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[摘要]
目的 研究澤漆石油醚、醋酸乙酯部位的化學(xué)成分及其抗腫瘤轉(zhuǎn)移活性。方法 澤漆全草采用50%丙酮提取、系統(tǒng)溶劑萃取,綜合運用硅膠柱色譜、凝膠柱色譜、HPLC制備色譜等方法分離純化澤漆石油醚、醋酸乙酯部位的化學(xué)成分;采用根據(jù)理化性質(zhì)和波譜分析方法鑒定其結(jié)構(gòu);通過MTT實驗篩選出非細(xì)胞毒性的化學(xué)成分,進(jìn)一步通過劃痕實驗來評價酚酸類化合物抗腫瘤轉(zhuǎn)移的活性。結(jié)果 從澤漆石油醚、醋酸乙酯部位分離鑒定了8個化合物,分別鑒定為沒食子酸(1)、咖啡酸(2)、間苯二酚(3)、連苯三酚(4)、沒食子酸甲酯(5)、沒食子酸乙酯(6)、楊梅素(7)、槲皮素(8)??鼓[瘤轉(zhuǎn)移活性篩選結(jié)果表明,化合物1、5、6均能劑量相關(guān)性地提高抗腫瘤轉(zhuǎn)移活性,其IC50分別為0.475、4.568、4.612 μmol/L。結(jié)論 化合物1、5、6顯示出較好的抗腫瘤細(xì)胞轉(zhuǎn)移活性,其中化合物1的作用最為顯著。
[Key word]
[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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