当前位置: X-MOL 学术J. Porphyr. Phthalocyanines › 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.)
Radiosynthesis, molecular modeling and biodistribution of 99mTc-Protoporphyrin as a preclinical model for tumor diagnosis
Journal of Porphyrins and Phthalocyanines ( IF 1.5 ) Pub Date : 2020-09-29 , DOI: 10.1142/s1088424620500352
Mohamed A. Gizawy 1, 2 , Mohsen M. T. El-Tahawy 3 , Mohamed A. Motaleb 1
Affiliation  

Porphyrins are among the most important and widely used compounds involved in a variety of chemical and biochemical applications. These molecules exhibit very special properties that encourage researchers to label many derivatives with diagnostic or therapeutic radionuclides for medical applications. This study reports the radiolabeling and biodistribution of 99mTc-protoporphyrin IX (99mTc-PPIX) as a novel potential solid-tumor imaging agent. The factors affecting the radiolabeling process were varied to achieve maximum radiochemical yield. 99mTc-PPIX was obtained in high yield of 97.34 ± 0.21% and high stability in serum up to 24 h. The radiochemical yield of 99mTc-PPIX was assessed by a combination of a paper chromatographic technique and HPLC. A computational analysis for all the potential structures that may be formed due to the interaction between protoporphyrin IX and technetium was performed via the DFT method of calculations in gas phase to predict the most likely structure. Molecular docking was further employed to shed light on the nature of the interaction between the most stable complexes with the target protein. Finally, the in-vivo biodistribution of 99mTc-PPIX complex was evaluated in solid-tumor-bearing mice and high tumor/tissue ratio of 5.17 ± 0.34 at 60 min post injection was obtained. Our finding clearly suggests 99mTc-PPIX as a potential SPECT agent for tumor imaging.

中文翻译:

99mTc-原卟啉的放射合成、分子建模和生物分布作为肿瘤诊断的临床前模型

卟啉是涉及各种化学和生化应用的最重要和最广泛使用的化合物之一。这些分子表现出非常特殊的特性,鼓励研究人员用诊断或治疗放射性核素标记许多衍生物用于医疗应用。本研究报告了放射性标记和生物分布99Tc-原卟啉 IX (99Tc-PPIX)作为一种新型潜在的实体瘤显像剂。改变影响放射性标记过程的因素以实现最大的放射化学产量。99Tc-PPIX 以 97.34 ± 0.21% 的高产率和在血清中长达 24 小时的高稳定性获得。放射化学产率99Tc-PPIX 通过纸层析技术和 HPLC 的组合进行评估。对由于原卟啉 IX 和锝之间的相互作用而可能形成的所有潜在结构进行了计算分析通过气相中的 DFT 计算方法可预测最可能的结构。分子对接进一步用于阐明最稳定的复合物与靶蛋白之间相互作用的性质。最后,体内生物分布99在实体瘤小鼠中评估 Tc-PPIX 复合物,并在注射后 60 分钟获得 5.17 ± 0.34 的高肿瘤/组织比率。我们的发现清楚地表明99Tc-PPIX 作为肿瘤成像的潜在 SPECT 试剂。
更新日期:2020-09-29
down
wechat
bug