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苦参废渣的体内和体外抗炎作用。

In vivo and in vitro anti-inflammatory effects of Sophora flavescens residues.

机构信息

Key Laboratory of State Administration of Traditional Chinese Medicine for Production & Development of Cantonese Medicinal Materials/School of Traditional Chinese Medicine, Guangdong Pharmaceutical University, Guangzhou Higher Education Mega Center, 280 Wai Huan Dong Road, Guangzhou 510006, PR China.

Guangdong Provincial Key Laboratory of Pharmaceutical Bioactive Substances/School of Basic Courses, Guangdong Pharmaceutical University, Guangzhou Higher Education Mega Center, 280 Wai Huan Dong Road, Guangzhou 510006, PR China.

出版信息

J Ethnopharmacol. 2018 Oct 5;224:497-503. doi: 10.1016/j.jep.2018.06.019. Epub 2018 Jun 18.

Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

The dried roots of Sophora flavescens Ait. (Leguminosae) is traditionally used as antipyretic medicine to reduce inflammation. It is well known that alkaloids and flavonoids are the main constituents of S. flavescens. However, the clinical researches and applications of S. flavescens is mainly based on its water-extracted alkaloids, its flavonoids may still remain in residues and have been underused. With development and manufacturing of S. flavescens in recent years, more herb residues are being produced. Since they are typically treated as waste and dumped openly in landfill sites, which can cause pollution, there is a great need to explore these wastes as recyclable resources and increase their added value. To date, whether other bioactive components would be found in the residues of S. flavescens is still unknown. If the extraction method of these active ingredients was established, the residues of S. flavescens could be turned from the harm to a benefit and make great sense of the comprehensive utilization of S. flavescens resources. This study aimed to establish an extraction method of the residues of S. flavescens and investigate the anti-inflammatory effect of it both in vivo and in vitro.

MATERIALS AND METHODS

Dried S. flavescens were decocted with distilled water firstly, then the residues were powdered and extracted with ethyl acetate by using ultrasonic wave. HPLC was utilized to analyze the chemical constituents of the water extracts of S. flavescens (WSF) and the ethyl acetate extracts of residues of S. flavescens (RSF). In vivo, the anti-inflammatory effect of WSF and RSF were evaluated using the xylene-induced auricle edema, acetic acid-induced peritoneal permeability and carrageenan-induced hind paw edema methods. In vitro, the inhibitory activities of WSF and RSF on NO, TNF-α, IL-6 and MCP-1 production of LPS-treated RAW264.7 cells were measured.

RESULTS

The major ingredients of RSF were flavonoids, while WSF almost had no flavonoids. In vivo, WSF and RSF (200 mg/kg) could significantly inhibit the edema in the xylene-induced mice auricle edema and carrageenan-induced hind paw edema as well as the peritoneal permeability increased by acetic acid. They can also lower production levels of PGE in inflamed paw tissues. In vitro experimental results showed that RSF (25-100 μg/mL) could significantly inhibit the release of pro-inflammatory cytokines NO, TNF-α, IL-6 and MCP-1 on LPS-induced RAW264.7 cells. The in vitro suppress effect of WSF had no dose-response relationship.

CONCLUSIONS

The residues of S. flavescens had obvious flavonoids with anti-inflammatory activity. This study provided evidence for the reuse of residues from S. flavescens in the food additive, medicine and cosmetic industries.

摘要

民族药理学相关性

苦参(豆科)的干根传统上被用作退热药物来减轻炎症。众所周知,生物碱和黄酮类化合物是苦参的主要成分。然而,苦参的临床研究和应用主要基于其水提生物碱,其黄酮类化合物可能仍残留在残渣中而未被充分利用。随着近年来苦参的开发和制造,产生了更多的药渣。由于它们通常被视为废物并露天倾倒在垃圾填埋场,这可能会造成污染,因此迫切需要探索这些废物作为可回收资源并提高其附加值。迄今为止,苦参残渣中是否还会发现其他生物活性成分尚不清楚。如果建立了这些活性成分的提取方法,苦参残渣就可以变废为宝,对苦参资源的综合利用具有重要意义。本研究旨在建立苦参残渣的提取方法,并从体内和体外两方面研究其抗炎作用。

材料与方法

首先用蒸馏水煎煮苦参,然后将残渣粉碎,用超声波法用乙酸乙酯提取。采用高效液相色谱法分析苦参水提物(WSF)和苦参残渣的乙酸乙酯提取物(RSF)的化学成分。体内实验中,采用二甲苯致小鼠耳廓肿胀、醋酸致腹腔通透性增加和角叉菜胶致大鼠足肿胀模型评价 WSF 和 RSF 的抗炎作用。体外实验中,测定 WSF 和 RSF 对 LPS 诱导的 RAW264.7 细胞产生的 NO、TNF-α、IL-6 和 MCP-1 的抑制作用。

结果

RSF 的主要成分是黄酮类化合物,而 WSF 几乎不含黄酮类化合物。体内实验结果表明,WSF 和 RSF(200mg/kg)能显著抑制二甲苯致小鼠耳廓肿胀和角叉菜胶致大鼠足肿胀,以及醋酸致腹腔通透性增加,还能降低炎症组织中 PGE 的产生水平。体外实验结果表明,RSF(25-100μg/ml)能显著抑制 LPS 诱导的 RAW264.7 细胞产生促炎细胞因子 NO、TNF-α、IL-6 和 MCP-1。WSF 的体外抑制作用无剂量反应关系。

结论

苦参残渣具有明显的抗炎活性,含有黄酮类化合物。本研究为苦参残渣在食品添加剂、医药和化妆品行业的再利用提供了依据。

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