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Radioiodination and in vivo assessment of the potential of newly synthesized pyrrolizine-5-carboxamides derivative in tumor model.
Applied Radiation and Isotopes ( IF 1.6 ) Pub Date : 2020-08-08 , DOI: 10.1016/j.apradiso.2020.109369
Ashgan F Mahmoud 1 , Mohamed H Aboumanei 1 , S Abdelhalim 1 , Yasser A Hassan 2 , I T Ibrahim 3
Affiliation  

Recently, pyrrolizine derivatives have been reported to possess numerous anticancer activities. In a previous study, (EZ)-6-((4-chlorobenzylidene)-amino)-7-cyano-N-(p-tolyl)-2,3-dihydro-1H-pyrrolizine carboxamide (EZPCA) compound was synthesized and the cytotoxic activity of EZPCA toward COX-2 enzyme (overexpressed in cancer cells) was reported. In order to assess the suitability of this compound as a promising pilot structure for in vivo applications, EZPCA was radiolabeled with radioiodine-131 (131I) and various factors affecting radiolabeling process were studied. Quality control studies of [131I]iodo-EZPCA were performed using paper chromatography and HPLC was used as a co-chromatographic technique for confirming the radiochemical yield. Biodistribution studies of [131I]iodo-EZPCA were undertaken in normal and tumor bearing mice. The radiochemical yield percentage of [131I]iodo-EZPCA was 94.20 ± 0.12%. The biodistribution results showed evident tumor uptake of [131I]iodo-EZPCA with promising target/non-target (T/NT) ratios. As a conclusion, these data suggest that [131I]iodo-EZPCA had high binding efficiency, high tumor uptake and sufficient stability to be used be used in diagnostic studies.



中文翻译:

放射性碘化和体内评估新合成的 pyrrolizine-5-carboxamides 衍生物在肿瘤模型中的潜力。

最近,据报道吡咯嗪衍生物具有多种抗癌活性。在之前的研究中,(EZ)-6-((4-chlorobenzylidene)-amino)-7- cyano - N -( p -tolyl)-2,3-dihydro-1H-pyrrolizine carboxamide (EZPCA) 化合物被合成并报道了 EZPCA 对 COX-2 酶(在癌细胞中过度表达)的细胞毒活性。为了评估该化合物作为体内应用的有前途的先导结构的适用性,EZPCA 用放射性碘 131 ( 131 I) 进行放射性标记,并研究了影响放射性标记过程的各种因素。[ 131 的质量控制研究I]iodo-EZPCA 使用纸色谱法进行,HPLC 用作共色谱技术以确认放射化学产率。[ 131 I]iodo-EZPCA 的生物分布研究在正常小鼠和荷瘤小鼠中进行。[ 131 I]碘-EZPCA的放射化学产率为94.20±0.12%。生物分布结果显示[ 131 I]碘-EZPCA的明显肿瘤吸收具有有希望的靶/非靶(T/NT)比率。作为结论,这些数据表明[ 131 I]碘-EZPCA具有高结合效率、高肿瘤吸收和足够的稳定性以用于诊断研究。

更新日期:2020-08-08
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