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Isolation and characterisation of pharmaceutically versatile molecules from <i>Rumex dentatus</i> and evaluation of their cytotoxic activity against human cancer cell lines

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DataCite Commons2023-02-17 更新2024-08-18 收录
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The disclosed study reveals isolation, characterization and anticancer evaluation of <i>Rumex dentatus</i>. The extracts and isolated compounds were used for cytotoxic activity against (lung (A549), pancreatic (MIAPaCa), colon (HCT-116), breast (MDA-MB-231) and breast (MDA-MB-468) cell lines. The extracts were screened for cytotoxicity using MTT colorimetric assay. Out of all extracts, methanolic (30) %: chloroform fraction (TAW6) with 75.01% inhibition at a concentration 100 µg/mL was observed. The selected extracts were further processed for column chromatography and led to isolation of seven compounds (A to G). The structural determination of isolated compounds was carried out using <sup>1</sup>HNMR, <sup>13</sup>CNMR, IR and HRMS. All the isolates were tested for cytotoxic activity and compound B was found most active with IC<sub>50</sub> values 11.29 µg against HCT-116 (Colon). The compound B was then used for detailed study via <i>transwell invasion assay</i> and <i>wound healing assay</i>. Thus the significant anticancer activity particularly against colon cancerous cell lines recommends that the (<i>Rumex dentatus)</i> could act as a potential drug candidate for cancer, more particularly for colon cancer.

本公开研究报道了齿果酸模(Rumex dentatus)的提取、分离鉴定与抗癌活性评价。所获提取物及分离得到的单体化合物,均用于针对肺(A549)、胰腺(MIAPaCa)、结肠(HCT-116)、乳腺(MDA-MB-231)及乳腺(MDA-MB-468)细胞系的细胞毒性活性检测。提取物的细胞毒性筛选采用MTT比色法完成。在所测试的全部提取物中,浓度为100 μg/mL的30%甲醇-氯仿馏分(TAW6)的细胞抑制率可达75.01%。选取活性优异的提取物进一步通过柱层析分离,最终得到7个单体化合物(编号A至G)。分离得到的单体化合物的结构鉴定通过氢谱(¹HNMR)、碳谱(¹³CNMR)、红外光谱(IR)及高分辨质谱(HRMS)完成。所有单体化合物均进行了细胞毒性活性测试,其中化合物B活性最强,针对结肠癌细胞系HCT-116的半数抑制浓度(IC₅₀)为11.29 μg。随后选取化合物B开展深入研究,采用Transwell侵袭实验(transwell invasion assay)与划痕愈合实验(wound healing assay)进行验证。综上,齿果酸模展现出显著的抗癌活性,尤其是针对结肠癌细胞系,表明其可作为抗肿瘤药物的潜在候选来源,在结肠癌治疗领域具备进一步开发价值。

提供机构:
Taylor & Francis
创建时间:
2022-06-24
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