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
Rok vydání: 2018
Předmět:
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