Department of Chemistry, Faculty of Art and Science, Celal Bayar University, Manisa, Turkey.
Cancer Biother Radiopharm. 2011 Oct;26(5):573-84. doi: 10.1089/cbr.2011.0998. Epub 2011 Sep 27.
The metabolic comparison of bleomycin (BLM) and bleomycin-glucuronide (BLMG) radiolabeled with (99m)Tc ((99m)Tc-BLM and (99m)Tc-BLMG, respectively) has been investigated in this study. Quality control procedures were carried out using thin-layer radiochromatography and high-performance liquid chromatography. To compare the metabolic behavior of BLM and its glucuronide conjugate radiolabeled with (99m)Tc, scintigraphic, and biodistributional techniques were applied using male New Zealand rabbits and Albino Wistar rats. The results obtained have shown that these compounds were successfully radiolabeled with a labeling yield of about 100%. Maximum uptakes of (99m)Tc-BLM and (99m)Tc-BLMG metabolized as N-glucuronide were observed within 2 hours in the liver, the bladder, and the spinal cord for (99m)Tc-BLM and the lung, the liver, the kidney, the large intestine, and the spinal cord for (99m)Tc-BLMG, respectively. Scintigraphy and biodistributional studies performed on the experimental animals have shown that radiopharmaceutical potentials of these compounds are completely different. At the same time, uptake of the (99m)Tc-BLMG was found to be better than that of (99m)Tc-BLM.
本研究对博来霉素（BLM）及其葡萄糖醛酸轭合物（BLMG）经（99m）Tc 标记物（分别为（99m）Tc-BLM 和（99m）Tc-BLMG）的代谢进行了比较。采用薄层层析放射色谱法和高效液相色谱法进行了质量控制程序。为了比较 BLM 及其与（99m）Tc 标记的葡萄糖醛酸轭合物的代谢行为，使用雄性新西兰兔和白化 Wistar 大鼠应用闪烁照相术和生物分布技术。结果表明，这些化合物成功地用约 100%的标记产率进行了放射性标记。（99m）Tc-BLM 和（99m）Tc-BLMG 的 N-葡萄糖醛酸轭合物在 2 小时内分别在肝脏、膀胱和脊髓中达到最大摄取，而（99m）Tc-BLMG 则在肺、肝脏、肾脏、大肠和脊髓中达到最大摄取。对实验动物进行的闪烁照相术和生物分布研究表明，这些化合物的放射性药物潜力完全不同。同时，（99m）Tc-BLMG 的摄取量优于（99m）Tc-BLM。
