The present study was aimed at investigation of the chemical composition, antioxidant and cytotoxic activities of topinambur Helianthus tuberosus L. extracts for its further application in medicine. Crude methanol extract from the tubers of H. tuberosus L. cultivated in Tajikistan, was analyzed by liquid chromatography–mass spectrometry (LC-MS/MS) method. Chlorogenic and 1,5-dicaffeoylquinic acids were identified as major components of the tuber methanol extract by NMR and peak matching in LC-MS/MS chromatogram with defined standards. Total phenolic and flavonoid contents of the methanol and aqueous extracts were determined using Folin – Ciocalteu and aluminum colorimetric methods, respectively. The methanol extract showed substantial phenolic and flavonoid contents in comparison to the aqueous extract. Total phenolic and flavonoid contents of 67.12 ± 1.2 mg caffeic acid equivalent and 3.53 ± 0.1 mg quercetin equivalent per gram of the methanol extract were determined. Their antioxidant capacity was evaluated using DPPH, ABTS, and FRAP assays. Half –inhibitory (IC50) values of the methanol extract were 13.61 ± 0.1 μg/mL for DPPH and 30.23 ± 0.4 μg/mL for ABTS test, respectively. The FRAP value of the methanol extract and positive control were 850.24 ± 14 and 2380 ± 46 mM FeSO4/mg extract, respectively. The aqueous extract exhibited low antioxidant activity. In addition, cytotoxicity of the methanol extracts was evaluated using MTT assay on CCRF-CEM and P-gp overexpressing CEM/ADR5000 cancer cell lines. The methanol extract showed a rather weak activity with IC50 values 265.0 μg/mL for CCRF-CEM and 345.9 μg/mL for CEM/ADR5000. As CEM/ADR5000 cells overexpress the ABC transporter P-gp, this result indicated that the extract apparently contained substances which affect P-gp, which need further investigations. In conclusion, methanol extract of H. tuberosus is rich with chlorogenic and 1,5-dicaffeoylquinic acid and exhibits strong antioxidant activity and weak cytotoxicity.

中文翻译：

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Topinambur (Helianthus tuberosus L.) 的绿原和富含 1,5-二咖啡酰奎宁酸的提取物表现出强抗氧化活性和弱细胞毒性

本研究旨在研究向日葵提取物的化学成分、抗氧化和细胞毒活性，以促进其在医学上的进一步应用。通过液相色谱-质谱 (LC-MS/MS) 方法分析塔吉克斯坦种植的马铃薯块茎的粗甲醇提取物。通过 NMR 和 LC-MS/MS 色谱图中的峰匹配，将绿原酸和 1,5-二咖啡酰奎宁酸确定为块茎甲醇提取物的主要成分，并与定义的标准品进行匹配。分别使用 Folin-Ciocalteu 和铝比色法测定甲醇和水提取物的总酚类和类黄酮含量。与水提取物相比，甲醇提取物显示出大量的酚类和类黄酮含量。总酚类和类黄酮含量为 67。每克甲醇提取物测定了 12 ± 1.2 mg 咖啡酸当量和 3.53 ± 0.1 mg 槲皮素当量。使用 DPPH、ABTS 和 FRAP 测定法评估它们的抗氧化能力。甲醇提取物的半抑制 (IC50) 值对于 DPPH 和 ABTS 测试分别为 13.61 ± 0.1 μg/mL 和 30.23 ± 0.4 μg/mL。甲醇提取物和阳性对照的 FRAP 值分别为 850.24 ± 14 和 2380 ± 46 mM FeSO4/mg 提取物。水提取物表现出低抗氧化活性。此外，甲醇提取物的细胞毒性使用 MTT 测定对 CCRF-CEM 和 P-gp 过表达 CEM/ADR5000 癌细胞系进行评估。甲醇提取物显示出相当弱的活性，CCRF-CEM 的 IC50 值为 265.0 μg/mL，CEM/ADR5000 的 IC50 值为 345.9 μg/mL。由于 CEM/ADR5000 细胞过度表达 ABC 转运蛋白 P-gp，该结果表明提取物明显含有影响P-gp的物质，需要进一步研究。综上所述，马铃薯甲醇提取物富含绿原酸和1,5-二咖啡酰奎宁酸，具有较强的抗氧化活性和较弱的细胞毒性。