Development of68Ga-SCN-DOTA-Capsaicin as an Imaging Agent Targeting Apoptosis and Cell Cycle Arrest in Breast Cancer
Autor: | Gun Gyun Kim, Jeong-Hoon Park, Jun Young Lee, Sang-Yeun Lee, Sang Wook Kim, Seung Dae Yang, Min Goo Hur |
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Rok vydání: | 2017 |
Předmět: |
0301 basic medicine
Cancer Research Biodistribution Cell cycle checkpoint Pharmacology 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Breast cancer Medicine DOTA Radiology Nuclear Medicine and imaging neoplasms medicine.diagnostic_test business.industry General Medicine medicine.disease Imaging agent 030104 developmental biology Oncology chemistry Capsaicin Positron emission tomography Apoptosis 030220 oncology & carcinogenesis business Nuclear medicine |
Zdroj: | Cancer Biotherapy and Radiopharmaceuticals. 32:169-175 |
ISSN: | 1557-8852 1084-9785 |
DOI: | 10.1089/cbr.2017.2186 |
Popis: | 68Ga-labeled capsaicin using a DOTA (1,4,7,10-tetraazocyclododecane-N,N',N″,N'″-tetraacetic acid) derivative [68Ga-SCN-Benzyl(Bn)-DOTA-capsaicin] was studied for the diagnosis of breast cancers, such as MCF-7 and SK-BR-3. The standard compound, 69Ga-SCN-Bn-DOTA-capsaicin, was also prepared and characterized by spectroscopic analysis. The binding affinity of 68Ga-SCN-Bn-DOTA-capsaicin was evaluated by using breast cancer cell lines (MCF-7, SK-BR-3) and colon cancer cell (CT-26); the biodistribution was carried out by using MCF-7-bearing nude mice, after which the positron emission tomography (PET) images were obtained at different time intervals (15-120 minutes). 68Ga-SCN-Bn-DOTA-capsaicin showed a cellular uptake of 0.93% Injected Dose (ID) after 30 minutes of incubation, whereas 68Ga-SCN-Bn-DOTA showed a lower uptake of 0.25% ID. The tumor-to-blood ID/g% ratios increased and were found to be 0.49, 0.22, and 0.77 for 15, 30, and 60 minutes, respectively. The small-animal PET study showed that the uptake of 68Ga-SCN-Bn-DOTA-capsaicin was higher in the tumor regions even at 30 minutes after injection. These results suggest that 68Ga-SCN-Bn-DOTA-capsaicin is a potential targeting agent for PET imaging of MCF-7. |
Databáze: | OpenAIRE |
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