Syntheses and preliminary evaluation of [18F]AlF‐NOTA‐G‐TMTP1 for PET imaging of high aggressive hepatocellular carcinoma. (1st March 2016)

• Record Type: Journal Article
• Authors: Li, Yesen; Zhang, Deliang; Shi, Ying; Guo, Zhide; Wu, Xinying; Ren, Jian‐Lin; Zhang, Xianzhong; Wu, Hua
• Is Part Of: Contrast media & molecular imaging. Volume 11:Number 4(2016:Jul./Aug.)
• Page Start: 262
• Page End: 271
• Publication Date: 2016-03-01
• Subjects: high metastatic -- 18F‐labeling -- G‐TMTP1 -- PET imaging -- 18F‐AlF chelation; Diagnostic imaging -- Periodicals; Magnetic resonance imaging -- Periodicals; Contrast media (Diagnostic imaging) -- Periodicals; Contrast Media -- Periodicals; Diagnostic Imaging -- Periodicals; Substances de contraste -- Périodiques; Diagnostics moléculaires -- Périodiques; Imagerie médicale; Substance de contraste; Périodique électronique (Descripteur de forme); Ressource Internet (Descripteur de forme); 616.0754
• DOI: 10.1002/cmmi.1688
• Languages: English
• ISSNs: 1555-4309

Abstract

Abstract : The goal of this study is to evaluate a new 18 F‐labeled imaging agent for diagnosing high metastatic (aggressive) hepatocellular carcinoma using positron emission tomography (PET). The new 18 F‐labeled imaging agent [ 18 F]AlF‐NOTA‐G‐TMTP1 was synthesized and radiolabeled with 18 F using NOTA‐AlF chelation method. The tumor‐targeting characteristics of [ 18 F]AlF‐NOTA‐G‐TMTP1 was assessed in HepG2, SMCC‐7721, HCC97L and HCCLM3 xenografts. The total synthesis time was about 20 min with radiochemical yield of 25 ± 6%. The specific activity was about 11.1–14.8 GBq/µmol at the end of synthesis based on the amount of peptide used and the amount of radioactivity trapped on the C18 column. The log P value of [ 18 F]AlF‐NOTA‐G‐TMTP1 was ‐3.166 ± 0.022. [ 18 F]AlF‐NOTA‐G‐TMTP1 accumulated in SMCC‐7721 and HCCLM3 tumors (high metastatic potential) in vivo and result in tumor/muscle (T/M) ratios of 4.5 ± 0.3 and 4.7 ± 0.2 (n = 4) as measured by PET at 40 min post‐injection (p.i.). Meanwhile, the tumor/muscle (T/M) ratios of HepG2 and HCC97L tumors (low metastatic potential) were1.6 ± 0.3 and 1.8 ± 0.4. The tumor uptake of [ 18 F]AlF‐NOTA‐G‐TMTP1 could be inhibited 61.9% and 57.6% by unlabeled G‐TMTP1 in SMCC‐7721 and HCCLM3 xenografts at 40 min p.i., respectively. Furthermore, [ 18 F]AlF‐NOTA‐G‐TMTP1 showed pretty low activity in the liver and intestines in all tumor bearing mice, such in vivo distribution pattern would be advantageous for the detection of hepatic carcinoma. Overall, [ 18 F]AlF‐NOTA‐G‐TMTP1 may specifically target high metastatic or/and aggressive hepatocellular carcinoma with low background activity and, therefore, holds the potential to be used as an imaging agent for detecting tumor lesions within the liver area. Copyright © 2016 John Wiley & Sons, Ltd. Abstract : A new 18 F‐labeled imaging agent [ 18 F]AlF‐NOTA‐G‐TMTP1 was synthesized and radiolabeled with 18 F using NOTA‐AlF chelation method. [ 18 F]AlF‐NOTA‐G‐TMTP1 can specifically target high metastatic or/and aggressive hepatocellular carcinoma with low background activity and, therefore, holds the potential to be used as an imaging agent for detecting tumor lesions within the liver area.