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离体和体内抗炎活性及雪兔子的化学成分研究。

In vitro and in vivo anti-inflammatory activity and chemical composition of Renealmia petasites Gagnep.

机构信息

Programa de Pós-Graduação Em Ciências Farmacêuticas, Laboratório de Produtos Naturais, Universidade Vila Velha, Av. Comissário José Dantas de Melo, 21, Boa Vista, Vila Velha, ES, 29102-920, Brazil.

Laboratório de Produtos Bioativos, Curso de Farmácia, Universidade Federal do Rio de Janeiro, Campus Macaé, Macaé, Brazil.

出版信息

Inflammopharmacology. 2021 Apr;29(2):451-465. doi: 10.1007/s10787-020-00786-4. Epub 2021 Jan 16.

Abstract

The study aimed to investigate the chemical composition and the anti-inflammatory activity of the hydroethanolic rhizomes, stems, and leaf extracts of Renealmia petasites using in vitro and in vivo assays. The chemical composition of the extracts was characterized in a linear iron trap mass spectrometer. Total phenolic, flavonoid, and tannin content were determined by spectrophotometry analyses. In vitro anti-inflammatory activity was investigated in lipopolysaccharide-stimulated macrophages evaluating the influence on the production of superoxide anion (O), nitric oxide (NO), and the pro-inflammatory cytokines tumor necrosis factor (TNF-α) and interleukin-6 (IL-6). In vivo effects were determined using the air pouch model in which were inoculated carrageenan and thereafter treated with 50 mg/kg of the hydroethanolic extracts of R. petasites. After 4 and 24 h, the cellular influx, protein exudation, cytokines, and nitric oxide were evaluated. Eight compounds were tentatively identified in the R. petasites extracts, suggesting five diarylheptanoids, one flavonoid, and two fatty alcohols. The in vitro results showed that the extracts were capable of blocking free radicals and/or inhibiting their intracellular actions by inhibiting the production of important mediators of the inflammatory process, such as NO, O, TNF-α, and IL-6. In vivo, R. petasites significantly decrease the influx of leukocytes, mainly neutrophils, protein exudation, NO, TNF-α, and IL-6 concentration in the air pouch model. The results evidenced that R. petasites can be considered a promising alternative therapy for the treatment and management of osteoarthritis and other inflammatory diseases.

摘要

本研究旨在采用体外和体内试验研究山蒟根茎、茎和叶的水乙醇提取物的化学成分和抗炎活性。使用线性铁陷阱质谱仪对提取物的化学成分进行了表征。通过分光光度分析测定了总酚、类黄酮和单宁的含量。在脂多糖刺激的巨噬细胞中研究了体外抗炎活性,评估了对超氧阴离子(O)、一氧化氮(NO)和促炎细胞因子肿瘤坏死因子(TNF-α)和白细胞介素-6(IL-6)产生的影响。使用气囊模型确定体内作用,在气囊中接种角叉菜胶,然后用 50mg/kg 的山蒟水乙醇提取物进行处理。在 4 小时和 24 小时后,评估细胞内流入、蛋白渗出、细胞因子和一氧化氮。在山蒟提取物中初步鉴定了 8 种化合物,提示有 5 种二芳基庚烷、1 种类黄酮和 2 种脂肪醇。体外结果表明,提取物能够通过阻断自由基和/或抑制其在细胞内的作用来阻止炎症过程中的重要介质(如 NO、O、TNF-α和 IL-6)的产生。在体内,山蒟明显减少了白细胞(主要是中性粒细胞)的流入、蛋白渗出、NO、TNF-α和 IL-6 在气囊模型中的浓度。结果表明,山蒟可被视为治疗和管理骨关节炎和其他炎症性疾病的有前途的替代疗法。

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