肿瘤被定义为异常组织肿块,导致这些异常组织肿块生长的最重要因素之一是血管内皮生长因子,通过在缺氧条件下释放细胞来刺激血管生成。缺氧在癌症治疗中起着至关重要的作用,因此监测缺氧非常重要。缺氧标志物匹莫硝唑(PIM)是癌症侵袭性的候选生物标志物。
该研究旨在使用碘131(131I)对PIM进行放射性碘化,以加入治疗方法。为此,PIM被衍生为能够被放射性碘化的PIM-TOS。
PIM通过甲苯磺酸化反应得到。衍生化产物(PIM-TOS)采用碘原法进行放射性碘化,并采用高效液相色谱和液相色谱-质谱联用进行分析。薄层放射色谱法用于其质量控制研究。
在甲苯磺酸化反应后成功得到PIM。PIM-TOS的放射性碘化产率超过85%。
在目前的研究中,使用131I的PIM的放射性碘化电位,作为一种潜在的治疗性缺氧药物进行了研究。应进行进一步的实验研究以开发新型的缺氧探针,包括治疗方法。
Tumors are defined as abnormal tissue masses, and one of the most important factors leading to the growth of these abnormal tissue masses is Vascular Endothelial Growth Factor, which stimulates angiogenesis by releasing cells under hypoxic conditions. Hypoxia has a vital role in cancer therapy, thus it is important to monitor hypoxia. The hypoxia marker Pimonidazole (PIM) is a candidate biomarker of cancer aggressiveness.
The study aimed to perform radioiodination of PIM with Iodine-131 (131I) to join a theranostic approach. For this purpose, PIM was derived as PIM-TOS to be able to be radioiodinated.
PIM was derived via a
tosylation reaction. Derivatization product (PIM-TOS) was radioiodinated by using iodogen method and was analyzed by High-Performance Liquid Chromatography and Liquid chromatography-mass spectrometry. Thin layer radiochromatography was utilized for its quality control studies.
PIM was derived successfully after the
tosylation reaction. The radioiodination yield of PIM-TOS was over 85%.
In the current study, radioiodination potential of PIM with 131I, as a potential theranostic hypoxia agent was investigated. Further experimental studies should be performed for developing a novel hypoxia probe including theranostics approaches.