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富含苯丙素的冬叶有效部位的抗炎和镇痛活性。

Anti-inflammatory and antinociceptive activities of a phenylpropanoid-enriched fraction of Duguetia furfuracea.

机构信息

Laboratório de Farmacologia da Dor e Inflamação, Universidade Federal de São João del-Rei, Divinópolis, 35501-296, Brazil.

Laboratório de Farmacognosia/Química de Produtos Naturais, Universidade Federal de São João del-Rei, Divinópolis, Brazil.

出版信息

Inflammopharmacology. 2021 Apr;29(2):409-422. doi: 10.1007/s10787-020-00775-7. Epub 2020 Nov 6.

DOI:10.1007/s10787-020-00775-7
PMID:33156477
Abstract

A previous study reported the in vivo anti-inflammatory and antinociceptive activities of essential oil of the underground stem bark of Duguetia furfuracea, termed EODf. This study aimed to obtain a phenylpropanoid-enriched fraction from the D. furfuracea (EFDf) essential oil and to investigate its anti-inflammatory and antinociceptive effects. The chemical composition of the EFDf was determined by gas chromatography-mass spectrometry (GC-MS). The in vivo anti-inflammatory activity was evaluated with a lipopolysaccharide (LPS)-induced paw oedema model. The effects of the EFDf on the polymorphonuclear leukocyte recruitment and the inducible nitric oxide synthase (iNOS) expression were evaluated in mice footpads. Moreover, the in vivo antinociceptive effect was assayed using the formalin test and the LPS-induced thermal hyperalgesia model. In the EFDf, 8 major compounds were identified, with α-asarone (36.4%) and 2,4,5-trimethoxystyrene (27.8%) the main constituents. A higher concentration of phenylpropanoid derivatives was found in the EFDf, 64.2% compared to the EODf (38%). The oral (p.o.) treatment with the EFDf at a dose of 3 mg/kg significantly attenuated the paw oedema, polymorphonuclear leukocyte migration, iNOS expression, and tumour necrosis factor alpha (TNF-α) production. The EFDf (10 and 30 mg/kg) also inhibited both phases of the formalin test and caused a significant increase in the reaction time in the LPS-induced thermal hyperalgesia model. Finally, EFDf-treated animals did not show any alteration of motor coordination. The results suggest that the enrichment of 2,4,5-trimethoxystyrene and α-asarone enhances the anti-inflammatory activity of the EFDf compared to the EODf. In contrast, the antinociception promoted by the EFDf was similar to the EODf and was mediated via activation of adenosinergic and opioidergic receptors.

摘要

先前的研究报道了地下茎皮的 essential oil of the underground stem bark of Duguetia furfuracea(D. furfuracea)具有抗炎和镇痛活性,称为 EODf。本研究旨在从 D. furfuracea 中获得富含苯丙素的馏分(EFDf),并研究其抗炎和镇痛作用。通过气相色谱-质谱联用(GC-MS)确定 EFDf 的化学成分。采用脂多糖(LPS)诱导的爪肿胀模型评价其体内抗炎活性。评估 EFDf 对多形核白细胞募集和诱导型一氧化氮合酶(iNOS)表达的影响。此外,通过福尔马林试验和 LPS 诱导的热痛觉过敏模型测定体内镇痛作用。在 EFDf 中,鉴定出 8 种主要化合物,其中α-细辛脑(36.4%)和 2,4,5-三甲氧基苯乙烯(27.8%)为主要成分。与 EODf(38%)相比,EFDf 中的苯丙素衍生物浓度更高,为 64.2%。EFDf(3mg/kg)口服(p.o.)治疗可显著减轻爪肿胀、多形核白细胞迁移、iNOS 表达和肿瘤坏死因子-α(TNF-α)产生。EFDf(10 和 30mg/kg)还抑制了福尔马林试验的两个阶段,并导致 LPS 诱导的热痛觉过敏模型中反应时间显著增加。最后,EFDf 处理的动物没有表现出任何运动协调能力的改变。结果表明,2,4,5-三甲氧基苯乙烯和α-细辛脑的富集增强了 EFDf 相对于 EODf 的抗炎活性。相比之下,EFDf 促进的镇痛作用与 EODf 相似,是通过激活腺苷能和阿片能受体介导的。

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