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邻甲氧基苯酚具有抗伤害感受和抗炎活性。

Ortho-eugenol exhibits anti-nociceptive and anti-inflammatory activities.

作者信息

Fonsêca Diogo V, Salgado Paula R R, Aragão Neto Humberto de C, Golzio Adriana M F O, Caldas Filho Marcelo R D, Melo Cynthia G F, Leite Fagner C, Piuvezam Marcia R, Pordeus Liana Clébia de Morais, Barbosa Filho José M, Almeida Reinaldo N

机构信息

Postgraduate Program in Natural Products and Bioactive Synthetics (PgPNSB), Federal University of Paraíba (UFPB), João Pessoa, PB, Brazil; Laboratory of Psychopharmacology, Federal University of Paraíba (UFPB), João Pessoa, PB, Brazil.

Laboratory of Psychopharmacology, Federal University of Paraíba (UFPB), João Pessoa, PB, Brazil.

出版信息

Int Immunopharmacol. 2016 Sep;38:402-8. doi: 10.1016/j.intimp.2016.06.005. Epub 2016 Jun 27.

DOI:10.1016/j.intimp.2016.06.005
PMID:27355133
Abstract

Ortho-eugenol is a much used phenylpropanoid whose ability to reduce pain and inflammation has never been studied. Researching ortho-eugenol's antinociceptive and anti-inflammatory activity, and its possible mechanisms of action is therefore of interest. The administration of vehicle, ortho-eugenol (50, 75 and 100mg/kg i.p.), morphine (6mg/kg, i.p.) or dexamethasone (2mg/kg, s.c.) occurred 30min before the completion of pharmacological tests. Pretreatment with ortho-eugenol did not change motor coordination test results, but reduced the number of writhes and licking times in the writhing test and glutamate test, respectively. The reaction time from thermal stimulus was significantly increased in the hot plate test after administration of ortho-eugenol. Treatment with yohimbine reversed the antinociceptive effect of ortho-eugenol, suggesting involvement of the adrenergic system. In anti-inflammatory tests, ortho-eugenol inhibited acetic acid induced vascular permeability and leukocyte migration, reducing TNF-α and IL-1β by virtue of its suppression of NF-κB and p38 phosphorylated forms in the peritonitis test. From these results, ortho-eugenol antinociceptive effects mediated by the adrenergic system and anti-inflammatory activity through regulation of proinflammatory cytokines and phosphorylation of NF-kB and p38 become evident for the first time.

摘要

邻丁香酚是一种常用的苯丙烷类化合物,其减轻疼痛和炎症的能力从未被研究过。因此,研究邻丁香酚的抗伤害感受和抗炎活性及其可能的作用机制具有重要意义。在完成药理测试前30分钟,分别给予溶媒、邻丁香酚(50、75和100mg/kg腹腔注射)、吗啡(6mg/kg,腹腔注射)或地塞米松(2mg/kg,皮下注射)。邻丁香酚预处理并未改变运动协调测试结果,但分别减少了扭体试验和谷氨酸试验中的扭体次数和舔舐次数。在热板试验中,给予邻丁香酚后热刺激的反应时间显著延长。育亨宾处理可逆转邻丁香酚的抗伤害感受作用,提示肾上腺素能系统参与其中。在抗炎试验中,邻丁香酚抑制乙酸诱导的血管通透性和白细胞迁移,在腹膜炎试验中通过抑制NF-κB和p38磷酸化形式减少TNF-α和IL-1β。从这些结果来看,邻丁香酚由肾上腺素能系统介导的抗伤害感受作用以及通过调节促炎细胞因子和NF-κB及p38磷酸化发挥的抗炎活性首次变得明显。

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