痛作用,表明该作用可能与阿片系统无关。综上所述,本报告强调了哈尔明碱作为未来镇痛剂的新候选药物。因此,正在进行进一步的研究,以了解哈尔明碱镇痛作用的确切机制。

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