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单叶骆驼蓬主要酚类物质的抗氧化和抗炎活性

Antioxidant and anti-inflammatory activities of the major phenolics from Zygophyllum simplex L.

作者信息

Abdallah Hossam M, Esmat Ahmed

机构信息

Department of Natural Products and Alternative Medicine, Faculty of Pharmacy, King Abdulaziz University, Jeddah 21589, Saudi Arabia; Department of Pharmacognosy, Faculty of Pharmacy, Cairo University, Cairo 11562, Egypt.

Department of Pharmacology and Toxicology, Faculty of Pharmacy, Ain Shams University, Cairo 11566, Egypt.

出版信息

J Ethnopharmacol. 2017 Jun 9;205:51-56. doi: 10.1016/j.jep.2017.04.022. Epub 2017 Apr 29.

DOI:10.1016/j.jep.2017.04.022
PMID:28465252
Abstract

ETHNOPHARMACOLOGICAL RELEVANCE

Zygophyllum simplex L. is a halophyte plant that follows Zygophyllaceae. The plant is growing in arid and semiarid regions. It has been used traditionally in Arabic region to treat gout, asthma and inflammation.

AIM OF STUDY

Although ant-inflammatory activity has been reported for this plant, this study aimed to isolate and identify the major constituents of Zygophyllum simplex L., as well as assessing their antioxidant and anti-inflammatory activities in-vitro. In this study, the mechanism of anti-inflammatory activity of the isolated compounds was assessed.

MATERIALS AND METHODS

Defatted fraction of the total methanol extract of the aerial parts of Z. simplex was repeatedly chromatographed on Diaion HP-20, polyamide, and RP columns to give five major phenolic compounds. The identity of the purified compounds was established by NMR experiments and comparing with previously known analogs. Moreover, the antioxidant and anti-inflammatory activities of the purified phenolics were investigated in-vitro through measuring of NFκB, PGE, IL-6, IL-1β and TNF-α levels in human peripheral blood mononuclear cells (PBMC) stimulated with phytohaemagglutinin (PHA).

RESULTS

Phytochemical investigation of the flowering aerial parts of Z. simplex resulted in isolation of five major metabolites identified as isorhamnetin-3-O-β-D-rutinoside (1), myricitrin (2), luteolin-7- O-β-D-glucoside (3), isorhamnetin-3-O-β-D-glucoside(4), and isorhamnetin (5). It is noteworthy to report that compounds 1-3 were isolated from the plant for the first time. It was reported that NFκB represents an important linkage between oxidative stress and inflammation. Compounds 2 and 3 have exhibited the highest antioxidant activity and showed the most efficient in decreasing NFκB p65 at the lowest concentration (1µM). Moreover; at 1µM concentrations, only compounds 2 and 3 significantly decreased IL-6, IL-1β and TNF-α levels from PHA treatment. Nevertheless, at 100µM, all isolated metabolites significantly decreased IL-6 compared to PHA treatment.

CONCLUSION

Five major phenolic compounds were isolated from Z. simplex. Anti-inflammatory activity exhibited by the isolated compounds augment the traditional use of this plant as anti-inflammatory. The effect was mediated via inhibition of NFκB through antioxidant mechanism and subsequent inhibition to other inflammatory mediators like TNF-α, IL-1β and IL-6.

摘要

民族药理学相关性

单叶骆驼蓬是一种隶属于蒺藜科的盐生植物。该植物生长于干旱和半干旱地区。在阿拉伯地区,它传统上被用于治疗痛风、哮喘和炎症。

研究目的

尽管已有报道称该植物具有抗炎活性,但本研究旨在分离并鉴定单叶骆驼蓬的主要成分,并评估其体外抗氧化和抗炎活性。在本研究中,对分离出的化合物的抗炎活性机制进行了评估。

材料与方法

单叶骆驼蓬地上部分总甲醇提取物的脱脂部分在Diaion HP - 20、聚酰胺和反相柱上反复进行色谱分离,得到五种主要的酚类化合物。通过核磁共振实验并与先前已知的类似物进行比较,确定了纯化化合物的结构。此外,通过测量用植物血凝素(PHA)刺激的人外周血单核细胞(PBMC)中NFκB、PGE、IL - 6、IL - 1β和TNF - α的水平,体外研究了纯化酚类化合物的抗氧化和抗炎活性。

结果

对单叶骆驼蓬开花地上部分进行植物化学研究,分离出五种主要代谢产物,分别鉴定为异鼠李素 - 3 - O - β - D - 芸香糖苷(1)、杨梅素(2)、木犀草素 - 7 - O - β - D - 葡萄糖苷(3)、异鼠李素 - 3 - O - β - D - 葡萄糖苷(4)和异鼠李素(5)。值得注意的是,化合物1 - 3是首次从该植物中分离得到。据报道,NFκB是氧化应激和炎症之间的重要联系。化合物2和3表现出最高的抗氧化活性,并且在最低浓度(1µM)时最有效地降低了NFκB p65。此外,在1µM浓度下,只有化合物2和3显著降低了PHA处理后的IL - 6、IL - 1β和TNF - α水平。然而,在100µM时,与PHA处理相比,所有分离出的代谢产物均显著降低了IL - 6水平。

结论

从单叶骆驼蓬中分离出五种主要的酚类化合物。分离出的化合物所表现出的抗炎活性增强了该植物作为抗炎药的传统用途。其作用是通过抗氧化机制抑制NFκB,随后抑制其他炎症介质如TNF - α、IL - 1β和IL - 6来介导的。

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