双分子取代苯酚类螯合剂的合成及对放射性钍的促排效果研究

Synthesis of bimolecule substituted phenols and their effect on rats for removal of radiothorium.

目的本文旨在寻找新的治疗用螯合剂，以加速排除沉积在体内的放射性钍，达到放射防护的目的。方法首先通过Ｍａｎｎｉｃｈ反应合成双分子取代苯酚类螯合剂，然后经动物实验：ＳＤ大鼠静脉中毒２３４Ｔｈ后立即肌注药物，２天后解剖动物测定２３４Ｔｈ量，计算排出量和蓄积量，研究其促排效果。结果所报道的螯合剂不仅能增加大鼠在尿、粪中２３４Ｔｈ的排除，同时能降低在肝、骨中的蓄积，呈现较好的促排效果。其中以化合物Ⅷ促排效果最好，２天后可排除６８％的２３４Ｔｈ；在肝、骨中的沉积仅为１１．７％，而对照组则是８７．６％。结论螯合剂Ⅷ值得进一步研究探讨。

Objectives\ To search for new therapeutic chelating agents for removal of incorporated radiothorium. Methods\ New chelating agents (bimolecule-substituted phenols) were synthesized through Mannich reaction.These compounds were administered i.m.to SD rats after i.v.injection of 234 Th .Two days later the radiothorium was assayed and the excretion and retention rates were calculated.Results\ These chelating agents could increase the excretion of 234 Th in urine and feces and decrease its retention in liver and skeleton of rats.Among them No.Ⅷ is the best one,which could promote excretion of 68%. 234 Th after two days and the retention of 234 Th deposited in the tissues (liver and skeleton) was only 11.7%,as compared with 87.6% in the control group. Conclusions\ The chelating agent No.Ⅷ is worth further investigation.