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首页> 外文期刊>Journal of Pharmacy and Pharmacology >Evaluation of the anti‐inflammatory activity of Tinospora cordifolia Tinospora cordifolia (Willd.) Miers chloroform extract – a preclinical study
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Evaluation of the anti‐inflammatory activity of Tinospora cordifolia Tinospora cordifolia (Willd.) Miers chloroform extract – a preclinical study

机译:inospora Cordifolia tinospora肠肠道(Willd.)Miers氯仿提取物的评估 - 一种临床前研究

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Abstract Objectives Tinospora cordifolia (Willd.) Miers is an inevitable ingredient of Ayurvedic rasayanas for the treatment of disorders with unregulated inflammation. However, studies regarding the mechanism of anti‐inflammatory potential of this plant at the molecular level are lacking. Methods In vitro evaluations were conducted in RAW 264.7 macrophages which were preincubated with chloroform extract of T.?cordifolia ( CETC ) and subsequently stimulated with LPS . The expressions of COX ‐2, TNF ‐α and iNOS genes were analysed by SQRT ‐ PCR and Western blot, cytokines ( IL ‐6, IL ‐1β and PGE 2 ) levels by ELISA , NF ‐κB activation and p38 MAPK phosphorylation by Immunoblot and confocal imaging. Anti‐inflammatory potential of CETC was validated further in a rat model of carrageenan‐induced hind paw edema. Phytochemical characterisation was carried out using the HPLC technique. Key findings The LPS ‐induced upregulation of proinflammatory biomarkers was significantly prevented by CETC , without inhibiting COX ‐1. CETC ‐ and LPS ‐incubated cells showed reduced phosphorylated p38 MAPK levels, and higher levels NF ‐κB were retained in cytoplasm. Rats pretreated with CETC showed a statistically significant decrease in paw oedema ( P? ≤ ? 0.05), and HPLC characterisation detected stigmasterol and β‐sitosterol. The LD 50 of CETC lies above 2000?mg/Kg body weight. Conclusions These findings encourage us strongly to focus on CETC to develop anti‐inflammatory drugs with lower degree of inhibition to the constitutively expressing COX ‐1.
机译:摘要目标Tinospora Cordifolia(Willd。)Miers是Ayurvedic Rasayanas的不可避免的成分,用于治疗疾病,患有未调节的炎症。然而,缺乏关于该植物在分子水平的抗炎潜力机制的研究。在体外评价中的方法是在原始的264.7巨噬细胞中进行的,该巨噬细胞与T.?cordifolia(CETc)的氯仿提取物预孵育,随后用LPS刺激。通过SQRT - PCR和Western印迹,细胞因子(IL-6,IL-1β和PGE 2)通过ELISA,NF-κB活化和P38 MAPK磷酸化进行分析COX -2,TNF-α和InOS基因的表达和共聚焦成像。 CETC的抗炎潜力在角叉菜胶诱导的后爪水肿的大鼠模型中进一步验证。使用HPLC技术进行植物化学表征。关键发现通过CETC显着防止了LPS-诱导促炎生物标志物的上调,无需抑制COX -1。 CETC - 和LPS-incubated细胞显示出降低的磷酸化P38 MAPK水平,并且较高水平的NF-κB被保留在细胞质中。用CETC预处理的大鼠显示爪子水肿(P≤≤0.05)的统计学上显着降低,HPLC表征检测到STIGMASTEROL和β-谷甾醇。 CETC的LD 50位于2000〜20℃/千克体重以上。结论这些调查结果鼓励我们强烈关注CETC,形成抑制抑制程度较低的抗炎药,对组成型COX -1。

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