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(-)-α-红没药醇在啮齿类动物中的抗伤害感受和抗炎活性。

Anti-nociceptive and anti-inflammatory activities of (-)-α-bisabolol in rodents.

机构信息

Universidade Federal do Ceará, Fortaleza, Brazil.

出版信息

Naunyn Schmiedebergs Arch Pharmacol. 2011 Dec;384(6):525-33. doi: 10.1007/s00210-011-0679-x. Epub 2011 Aug 26.

Abstract

(-)-α-Bisabolol is an unsaturated, optically active sesquiterpene alcohol obtained by the direct distillation of essential oil from plants such as Vanillosmopsis erythropappa and Matricaria chamomilla. (-)-α-Bisabolol has generated considerable economic interest, as it possesses a delicate floral odour and has been shown to have antiseptic and gastroprotective activities. In this study, (-)-α-bisabolol was tested in standardised rodent models by gavage administration at doses of 100 and 200 mg/kg in the models of inflammation and 25 and 50 mg/kg in the models of nociception. In the inflammatory models of paw oedema induced by carrageenan and dextran, the mice treated with (-)-α-bisabolol showed smaller oedemas compared to animals treated only with the vehicle. (-)-α-Bisabolol was capable of reducing paw oedemas induced by 5-HT but not oedemas induced by histamine. (-)-α-Bisabolol demonstrated anti-nociceptive activity in the models of visceral nociception induced by acetic acid and in the second phase of the nociception test induced by the intraplantar administration of formalin. (-)-α-Bisabolol did not have any effect in a thermal nociception model using a hot plate but was able to diminish mechanical inflammatory hypernociception evoked by carrageenan. These findings suggest that the anti-nociceptive action of (-)-α-bisabolol is not linked to a central mechanism but instead is related to the inflammatory process. (-)-α-Bisabolol was able to decrease leukocyte migration, protein extravasations and the amount of TNF-α to the peritoneal cavity in response to carrageenan. Additionally, (-)-α-bisabolol reduced neutrophil degranulation in response to phorbol-myristate-acetate. We demonstrate, for the first time, the peripheral anti-inflammatory and anti-nociceptive activities of (-)-α-bisabolol.

摘要

(-)-α- 红没药醇是一种不饱和、光学活性的倍半萜醇,可通过直接蒸馏香草醇或母菊薁从植物精油中获得。(-)-α- 红没药醇具有相当大的经济价值,因为它具有细腻的花香,并已被证明具有防腐和胃保护活性。在这项研究中,(-)-α- 红没药醇通过灌胃给药在炎症模型中以 100 和 200mg/kg 的剂量和在疼痛模型中以 25 和 50mg/kg 的剂量进行了标准化啮齿动物模型的测试。在由卡拉胶和右旋糖酐诱导的爪水肿炎症模型中,与仅用载体处理的动物相比,用(-)-α- 红没药醇处理的小鼠的水肿较小。(-)-α- 红没药醇能够减少 5-HT 诱导的爪水肿,但不能减少组胺诱导的水肿。(-)-α- 红没药醇在由乙酸诱导的内脏疼痛模型和由福尔马林皮内给药诱导的疼痛测试的第二阶段中表现出抗伤害感受作用。(-)-α- 红没药醇在使用热板的热伤害感受模型中没有任何作用,但能够减轻由卡拉胶引起的机械性炎症性超敏反应。这些发现表明,(-)-α- 红没药醇的抗伤害感受作用与中枢机制无关,而是与炎症过程有关。(-)-α- 红没药醇能够减少白细胞迁移、蛋白渗出和对卡拉胶的腹腔中 TNF-α 的量。此外,(-)-α- 红没药醇减少了对佛波醇-12,13- 二丁酸酯的中性粒细胞脱颗粒。我们首次证明了(-)-α- 红没药醇的外周抗炎和抗伤害感受作用。

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