高等学校化学学报 ›› 2002, Vol. 23 ›› Issue (5): 777.

• 研究论文 • 上一篇    下一篇

新型稀土杂多蓝的合成及其抗艾滋病病毒(HIV-1)活性和毒性研究

刘术侠1, 李阳先1, 韩正波1, 王恩波1, 曾毅2, 李泽淋2   

  1. 1. 东北师范大学化学学院, 长春 130024;
    2. 中国预防医学科学院, 北京 100050
  • 收稿日期:2000-09-18 出版日期:2002-05-24 发布日期:2002-05-24
  • 通讯作者: 王恩波(1938年出生),男,教授,博士生导师,从事杂多酸化学的结构与性能研究.
  • 基金资助:

    国家科技部重大课题(批准号:96-901-01-3OA)资助.

Synthesis, Anti-HIV-1 Activity and Toxicity of New Rare Earth-containing Heteropoly Blues

LIU Shu-Xia1, LI Yang-Guang1, HAN Zheng-Bo1, WANG En-Bo1, ZENG Yi2, LI Ze-Lin2   

  1. 1. Faculty of Chemistry, Northeast Normal University, Changchun 130024, China;
    2. Chinese Academy of Preventive Medicine Science, Beijing 100050, China
  • Received:2000-09-18 Online:2002-05-24 Published:2002-05-24

摘要: 合成了Keggin结构钨硅、钨锗、钨磷、钨砷两电子及四电子稀土钐盐杂多蓝,铈量滴定及元素分析方法确定了化合物的还原电子数及化学组成,采用IR,UV-Vis,183W NMR和ESR等对其结构进行了表征.在人T淋巴细胞MT-4内,对合成的化合物进行了系统的抗艾滋病毒(HIV-1)活性及毒性测定.发现Keggin结构钨硅、钨锗四电子稀土钐盐杂多蓝具有较强的抗HIV-1活性,其中钨锗酸钐四电子杂多蓝(代号HPBR-2)具有较高的治疗指数.

关键词: 稀土杂多蓝, 合成, 抗HIV活性, 毒性

Abstract: Two- and four- electron heteropoly blues of samarium-containing polyoxotungstosilicate, poly-oxotungstogermanate, polyoxotungstophosphate and polyoxotungstoarsenate with Keggin structure have been 'synthesized, stoichiometrily determined by elemental analyses and cerimetric titration, and characterized by IR, UV-Vis, 183W NMR and ESR spectra.The anti-HIVactivities and toxicities of these compounds have been determined in human Tlymph cells MT-4.It has been found that the four-electron heteropoly blue of samarium-containing polyoxotungstogermanate (HPBR-2) has a high therapeusis index.Medicine tolerance test shows that the cells have no obvious resistance to HPBR-2.The half-inhibition concentrations IC50 of HPBR-2 to acutely infected MT-4 cells have no distinct difference between generation 0 and generation 9.The acute toxicity and Ames test of HPBR-2 have also been carried out.HPBR-2 can not mutate the bacterium typhosum.The half toxicity dose LD50 of HPBR-2 orally administrated to mice is 2988 mg/kg and the maximum tolerance dose is 800 mg/kg, which is 2000 times as high as the dose orally administrated to the human being(20 mg/50 kg).HPBR-2 belongs to one of the complexes with high safety factors.

Key words: Rare earth-containing heteropoly blues, Synthesis, Anti-HIV activity, Toxicity

中图分类号: 

TrendMD: