The clinical impact and accessibility of 99m Tc tracers for cancer diagnosis would be greatly enhanced by the availability of a new, simple and easy labeling process and radiopharmaceuticals. 5-Fluorouracil (5-FU) is an anti-tumor drug which has played an important role for the treatment of breast carcinoma. In the present study, a new derivative of 5-FU was synthesized as (1-[{1'-(1''-deoxy-2'',3'':4'',5''-di-O-isopropylidene-β-D-fructopyranose-1''-yl)-1'H-1',2',3'-triazol-4'-yl}methyl]-5-fluorouracil) (E), and radiolabeled with 99m Tc. It was analyzed by radio thin layer chromatography (RTLC) for quality control and stability. The radiolabeled complex was subjected to in vitro cell binding studies to determine healthy and cancer cell affinity using HaCaT and MCF-7 cells, respectively. In addition, in vitro cytotoxicity studies of compound E were performed with HaCaT and MCF-5 cells. The radiochemical purity of the [99m Tc]TcE was found to be higher than 90 % at room temperature up to 6 h. The radiolabeled complex showed higher specific binding to MCF-7 cells than HaCaT cells. IC50 values of E were found 31.5±3.4 and 20.7±2.77 μM for MCF-7 and HaCaT cells, respectively. The results demonstrated the potential of a new radiolabeled E with 99m Tc has selective for breast cancer cells.

中文翻译：

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通过细胞培养研究对新型 5-氟尿嘧啶衍生物进行放射性标记和体外评估

99m Tc 示踪剂用于癌症诊断的临床影响和可及性将通过新的、简单易行的标记过程和放射性药物的可用性得到极大提高。5-氟尿嘧啶（5-FU）是一种抗肿瘤药物，在乳腺癌的治疗中发挥了重要作用。在本研究中，5-FU 的新衍生物合成为 (1-[{1'-(1''-deoxy-2'',3'':4'',5''-di-O-异亚丙基-β-D-吡喃果糖-1''-基)-1'H-1',2',3'-三唑-4'-基}甲基]-5-氟尿嘧啶) (E), 并用 99m 放射性标记吨。通过无线电薄层色谱 (RTLC) 对其进行分析以进行质量控制和稳定性。使用 HaCaT 和 MCF-7 细胞对放射性标记的复合物进行体外细胞结合研究，以确定健康细胞和癌细胞的亲和力，分别。此外，化合物 E 的体外细胞毒性研究是用 HaCaT 和 MCF-5 细胞进行的。发现 [99m Tc]TcE 的放射化学纯度在室温下最多 6 小时高于 90%。与 HaCaT 细胞相比，放射性标记复合物对 MCF-7 细胞的特异性结合更高。对于 MCF-7 和 HaCaT 细胞，发现 E 的 IC50 值分别为 31.5±3.4 和 20.7±2.77 μM。结果证明了具有 99m Tc 的新型放射性标记 E 对乳腺癌细胞具有选择性的潜力。MCF-7 和 HaCaT 细胞分别为 5±3.4 和 20.7±2.77 μM。结果证明了具有 99m Tc 的新型放射性标记 E 对乳腺癌细胞具有选择性的潜力。MCF-7 和 HaCaT 细胞分别为 5±3.4 和 20.7±2.77 μM。结果证明了具有 99m Tc 的新型放射性标记 E 对乳腺癌细胞具有选择性的潜力。