当前位置: X-MOL 学术J. Radioanal. Nucl. Chem. › 论文详情
Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)
Synthesis, 99mTc-radiolabeling and in vivo evaluation of a new sulphonamide derivative for solid tumor imaging
Journal of Radioanalytical and Nuclear Chemistry ( IF 1.5 ) Pub Date : 2020-08-05 , DOI: 10.1007/s10967-020-07317-z
H. A. Shamsel-Din , E. G. Zaki

A novel sulphonamide derivative (EPBS) was prepared at high yield and characterized by 1H NMR and infrared radiation spectroscopy. Its cytotoxic activity was examined in breast carcinoma (MCF-7) cells at a dose of 25 μg/mL. Approximately 68 percent effective inhibition has been achieved. Furthermore, the synthesized ligand was directly radiolabeled with technetium-99m using sodium borohydride. High radiochemical purities (95.5%) were determined using radio-paper chromatography and electrophoresis. Its in vivo evaluation in tumor bearing mice demonstrated a high tumor uptake of the 99mTc-EPBS complex at 30 min post injection (6.74%) and tumor/muscle (T/NT) ratio equal to 5.04 ± 0.05. In conclusion, 99mTc-EPBS agent showed favorable characteristics for the radio-diagnosis of solid tumors.

中文翻译:

用于实体瘤成像的新型磺胺衍生物的合成、99mTc 放射性标记和体内评价

以高产率制备了一种新型磺酰胺衍生物 (EPBS),并通过 1 H NMR 和红外辐射光谱对其进行了表征。在乳腺癌 (MCF-7) 细胞中以 25 μg/mL 的剂量检查其细胞毒活性。已经实现了大约 68% 的有效抑制。此外,合成的配体使用硼氢化钠直接用锝 99m 进行放射性标记。使用放射纸色谱法和电泳法测定了高放射化学纯度 (95.5%)。其在荷瘤小鼠中的体内评估表明,在注射后 30 分钟 (6.74%) 和肿瘤/肌肉 (T/NT) 比率等于 5.04 ± 0.05 时,99mTc-EPBS 复合物的肿瘤吸收率很高。总而言之,99mTc-EPBS 试剂显示出对实体瘤的放射诊断有利的特性。
更新日期:2020-08-05
down
wechat
bug