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迷迭香水提物、迷迭香酸及其乙酰酯衍生物的体内镇痛和抗炎活性。

In vivo analgesic and anti-inflammatory activities of Rosmarinus officinalis aqueous extracts, rosmarinic acid and its acetyl ester derivative.

机构信息

Núcleo de Pesquisas em Ciências Exatas e Tecnológicas, Universidade de Franca, Franca, SP, Brazil.

出版信息

Pharm Biol. 2013 Sep;51(9):1087-90. doi: 10.3109/13880209.2013.776613. Epub 2013 Jun 5.

DOI:10.3109/13880209.2013.776613
PMID:23738822
Abstract

CONTEXT

Despite several pharmacological applications of Rosmarinus officinalis L. (Lamiaceae), studies on its analgesic and anti-inflammatory properties have been scarce.

OBJECTIVE

The aim of this work was to use in vivo models to evaluate the analgesic and anti-inflammatory activities of the aqueous extracts obtained from leaves (AEL) and stems (AES) of Rosmarinus officinalis, as well as its isolated compound--rosmarinic acid (RA). We also prepared and assessed the acetyl ester derivative of RA.

MATERIALS AND METHODS

The analgesic activity was evaluated using abdominal constriction and formalin tests. For the evaluation of the anti-inflammatory effects, carrageenin-induced paw edema in rats were used. The extracts were used at doses of 100, 200 and 400 mg kg⁻¹ compounds were tested at 10, 20 and 40 mg kg⁻¹.

RESULTS

Orally administered AEL, AES and RA were not significantly active at any of the doses tested during the abdominal constriction test; the acetyl ester derivative of RA displayed significant analgesic activity. In the carrageenin-induced paw edema assay, the acetyl derivative of RA at all the tested doses produced significant anti-inflammatory effects and reduced the number of paw licks in the second phase of the formalin test.

DISCUSSION AND CONCLUSION

The results suggest that the analgesic effects of the acetyl derivative of RA operate via a peripheral-mediated mechanism. The acetyl ester derivative of RA is potentially applicable as a new lead compound for the management of pain and inflammation.

摘要

背景

尽管迷迭香(唇形科)有多种药理学应用,但对其镇痛和抗炎特性的研究却很少。

目的

本工作的目的是使用体内模型来评估迷迭香叶(AEL)和茎(AES)的水提物以及其分离化合物迷迭香酸(RA)的镇痛和抗炎活性。我们还制备并评估了 RA 的乙酰酯衍生物。

材料和方法

采用腹部收缩和福尔马林试验评估镇痛活性。用角叉菜胶诱导的大鼠足肿胀来评价抗炎作用。提取物以 100、200 和 400mg/kg 的剂量使用,化合物以 10、20 和 40mg/kg 的剂量使用。

结果

在腹部收缩试验中,口服给予的 AEL、AES 和 RA 在测试的任何剂量下均无明显活性;RA 的乙酰酯衍生物具有显著的镇痛活性。在角叉菜胶诱导的足肿胀试验中,RA 的乙酰衍生物在所有测试剂量下均产生显著的抗炎作用,并减少了福尔马林试验第二阶段的足舔次数。

讨论和结论

结果表明,RA 的乙酰衍生物的镇痛作用通过外周介导的机制发挥作用。RA 的乙酰酯衍生物有可能作为一种新型先导化合物,用于疼痛和炎症的管理。

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