A Novel Tumor Hypoxia Imaging Agent: [^99mTc]Tc(CO)₃-CPA-2-NIM.

IF 1.5 4区医学 Q3 PHARMACOLOGY & PHARMACY Current radiopharmaceuticals Pub Date : 2023-01-01 DOI:10.2174/1874471016666230320144641

Xiao Lin, Xiaojie Tan, Fengyu Wu, Qian Yu

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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 [^99mTc]Tc(CO)₃-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 [^99mTc]Tc(CO)₃-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. In vitro 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 [^99mTc]Tc(CO)₃-CPA-2-NIM has the possibility of becoming a tumor hypoxia imaging agent.

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新型肿瘤缺氧显像剂:[99mTc]Tc(CO)3-CPA-2-NIM。

简介:低氧显像剂可以选择性地停留在缺氧组织中，可以直接反映缺氧的部位和程度。方法:合成一种新型肿瘤缺氧显像探针[99mTc]Tc(CO)3-CPA-2-NIM，并对其生物学行为进行评价，评价其成为合格肿瘤缺氧显像剂的可能性。结果:HPLC纯化后[99mTc]Tc(CO)3-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)，表明该配合物为亲水性配合物。体外细胞实验表明，该复合物对氧浓度< 10 ppm(百万分之一)的缺氧具有选择性。在S180荷瘤小鼠体内的生物分布实验表明，注射后2 h，肿瘤摄取以小鼠瘤肌比达到最高。结论:配合物[99mTc]Tc(CO)3-CPA-2-NIM有可能成为肿瘤缺氧显像剂。

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来源期刊

Current radiopharmaceuticals PHARMACOLOGY & PHARMACY-

CiteScore

3.20

自引率

4.30%

发文量