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具有高水平类黄酮的组分抑制伤害感受的外周和中枢机制。

fraction with a high level of flavonoid inhibits peripheral and central mechanisms of nociception.

作者信息

Fernandes Daniele Corrêa, Martins Bruna Paiva, Silva Girlaine Pereira da, Fonseca Eduardo Nunes da, Santos Shirley Vânia Moura, Velozo Leosvaldo Salazar Marques, Gayer Carlos Roberto Machado, Sabino Kátia Costa de Carvalho, Coelho Marsen Garcia Pinto

机构信息

Department of Biochemistry and Institute of Biology Roberto Alcantara Gomes, State University of Rio de Janeiro, Rio de Janeiro, Brazil.

Department of Plant Biology, Institute of Biology Roberto Alcantara Gomes, State University of Rio de Janeiro, Rio de Janeiro, Brazil.

出版信息

J Tradit Complement Med. 2021 Jul 15;12(2):123-130. doi: 10.1016/j.jtcme.2021.07.001. eCollection 2022 Mar.

DOI:10.1016/j.jtcme.2021.07.001
PMID:35528477
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC9072821/
Abstract

BACKGROUND AND AIM

(Kunth.) Micheli is popularly used for acute and chronic inflammatory conditions. The anti-inflammatory activity was previously demonstrated for its flavonoid-enriched fractions. The aim of this work assessed the antinociceptive properties of both aqueous extract and its fractions.

EXPERIMENTAL PROCEDURE

The antinociceptive activity was determined by acetic acid-induced writhing, formalin test, tail immersion test, hot-plate test, xylene-induced ear edema methods, and the evaluation of its mechanism was performed in the writhing model. The aqueous extract of (AEEm) was fractionated, yielding Fr20, and Fr40. Fr40 composition was determined by HPLC-DAD-ESI-MS.

RESULTS AND CONCLUSION

Fr20 (all doses) and Fr40 (100 mg/kg) reduced the nociception in the tail-flick model. Both fractions increased the percentage of maximum possible effect with 25 mg/kg, in the hot-plate assay, at 60 min, while AEEm reduced pain only with 50 and 100 mg/kg. There was a reduction in xylene-edema index, with Fr40 (25 mg/kg), AEEm (50 mg/kg) and Fr20 (50 mg/kg). All doses of AEEm, Fr20, and Fr40 reduced both phases of the formalin model. In the abdominal contortion model, Fr40 presented the highest activity, reducing 96% of contortions and its antinociceptive mechanism was evaluated. The results indicated the involvement of NO and adrenergic activation pathways. The main components of Fr40 are swertisin, swertiajaponin, isoorientin 7,3'-dimethyl ether, swertisin-O-rhamnoside, isoorientin, isovitexin, isovitexin-Orhamnoside, and isovitexin-7-O-glucoside. The aqueous extract of leaves and its fractions exhibited significant analgesic effect, mediated through both peripheral and central mechanisms being considered a potentially antinociceptive drug.

摘要

背景与目的

(Kunth.)Micheli常用于急慢性炎症。先前已证明其富含黄酮类的组分具有抗炎活性。本研究的目的是评估水提取物及其组分的抗伤害感受特性。

实验步骤

通过醋酸诱导扭体试验、福尔马林试验、尾浸试验、热板试验、二甲苯诱导耳肿胀试验测定抗伤害感受活性,并在扭体模型中评估其作用机制。对(AEEm)的水提取物进行分离,得到Fr20和Fr40。通过HPLC-DAD-ESI-MS测定Fr40的成分。

结果与结论

Fr20(所有剂量)和Fr40(100mg/kg)在甩尾模型中降低了伤害感受。在热板试验中,两种组分在60分钟时以25mg/kg剂量增加了最大可能效应的百分比,而AEEm仅在50和100mg/kg剂量时减轻疼痛。Fr40(25mg/kg)、AEEm(50mg/kg)和Fr20(50mg/kg)使二甲苯肿胀指数降低。AEEm、Fr20和Fr40的所有剂量均降低了福尔马林模型的两个阶段。在腹部扭体模型中,Fr40表现出最高活性,减少了96%的扭体次数,并评估了其抗伤害感受机制。结果表明涉及一氧化氮和肾上腺素能激活途径。Fr40的主要成分是獐牙菜苷、獐牙菜苦苷二甲基醚、异荭草素、獐牙菜苷-O-鼠李糖苷、异荭草素、异牡荆素、异牡荆素-鼠李糖苷和异牡荆素-7-O-葡萄糖苷。叶的水提取物及其组分通过外周和中枢机制均表现出显著的镇痛作用,被认为是一种潜在的抗伤害感受药物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/bed72364e6d4/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/662619da4df3/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/a5bdeb2d8b0b/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/67a8bfd305f0/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/b21e11b76a8b/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/bed72364e6d4/gr4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/662619da4df3/ga1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/a5bdeb2d8b0b/gr1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/67a8bfd305f0/gr2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/b21e11b76a8b/gr3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/788c/9072821/bed72364e6d4/gr4.jpg

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