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[摘要]
目的 研究泽漆石油醚、醋酸乙酯部位的化学成分及其抗肿瘤转移活性。方法 泽漆全草采用50%丙酮提取、系统溶剂萃取,综合运用硅胶柱色谱、凝胶柱色谱、HPLC制备色谱等方法分离纯化泽漆石油醚、醋酸乙酯部位的化学成分;采用根据理化性质和波谱分析方法鉴定其结构;通过MTT实验筛选出非细胞毒性的化学成分,进一步通过划痕实验来评价酚酸类化合物抗肿瘤转移的活性。结果 从泽漆石油醚、醋酸乙酯部位分离鉴定了8个化合物,分别鉴定为没食子酸(1)、咖啡酸(2)、间苯二酚(3)、连苯三酚(4)、没食子酸甲酯(5)、没食子酸乙酯(6)、杨梅素(7)、槲皮素(8)。抗肿瘤转移活性筛选结果表明,化合物1、5、6均能剂量相关性地提高抗肿瘤转移活性,其IC50分别为0.475、4.568、4.612 μmol/L。结论 化合物1、5、6显示出较好的抗肿瘤细胞转移活性,其中化合物1的作用最为显著。
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[Abstract]
Objective To study the chemical constituents in petroleum ether and ethyl acetate extracting fraction from Euphorbia helioscopia. and their antitumor metastatic activities. Methods E. helioscopia was extracted with 50% acetone and systematic solvent. The chemical constituents were isolated by chromatography on silica gel column, ODS column, and preparative HPLC; their structures were identified by physicochemical constants and spectroscopic methods. The non-cytotoxic concentration of compounds was tested by MTT assay. Wound healing assay was used to evaluate the antitumor metastatic activity of phenolic acids. Results Eight compounds were isolated from the petroleum ether and ethyl acetate extracting fraction of E. helioscopia and their structures were identified as gallic acid (1), caffeic acid (2), resorcinol (3), pyrogallol (4), methyl gallate (5), ethyl gallate (6), myrecetin (7), and quercetin (8). The antitumor metastatic activity screening results showed that compound 1, 5, 6 could increase the antitumor metastatic activity in a dose-dependent manner, and their IC50 values were 0.475, 4.568, and 4.612 μmol/L. Conclusion Compound 1, 5, and 6 show better antitumor metastatic activity. Compound 1 exhibits the most significant antitumor metastatic activity.
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