孙梅贞,杨照华,倪震黎,陈桂宝,刘实晶,陈红红,罗梅初.双分子取代苯酚氨羧酸螯合剂对放射性钍促排活性的构效关系[J].中华放射医学与防护杂志,1999,19(3):183-185
双分子取代苯酚氨羧酸螯合剂对放射性钍促排活性的构效关系
Structure activity relationship study of chelating agents of double molecular substituted phenols amino carboxylic acid for decorporated radiothorium
投稿时间:1998-04-19  修订日期:1998-07-21
DOI:
中文关键词:  螯合剂  234Th  促排活性
英文关键词:Chelating agent  Thorium-234  Decorporated bioactivity
基金项目:国家自然科学基金
作者单位
孙梅贞 200032 上海医科大学放射医学研究所 
杨照华 200032 上海医科大学放射医学研究所 
倪震黎 200032 上海医科大学放射医学研究所 
陈桂宝 200032 上海医科大学放射医学研究所 
刘实晶 200032 上海医科大学放射医学研究所 
陈红红 200032 上海医科大学放射医学研究所 
罗梅初 200032 上海医科大学放射医学研究所 
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中文摘要:
      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。
英文摘要:
      Objective To study the effects of synthesized chelating agents of double molecular substituted phenols amino carboxylic acid on decorporated radiothorium in rats and to explore the relationship between their chemical structure and bioactivity. Methods Chelating agents could increase the excretion of 234 Th in urine and feces and decrease its retention in liver and skeleton of rats as compared with the control group. Results The chelating agents showed different bioactivity for decorporated thorium except 4 agents.Three of them could increase excretion of 234 Th in urine and feces by 60-70% and decrease markedly retention of 234 Th in liver and skeleton. Conclusion Chelating agents of the catechol series have been proved to be superior to others.They are the best ones while the resorcinol is the worst and hydroquinone is ranked between them.
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