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Published on: April 25, 2025
Novel indium-111 labeled gastrin peptide analogues (MG-CL1-4): synthesis and quality control
Syed Ali-Raza Naqvi1, Zulfiqar Ali Khan, Saeed Ahmad Nagra
1Department of Chemistry, Government College University, Faisalabad, Pakistan.
Abstract:
Radiolabeled neuropeptides are widely investigated to diagnose and therapy of tumors. These peptides get internalization after binding with particular receptors at the surface of cells and finally move to lysosome. Internalization into tumor cells helps in mapping the infected site. Minigastrin peptide analogues (MG-CL1-4) were synthesised and labeled with 111-In radioisotope under different sets of conditions for imaging CCk-2 receptor bearing tumors. Different parameters such as temperature (80-100°C), pH (4-12), incubation time (5-30 minutes) and dilution effect were investigated to get the maximum labeling yield and stability. The results indicated that MG-CL1-4 is successfully labeled with indium-111 at pH 4.5 with heating at 98°C for 15 minute. At these conditions i.e. heating, pH and incubation minimum oxidized and maximum labeling yield, more than 94 %, was obtained. The labeling stability was studied by incubating the radiolabeled complex for predefined time points in PBSA and blood serum. Results show that more than 90% radiolabeled MG-CL1-4 remained intact.
Insights
Researchers optimized the radiolabeling of minigastrin analogues (MG-CL1-4) with indium-111 for tumor imaging. Optimal conditions yielded over 94% labeling efficiency and high stability for CCK-2 receptor-bearing tumors.
Area of Science:
- Nuclear Medicine
- Radiopharmaceutical Chemistry
- Oncology
Background:
- Radiolabeled neuropeptides are crucial for tumor diagnosis and therapy.
- Peptide internalization into tumor cells aids in mapping affected areas.
- Minigastrin analogues target cholecystokinin-2 (CCK-2) receptors, often overexpressed in tumors.
Purpose of the Study:
- To synthesize and optimize the radiolabeling of minigastrin peptide analogues (MG-CL1-4) with indium-111.
- To achieve high labeling yield and stability for effective imaging of CCK-2 receptor-bearing tumors.
- To determine optimal conditions for radiolabeling, including temperature, pH, and incubation time.
Main Methods:
- Synthesis of minigastrin peptide analogues (MG-CL1-4).
- Radiolabeling with indium-111 under varying conditions (temperature, pH, time).
- Optimization of labeling parameters to maximize yield and stability.
- Stability assessment of the radiolabeled complex in PBSA and blood serum.
Main Results:
- MG-CL1-4 was successfully labeled with indium-111.
- Optimal labeling achieved at pH 4.5, 98°C for 15 minutes.
- Labeling yield exceeded 94% with minimal oxidation under optimized conditions.
- Radiolabeled complex demonstrated over 90% stability in PBSA and blood serum.
Conclusions:
- Optimized radiolabeling of MG-CL1-4 with indium-111 is feasible.
- The developed method provides high yield and stability for potential tumor imaging applications.
- MG-CL1-4 shows promise as a targeting agent for CCK-2 receptor-positive tumors.
