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目的对18β-甘草次酸2位、3位、11位和29位进行结构修饰,增强其抑制白血病细胞生长和诱导细胞凋亡活性。方法以18β-甘草次酸为起始原料,经氧化、酯化、缩合、脱氢等反应得到目标化合物;以台盼蓝排斥试验和AO-EB双荧光染色法检测目标化合物对HL-60细胞的生长抑制活性及诱导细胞凋亡活性。结果与结论合成了14个18β-甘草次酸类化合物,其结构经核磁共振氢谱、红外光谱及质谱确证。体外活性测定结果表明,合成的化合物表现出不同程度的细胞生长抑制活性,其中A环结构改造后的化合物Ⅶ和Ⅸ活性较强,且呈现时间和剂量依赖性。
OBJECTIVE: To modify the structure of 2β, 3, 11 and 29 of 18β-glycyrrhetinic acid and enhance the activity of leukemia cell growth and induce apoptosis. Methods The target compounds were obtained by reaction of 18β-glycyrrhetinic acid with oxidation, esterification, condensation and dehydrogenation. The target compounds were detected by trypan blue exclusion test and AO-EB double fluorescence staining. Growth inhibitory activity and induce apoptosis activity. RESULTS AND CONCLUSIONS A total of 14 18β-glycyrrhetinic acid compounds were synthesized and their structures were confirmed by 1H-NMR, FT-IR and MS. The results of in vitro activity assay showed that the synthesized compounds showed different degree of cell growth inhibitory activity, and the compounds A and VII with structural modification of A ring were more active and in a time-and dose-dependent manner.