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目的对已合成的15个双分子取代苯酚氨羧酸螯合剂经动物实验观察对234Th的促排活性,以探讨化学结构与促排活性的构效关系。方法以大鼠尿、粪中234Th排出量的增高,组织(肝、骨)中蓄积量的降低与对照组比较作为评价指标。结果15个螯合剂中除4个外均显示不同程度的促排活性,其中有3个其尿、粪中234Th的排出量达60%~70%,肝、骨中234Th的蓄积量明显降低。结论取代基中邻苯二酚类的促排活性为最好,为本实验之冠,间苯二酚的活性最差,对苯二酚居中。
OBJECTIVE To investigate the chemosensitivity of 234Th to 15 bi-substituted phenol-amino-carboxylic acid chelators synthesized by animal experiments to explore the structure-activity relationship between chemical structure and promoting activity. Methods The excretion of 234Th in urine and feces of rats was increased, and the decrease of the accumulation in tissues (liver and bone) compared with the control group was taken as the evaluation index. Results Except four of the 15 chelators, all showed excretion activity to varying degrees. Among them, 3 of them showed urinary excretion of 234Th in excrement and 60% ~ 70% of 234Th in excrement, while 234Th in liver and bone decreased significantly. CONCLUSION The catechols in the substituents have the best promoting activity. For the purpose of this experiment, the resorcinol activity is the worst and the hydroquinone is the center.