【摘要】 目的以常用血液肿瘤细胞株为研究对象,体外加入紫草素(代号SK01)、β-羟基-异戊酰紫草素(代号SK17)及其16种人工半合成的紫草素衍生物,研究对血液肿瘤细胞株的增殖抑制作用,从中筛选出低毒高效的紫草素类化合物。方法 CCK-8法检测紫草素及其衍生物对血液肿瘤细胞株的增殖抑制作用即药物半数抑制浓度。结果紫草素-二甲醚衍生物(代号SK36)对多种血液肿瘤细胞株均有很强的细胞毒作用,但对正常细胞株的毒性作用则明显低于SK01和SK17,表现出较好选择性。实验中我们还发现大部分母核Ⅰ紫草素衍生物药物活性强于相对应的母核Ⅱ衍生物。结论 SK36能有效抑制多种血液肿瘤细胞株增殖,而对正常细胞株毒性较小,有较强的选择性,值得进一步开展基础及临床研究。更多还原

【Abstract】 Objective To acquire compounds with low toxicity and high antitumo r activity,We detected the inhibitory effects of shikonin,β-hydroxyisovaleryl shikonin and sixteen kinds of artificial semi-synthetic shikonin derivatives on hematological malignant cell lines proliferation in vitro.Methods The inhibitory effects of cell proliferation were evaluated by CCK-8 assay.Results dimethyl eth er shikonin derivatives(SK36) can inhibit cell proliferation of hematological m alignant cell lines,and displayed the no toxicity to normal cells than SK01 an d SK17,thereby the selectivity appeared between cancer cells and normal cell.A dditionally,The compounds with mother nucleus I were found to be more effecti ve to cancer cells than that of ones possessing nucleus Ⅱ.Conclusion SK36 can inhibit cell proliferation of hematological malignant cell lines,more important ly,it has low toxicity effect to normal cell line.It is worth for further basi c and clinical research.更多还原