摘要
设计合成含精氨酸-精氨酸-亮氨酸(RRL)序列的多肽,并用氯胺-T法对其进行131I标记,标记率约60%,放化纯度>99%。体外放置24 h放化纯度仍≥90%。肿瘤对131I标记多肽的摄取在注射后明显高于其他器官,注药后24 h,肿瘤对131I-多肽的摄取约为0.65%ID/g,肿瘤与肌肉的放射性摄取比(T/NT)达9.08。以上结果表明:通过氯胺-T法对该多肽进行131I标记是可行的,标记物可在体外稳定存放24 h;131I-多肽可以靶向肿瘤血管,有进一步研究的价值。
A radioiodinated peptide of arginine-arginine-leucine（RRL） for tumor angiogenic endothelium imaging was designed and synthesized. Radioiodination of the RRL peptides was performed by the chloramine-T method. ^131I labeled peptides was injected into the nude mice bearing human prostate carcinoma via tail vein. Biodistribution results in vivo was obtained. HPLC of the crude product yielded a main peak containing 99.56% of the absorbance at 220 nm. The ^131I labeling rate of RRL peptides was about 60 %. The radiochemical purity was more than 99%. The radiochemical purity of the labeled compound remained 90% at 24 h in human blood serum at 37 ~C. In the biodistribution studies, the ^131I labeled RRL peptide accumulated in the tumor to a higher level than in the other organs, the uptake was about 0. 65% ID/g, and the radiouptake ratio of tumor to non-tumor （T/NT） was 9.08.
出处
《同位素》
CAS
2009年第2期96-100,共5页
Journal of Isotopes
基金
国家自然科学基金资助项目(30870729
30670583
30470498)
国家重点基础研究发展计划基金-973计划资助项目(2006CB705705)
北京大学985Ⅱ期基金资助项目(985-2-056)
