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小檗碱丰富提取物通过调节炎症生物标志物发挥抗炎潜力。

Anti-inflammatory potential of berberine-rich extract via modulation of inflammation biomarkers.

机构信息

Department of Bioinformatics & Biotechnology, Faculty of Life Sciences, Government College University, Faisalabad, Pakistan.

Department of Pharmacology, Faculty of Pharmaceutical Sciences, Government College University, Faisalabad, Pakistan.

出版信息

J Food Biochem. 2022 Dec;46(12):e14389. doi: 10.1111/jfbc.14389. Epub 2022 Sep 19.

Abstract

Berberine-rich extract (BRE) prepared from Berberis lycium root bark using green extraction approach and its marker compound berberine has a broad spectrum of clinical applications. Berberine's potential pharmacological effects include anticancer, antidiarrheal, antidiabetic, antimicrobial and anti-inflammatory activities. In current work, BRE and berberine were evaluated for their therapeutic prospects in inflammation models. The comparative effect of BRE and berberine against inflammation was determined through in vitro chemiluminescence technique. The in vivo anti-inflammatory evaluation of BRE and berberine (25, 75, and 125 mg/kg) compared to diclofenac (10 mg/kg) was performed in carrageenan and formaldehyde-induced inflammation in Wistar rats. Histopathological and biochemical studies were conducted to find the comparative anti-inflammatory potential of BRE and berberine on pathological hallmarks induced by formaldehyde. Moreover, the modulatory effects on inflammatory biomarkers were also investigated through qPCR. ELISA (enzyme-linked immunoassay test assay) was performed to investigate the expression of pathological protein biomarkers like TNF-α and IL-6 and levels of antioxidant enzymes were estimated in liver homogenates. Both BRE and berberine markedly (p < .001) reduced paw diameter and inflammation in carrageenan and formaldehyde-induced inflammation. The levels of antioxidant enzymes were recovered (p < .001) by BRE and berberine treatments, and compared to the formaldehyde-treated inflammation model. Both BRE and berberine remarkably downregulated the mRNA and protein expression of inflammatory biomarkers. BRE similar to berberine mitigated the level of antioxidant enzymes in liver homogenate. The undertaken study suggests that BRE, a natural, green, and therapeutically bioequivalent to berberine could be used as an economical phytomedicine in the treatment of inflammatory disorders. PRACTICAL APPLICATIONS: Anti-inflammatory drugs like NSAIDS are associated with serious adverse effects like gastrointestinal ulcer, worsening of preexisting cardiovascular disorders, and renal failure. Therefore, there is a constant demand to develop novel, inexpensive therapeutic strategies to treat the inflammatory disorder with the least harmful effects. Pure phytochemicals with anti-inflammatory potential are costly and hard to isolate, therefore green microwave-assisted extraction technique is developed to get the rich bioequivalent extract. Berberis lycium a medicinal plant with berberine as a major bioactive constituent, has wide acceptance in traditionally used medicine and as food. Pharmacological studies revealed its hepatoprotective, anticancer, antidiabetic, and antihypertensive activities. BRE was prepared by green microwave-assisted extraction and enrichment by resin column to get a higher yield of berberine. The comparative anti-inflammatory effect of BRE and berberine was determined by in vitro and in vivo studies. Results obtained from this experimental work contribute beneficial guidance that reinforces the use of the BRE to treat inflammatory disorders.

摘要

从枸杞根皮中用绿色提取方法制备的小檗碱含量丰富的提取物(BRE)及其标记化合物小檗碱具有广泛的临床应用。小檗碱的潜在药理作用包括抗癌、抗腹泻、抗糖尿病、抗菌和抗炎作用。在当前的工作中,评估了 BRE 和小檗碱在炎症模型中的治疗前景。通过体外化学发光技术确定了 BRE 和小檗碱对抗炎症的比较效果。在卡拉胶和甲醛诱导的 Wistar 大鼠炎症中,与双氯芬酸钠(10mg/kg)相比,对 BRE(25、75 和 125mg/kg)和小檗碱的体内抗炎评价。进行了组织病理学和生化研究,以发现 BRE 和小檗碱对甲醛诱导的病理特征的比较抗炎潜力。此外,还通过 qPCR 研究了对炎症生物标志物的调节作用。通过酶联免疫吸附试验(ELISA)检测 TNF-α和 IL-6等病理蛋白生物标志物的表达,并估计肝匀浆中抗氧化酶的水平。BRE 和小檗碱均显著(p<.001)降低了卡拉胶和甲醛诱导的炎症中足趾直径和炎症。BRE 和小檗碱处理恢复了抗氧化酶的水平(p<.001),与甲醛处理的炎症模型相比。BRE 和小檗碱均显著下调了炎症生物标志物的 mRNA 和蛋白表达。BRE 与小檗碱一样,减轻了肝匀浆中抗氧化酶的水平。进行的研究表明,BRE 是一种天然的、绿色的、与小檗碱治疗等效的药物,可作为治疗炎症性疾病的经济植物药。实际应用:非甾体抗炎药等抗炎药物与严重的不良反应有关,如胃肠道溃疡、现有心血管疾病恶化和肾衰竭。因此,不断需要开发新的、廉价的治疗策略,以对炎症性疾病进行治疗,而副作用最小。具有抗炎潜力的纯植物化学物质成本高,难以分离,因此开发了绿色微波辅助提取技术来获得富含生物等效物的提取物。枸杞是一种药用植物,小檗碱是其主要生物活性成分,在传统药物和食品中被广泛接受。药理研究显示其具有保肝、抗癌、抗糖尿病和降压作用。BRE 通过绿色微波辅助提取和树脂柱富集制备,以获得更高的小檗碱产量。通过体外和体内研究确定了 BRE 和小檗碱的比较抗炎作用。这项实验工作获得的结果提供了有益的指导,加强了 BRE 用于治疗炎症性疾病的使用。

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