Abstract The golden thistle, Scolymus hispanicus L. (Asteraceae), is a prickly perennial herb that is widely grown in Mediterranean and in Southeastern Europe. The aim of current study was to isolate and identify the constituents of S. hispanicus L. chloroform fraction, and assess their anti-inflammatory activity in-vitro. Chemical investigation led to isolation of one new guaianolide sesquiterpene; namely iso-japonicolactone (4), three tritepenes namely lupeol acetate (1), lupeol (2), and oleanolic acid (5), and the sterol stigmasterol (3). The isolated compounds demonstrated free radical scavenging activity against DPPH with compound 4 being able to scavenge more than 90% of DPPH radical at 100 µM. Treatment of the peripheral blood mononuclear cells (PBMC) stimulated with phytohaemagglutinin (PHA) with the isolated compounds resulted in a decrease in nuclear factor kappa (NFκB) p65 content in a dose-dependent manner. Compound 4 was the most efficient in decreasing NFκB p65 at the lowest concentration (1 µM), followed by compound 5. In addition, cell treatment with isolated compounds resulted in dose-related reduction of interleukins (IL-6 and IL-1β), and tumor necrosis factor (TNF-α). To the best of our knowledge this is the first report for the isolation of iso-japonicolactone and the detailed study of its anti-inflammatory activity. The potent anti-inflammatory compounds in this study could be considered as a nucleus for developing anti-inflammatory drugs through further biological studies on the molecular level.

中文翻译：

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Scolymus hispanicus L 亲脂性代谢物的抗炎活性

摘要 金蓟，Scolymus hispanicus L.（菊科）是一种多年生带刺草本植物，广泛生长于地中海和东南欧。当前研究的目的是分离和鉴定 S. hispanicus L. 氯仿组分的成分，并评估它们的体外抗炎活性。化学研究导致分离出一种新的愈创木内酯倍半萜；即异-japonicolactone (4)，三种三萜烯，即羽扇豆醇乙酸酯 (1)、羽扇豆醇 (2) 和齐墩果酸 (5)，以及甾醇豆甾醇 (3)。分离的化合物显示出对 DPPH 的自由基清除活性，化合物 4 能够在 100 µM 下清除 90% 以上的 DPPH 自由基。用分离的化合物处理用植物血凝素 (PHA) 刺激的外周血单核细胞 (PBMC) 导致核因子 kappa (NFκB) p65 含量以剂量依赖性方式减少。化合物 4 在最低浓度 (1 µM) 下最有效地降低 NFκB p65，其次是化合物 5。 此外，用分离的化合物处理细胞导致白细胞介素（IL-6 和 IL-1β）的剂量相关减少，和肿瘤坏死因子（TNF-α）。据我们所知，这是分离异粳内酯及其抗炎活性的详细研究的第一份报告。本研究中的强效抗炎化合物可以被视为通过分子水平的进一步生物学研究开发抗炎药物的核心。