一种新型肿瘤乏氧显影剂：[Tc]Tc(CO)-CPA-2-NIM。

A Novel Tumor Hypoxia Imaging Agent: [Tc]Tc(CO)-CPA-2-NIM.

机构信息

Department of Environmental Chemistry, National Institute of Environmental Health, CDC, China.

Department of Gastrointestinal Surgery, The Affiliated Hospital of Qingdao University, Qingdao, Shandong, 266000, China.

出版信息

Curr Radiopharm. 2023;16(4):300-307. doi: 10.2174/1874471016666230320144641.

DOI:10.2174/1874471016666230320144641

PMID:36959152

Abstract

INTRODUCTION

Hypoxia imaging agents can selectively remain in hypoxic tissue, which can directly reflect the location and degree of hypoxia.

METHODS

Synthesized a novel tumor hypoxia imaging probe [Tc]Tc(CO)-CPA-2-NIM and evaluated its biological behavior with the purpose to assess its possibility of becoming a qualified tumor hypoxia imaging agent.

RESULTS

Radiochemcial purity of [Tc]Tc(CO)-CPA-2-NIM was greater than 95% after HPLC purification. Lipophilicity coefficient of this complex was -1.74 ± 0.10 (n = 5, number of experiments), indicating it was a hydrophilic complex. cell experiments demonstrated that this complex has selectivity for hypoxia at oxygen concentrations < 10 ppm (parts per million). Biodistribution experiment in S180 tumor bearing mice showed that tumor uptake reached its highest at 2 h post-injection with mice tumor-to-muscle ratio.

CONCLUSIONS

Complex [Tc]Tc(CO)-CPA-2-NIM has the possibility of becoming a tumor hypoxia imaging agent.

摘要

简介

缺氧成像剂可以选择性地保留在缺氧组织中，直接反映缺氧的位置和程度。

方法

合成了一种新型肿瘤缺氧成像探针[Tc]Tc(CO)-CPA-2-NIM，并评估了其生物学行为，目的是评估其成为合格的肿瘤缺氧成像剂的可能性。

结果

经 HPLC 纯化后，[Tc]Tc(CO)-CPA-2-NIM 的放射化学纯度大于 95%。该配合物的亲脂性系数为-1.74±0.10（n=5，实验次数），表明它是一种亲水性配合物。细胞实验表明，该配合物在氧浓度<10ppm（百万分率）时对缺氧具有选择性。在 S180 荷瘤小鼠的生物分布实验中，注射后 2 小时肿瘤摄取达到最高，肿瘤与肌肉的比值。