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Preparation and assessment of a new radiotracer technetium-99m-6-hydrazinonicotinic acid-tyrosine as a targeting agent in tumor detecting through single photon emission tomography.
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2020-08-26 , DOI: 10.1016/j.bioorg.2020.104181
Hemat Yaghoubi Mogadam 1 , Mostafa Erfani 2 , Mohammad Nikpassand 1 , Masoud Mokhtary 1
Affiliation  

The goal of investigation was to bring up an impressive way to synthesize technetium-99 m-6-hydrazinonicotinic acid-tyrosine (99mTc-HYNIC-Tyr), a newfound radiotracer, and to assess the capacity of being as a tumor scintigraphy agent. The conjugate was prepared by solid phase method using tritely chloride resin. The precursor HYNIC-Tyr was labeled with 99mTc which was accomplished at 100 °C through the coligands tricine and EDDA. Furthermore, the serum albumin binding, cellular attachment, organs uptake and tumor accumulation were measured. C6 glioma cells were used for cellular and tumor uptake studies. 99mTc-HYNIC-Tyr was prepared with labeling yield of >99% (n = 3). Radiotracer showed stability in serum proteins in incubates temperature. Specific cellular attachment of radiotracer was noticeable in C6 glioma cells with dissociation constant in nano molar range (21.03 ± 1.54 nM). The amount of uptake in C6 rat glioma xenograft was 2.61 ± 0.12 percent of injection dose per gram after 30 min. In whole-body scintigraphy, C6 glioma tumor was easy to be traced and interpreted at 1 h after administration of radiotracer. Our data suggest that 99mTc-HYNIC-Tyr, a new radiotracer based on amino acid, efficiently differentiates the tumor cells and goes into them. Our results indicate that this radiotracer has excellent capacity to detect tumor cells in rat and to be included as a radiopharmaceutical for detecting cancer tumors.



中文翻译:

新型放射性示踪剂tech-99m-6-肼基烟酸-酪氨酸作为靶向剂在单光子发射断层显像中的制备和评估。

研究的目的是提出一种令人印象深刻的方法来合成新发现的放射性示踪剂tech 99 m-6-肼基烟酸-酪氨酸(99m Tc-HYNIC-Tyr),并评估其作为肿瘤闪烁显像剂的能力。使用三苯甲基氯化物树脂通过固相方法制备缀合物。用99m Tc标记前体HYNIC-Tyr,可在100°C下通过大肠埃希氏菌和EDDA完成。此外,测量血清白蛋白结合,细胞附着,器官摄取和肿瘤积累。C6胶质瘤细胞用于细胞和肿瘤摄取研究。99m制备Tc-HYNIC-Tyr,标记收率> 99%(n = 3)。放射性示踪剂在孵育温度下对血清蛋白表现出稳定性。在C6胶质瘤细胞中,放射性示踪剂的特异性细胞附着是明显的,其解离常数在纳摩尔范围(21.03±1.54 nM)。30分钟后,C6大鼠神经胶质瘤异种移植的摄取量为每克注射剂量的2.61±0.12%。在全身闪烁显像术中,在施用放射性示踪剂后1 h易于追踪和解释C6胶质瘤肿瘤。我们的数据表明99mTc-HYNIC-Tyr是一种基于氨基酸的新型放射性示踪剂,可有效分化肿瘤细胞并进入其中。我们的结果表明,这种放射性示踪剂具有出色的检测大鼠肿瘤细胞的能力,可作为一种放射性药物用于检测癌症。

更新日期:2020-09-10
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