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

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

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，183 W 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．

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-HIV activities and toxicities of these compounds have been determined in human T lymph 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 2 988 mg/kg and the maximum tolerance dose is 800 mg/kg, which is 2 000 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.