Noninvasive PET Imaging of a Ga-68-Radiolabeled RRL-Derived Peptide in Hepatocarcinoma Murine Models
Autor: | Yan Huo, Xiaoxi Pang, Haoyuan Shen, Rongfu Wang, Xueqi Chen, Lei Kang, Xuhe Liao, Ping Yan, Chunli Zhang |
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Rok vydání: | 2018 |
Předmět: |
Cancer Research
Biodistribution Carcinoma Hepatocellular Peptide Gallium Radioisotopes 030218 nuclear medicine & medical imaging law.invention Flow cytometry 03 medical and health sciences Mice 0302 clinical medicine Confocal microscopy law Cell Line Tumor medicine Animals Humans Radiology Nuclear Medicine and imaging Tissue Distribution Gamma counter chemistry.chemical_classification medicine.diagnostic_test Liver Neoplasms Fluorescence Disease Models Animal Oncology chemistry Positron emission tomography Positron-Emission Tomography Biophysics Molecular imaging Peptides |
Zdroj: | Molecular imaging and biology. 21(2) |
ISSN: | 1860-2002 |
Popis: | Tc-99m- and I-131-labeled arginine-arginine-leucine (RRL) peptides have shown the feasibility of tumor imaging in our previous studies. However, there have been no reports using RRL peptide for positron emission tomography (PET) imaging. In this study, RRL was radiolabeled with Ga-68 under optimized reaction conditions to develop a better specific and effective tumor imaging agent. RRL was synthesized and conjugated to a bifunctional chelating agent (DOTA-NHS), then radiolabeled with Ga-68. Labeling yield was optimized by varying pH, temperature, and reaction time and the stability was evaluated in human fresh serum. Cellular uptakes of [68Ga]DOTA-RRL and FITC-conjugated RRL in HepG2 cells were evaluated using a gamma counter, confocal microscopy, and flow cytometry. PET images and biodistribution were performed in HepG2 tumor-bearing mice after injection of [68Ga]DOTA-RRL or [68Ga]GaCl3 at different time points. Further, blocking study was investigated using cold RRL. The labeling yield of [68Ga]DOTA-RRL was 80.6 ± 3.9 % with a pH of 3.5–4.5 at 100 °C for 15 min. The cellular uptake of [68Ga]DOTA-RRL in HepG2 cells was significantly higher than that of [68Ga]GaCl3 (P |
Databáze: | OpenAIRE |
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