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~(125)I-interleukin-8 radiolabelling and in vivo distribution

机译:〜(125)I-白介素8放射性标记和体内分布

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To study the radioiodinating condition of interleukin-8(IL-8) and observe its biodistribution in mice for understanding the possibility of its application in nuclear medicine, we labelled IL-8 with ~(125)I using Bolton-Hunter reagent, and the distributions in mice at 5 min, 30 min, 1h, 6h and 24h after injection of ~(125)I -IL-8 were measured. The blood clearance curve was obtained and fitted with the two-compartment model. The results showed that ~(125)I-IL-8 was obtained with a labeling efficiency of 12.2% +- 6.5% and a radiochemical purity of 91.4% +- 6.5%. Its specific activity was 14.8 kBq/μg IL-8. A fast phase half - life T_(1/2α) of 0.32 h and a slow phase half - life T_(1/2β) of 8.01 h were calculated from the blood clearance curve. The uptakes of radioactivities in kidneys and lung had the peaks of 85.87%ID/g and 16.17%ID/g at 30 min after intravenous injection, respectively. The uptakes in liver and spleen were 12.05%ID/g and 8.97%ID/g as the maximum at 5 min after injection. The clearance in blood and other organs was fast. Except for kidneys and lung, ~(125)I -IL-8 was less than 1%ID/g 24 h after administration. It is concluded that radioiodinated IL-8 is a promising radiopharmaceutical in nuclear medicine, especially for imaging infection. But to enhance the labeling efficiency of radioiodinated IL-8 and to decrease its in vivo deiodination are the subjects necessary to be further investigated.
机译:为了研究白介素8(IL-8)的放射性碘条件,并观察其在小鼠中的生物分布,以了解其在核医学中的应用可能性,我们使用Bolton-Hunter试剂将〜(125)I标记为IL-8,测量了〜(125)I -IL-8注射后5分钟,30分钟,1小时,6小时和24小时在小鼠中的分布。获得血液清除曲线,并与两室模型拟合。结果显示获得〜(125)I-IL-8,其标记效率为12.2%±6.5%,放射化学纯度为91.4%±6.5%。其比活性为14.8 kBq /μgIL-8。从血液清除率曲线计算出快相半衰期T_(1 /2α)为0.32 h,慢相半衰期T_(1 /2β)为8.01 h。静脉注射后30分钟,肾脏和肺部放射性的吸收峰​​值分别为85.87%ID / g和16.17%ID / g。注射后5分钟,肝脏和脾脏的摄取最大为12.05%ID / g和8.97%ID / g。血液和其他器官的清除速度很快。除肾和肺外,给药后24小时〜(125)I -IL-8小于1%ID / g。结论是,放射性碘化的IL-8在核医学中,特别是对于影像感染,是一种有前途的放射性药物。但是,为了提高放射性碘标记的IL-8的标记效率并降低其体内的脱碘作用,有待进一步研究。

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