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心叶球花对结肠癌细胞的影响:抗氧化活性、炎性细胞因子分析及分子对接研究

Effects of Globularia cordifolia on colon cancer cells: antioxidant activity, inflammatory cytokine analysis and molecular docking studies.

作者信息

Torunoglu Emine Incilay, Aytar Erdi Can, Aydın Betul, Durmaz Alper, Balpınar Özge, Ertuğrul Muhammed Sait, Yarım Gül Fatma

机构信息

Faculty of Medicine, Department of Medical Biochemistry, Necmettin Erbakan University, Konya, Turkey.

Faculty of Agriculture Department of Horticulture, Usak University, Uşak, Turkey.

出版信息

J Sci Food Agric. 2025 Apr;105(6):3382-3396. doi: 10.1002/jsfa.14100. Epub 2024 Dec 27.

Abstract

BACKGROUND

The present study aimed to comprehensively evaluate the anticancer, anti-inflammatory, and antioxidant properties of Globularia cordifolia L.

SAMPLES

The plant material was collected and extracted using the maceration method. Antioxidant activities were assessed through DPPH (i.e. 2,2-diphenyl-1-picrylhydrazyl) and iron chelation assays, whereas phenolic and flavonoid contents were measured using spectrophotometric methods. Gas chromatography-mass spectrometry analysis was performed to identify biologically active compounds. The cytotoxic effect on colon cancer cells was evaluated using MTT [i.e. 2,3-bis-(2-methoxy-4-nitro-5-sulfophenyl)-2H-tetrazolium-5-carboxanilide] assays, and inflammatory cytokine levels were measured through an enzyme-linked immunosorbent assay. Molecular docking studies investigated the interactions of bioactive compounds with the 4UYA protein, and ADME (i.e. absorption, distribution, metabolism, excretion and toxicity) modeling predicted their toxicity.

RESULTS

The study revealed that the extract exhibited strong antioxidant activity with a median 50% inhibitory concentration (IC) value of 39.48 ± 2.15 μg mL in the DPPH assay and an effective iron chelation capacity with an IC value of 4.28 ± 0.19 mg mL. The total phenolic content was 662.51 ± 20.95 mg gallic acid equivalents g, and the flavonoid content was 114.99 ± 0.51 mg quercetin equivalents g, demonstrating the extract's richness in phenolic and flavonoid compounds. Significant antiproliferative effects were observed in colon cancer cells at a dose of 250 μg mL. Inflammatory cytokine analysis indicated a reduction in pro-inflammatory responses. Molecular docking studies showed strong binding affinities between the bioactive compounds and the 4UYA protein, suggesting the mechanisms of action.

CONCLUSION

The findings indicate that G. cordifolia extract exhibits strong antioxidant, anti-inflammatory and antiproliferative properties, making it a promising biomolecular agent for colon cancer therapy. The high phenolic and flavonoid contents, combined with the bioactive compounds' interactions with key molecular targets, underscore its potential therapeutic applications. © 2024 Society of Chemical Industry.

摘要

背景

本研究旨在全面评估心叶球花的抗癌、抗炎和抗氧化特性。

样本

采集植物材料并采用浸渍法进行提取。通过DPPH(即2,2-二苯基-1-苦基肼)和铁螯合试验评估抗氧化活性,而酚类和黄酮类含量则采用分光光度法进行测定。进行气相色谱-质谱分析以鉴定生物活性化合物。使用MTT[即2,3-双-(2-甲氧基-4-硝基-5-磺基苯基)-2H-四唑-5-甲酰苯胺]试验评估对结肠癌细胞的细胞毒性作用,并通过酶联免疫吸附测定法测量炎性细胞因子水平。分子对接研究调查了生物活性化合物与4UYA蛋白的相互作用,ADME(即吸收、分布、代谢、排泄和毒性)模型预测了它们的毒性。

结果

研究表明,提取物在DPPH试验中表现出较强的抗氧化活性,半数抑制浓度(IC)中值为39.48±2.15μg/mL,并且具有有效的铁螯合能力,IC值为4.28±0.19mg/mL。总酚含量为662.51±20.95mg没食子酸当量/g,黄酮类含量为114.99±0.51mg槲皮素当量/g,表明提取物富含酚类和黄酮类化合物。在250μg/mL的剂量下,观察到对结肠癌细胞有显著的抗增殖作用。炎性细胞因子分析表明促炎反应有所降低。分子对接研究显示生物活性化合物与4UYA蛋白之间具有很强的结合亲和力,提示了其作用机制。

结论

研究结果表明,心叶球花提取物具有较强的抗氧化、抗炎和抗增殖特性,使其成为结肠癌治疗中一种有前景的生物分子药物。高酚类和黄酮类含量,以及生物活性化合物与关键分子靶点的相互作用,突出了其潜在的治疗应用价值。©2024化学工业协会。

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