~(211)At,~(131)I标记蛋白质的合成
SYNTHESIS OF ~(211)At AND ~(131)I LABELLED PROTEINS
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摘要: 本文报道间接法标记蛋白质:首先用放射性核素标记一种有机化合物,然后将此种化合物偶联到蛋白质上。α核素~(211)At同对氨基苯甲酸制备的重氮化合物反应,获得对-~(211)At-苯甲酸,然后经乙醚萃取和反相高效液体色谱分离,通过活化羧基反应偶联到IgG或牛血清白蛋白(BSA)上。Sephadex G-75用于从反应产物中分离标记蛋白质,相对法比较放射性计数测定标记产额。全程标记率不低于初始~(211)At放射性活度的40%。动物实验的结果表明,此种结合的标记蛋白质在体内条件下稳定。~(211)At在小鼠血液中的保留,在~(211)At-IgG处理的小鼠中比在Na~(211)At处理的小鼠中高得多,IgG-At键在体内应是稳定的。Abstract: This article presents an indirect method of labelling proteins. an organic compound is labelled by radionuclide and then the compound is conjugated to a protein. The α- particle emmiting nuclide ~(211)At was reacted with diazo-compound of para-aminobenzoic acid to obtain para-astato-benzoic acid. The labelled compound was separated by ether extraction and reversedphase high performance liquid chromatography, and then was conjugated with IgG or bovine serum albuminr(BSA) by an activating reaction of carboxy. Sephadex G-75 column was used to separate the labelled protein from reactive products and the labelling yield was determined by the relative method comparing radioactive counts. The conjugate contained at least 40% of the initial activity of ~(211)At. The results of the animal experiments showed that the conjugate was stable in vivo. The retention of ~(211)At in blood of mice was much greater in the ~(211) At-IgG treated mice than in the Na~(211)At treated mice, implying that the bond between the IgG and astatine was stable in vivo.