Keywords

131I Labeling, Rrl Peptide, Tumor, Molecular Imaging

Abstract

Study the application value of arginine-arginine-leucine (RRL), a small molecule peptide imaging agent that can specifically bind to tumor vascular endothelial cells, for tumor molecular imaging in melanoma mouse models. The chloramine-T method was used to label the small molecule peptide RRL with 131I, and the labeling conditions were optimized; the optimal labeling conditions were 50 ¦Ìg of RRL, 10 ¦ÌL of Na131I (74 MBq), 90 ¦Ìg of chloramine-T, and a total reaction volume of 100 ¦ÌL. , shake and react for 3 minutes. Marking rate >69%. The labeled product was purified using SephadexG25 column, and the radiochemical purity after purification was >95%. Green fluorescein (FITC) was used to label RRL, and in vitro cell binding experiments were conducted to observe the binding ability of RRL in different cells through the intensity of the fluorescence signal. In vitro cell binding experiment results show that RRL can not only specifically bind to tumor-derived vascular endothelial cells, but also to tumor parenchymal cells; SPECT imaging results of 131I-RRL on melanoma animal models show that 131I-RRL can specifically bind to tumor-derived vascular endothelial cells. Concentrated in tumor tissue, radioactive concentration foci were clearly visible 24 hours later. The above results show that the small molecule peptide RRL is a promising carrier for tumor radionuclide molecular imaging and treatment.

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Original research done by Lu Xia, Wang Rongfu, Zhang Chunli

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