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细胞膜P-糖蛋白(P-gp)介导的药物外流是肿瘤多药耐药(MDR)产生的重要机制,异黄酮类化合物可以通过抑制P-gp活性发挥MDR逆转作用.通过对P-gp抑制剂进行结构分析,以金雀异黄素为母体,在其7位、8位及4’位分别引进碱性边链,设计、合成了20个金雀异黄素衍生物(其中16个未见文献报道),并检测了其多药耐药逆转活性.结果表明,大多数目标化合物对人白血病耐药细胞株K562/A02具有不同程度的耐药逆转作用.其中目标化合物8a,8b,8d,8e逆转作用较强,逆转倍数分别为8.97,6.36,5.19和5.82.
P-glycoprotein (P-gp) -mediated drug efflux is an important mechanism of tumor multidrug resistance (MDR), isoflavones can play a role in reversing MDR by inhibiting the activity of P-gp.Through P-gp Inhibitors were structurally analyzed. Genistein was introduced into genistein at the 7th, 8th and the 4th respectively, and 20 genistein derivatives were designed and synthesized (16 of them Not reported in the literature), and tested its multidrug resistance reversal activity.The results show that most of the target compounds on human leukemia cell line K562 / A02 with varying degrees of reversal of drug resistance in which the target compounds 8a, 8b, 8d, 8e strong reversal, reversal fold were 8.97,6.36,5.19 and 5.82.