中文摘要：

采用化学方法对18β-甘草次酸A环进行改造,合成了一系列新型18β-甘草次酸A环官能团化衍生物.对人白血病细胞株HL-60、K562、肝癌细胞BEL-7404及乳腺癌细胞MDA-MB-231的体外抗肿瘤活性筛选结果表明,化合物5对4种肿瘤细胞系的抑制活性均强于18β-甘草次酸;构效关系分析表明,A环内烯键的形成对抑制肿瘤细胞增殖有重要影响;同时利用Hoechst33258和AO/EB染色,在荧光显微镜下观察到了细胞凋亡小体的形成.

英文摘要：

Thirteen analogues of 18β-glycyrrhetinic acid were synthesized using various chemical methods and one of them exhibited certain cytotoxicity against cell-lines of HL60 cells,K562 cells,BEL-7404 cells and MDA-MB-231,respectively,via MTT method.The results show that compound 5 with C-C bond in the A-ring of 18β-glycyrrhetinic acid has markedly antiproliferative effect on these four tumor cells compared with 18β-glycyrrhetinic acid.K562 cells with nuclear apoptotic bodies were observed after staining with Hoechst 33258 and AO/EB with flourescence microscope.