In vitro/In vivo Study of a New Bombesin Derivative with Tripeptide (Gly-Gly-Gly) Spacer as Potential Targeted Tumor Imaging Agent
Abstract:
Background and
Purpose
Bombesin is a 14-amino acid peptide with high biological functions which has a high affinity to GRP )Gastrin releasing peptide( receptor. GRP receptors are overexpressed in many malignant tumors such as prostate and breast cancers. The purpose of this study was to prepare [HYNIC-(Gly)3-D-Phe13]Bombesin(7-14) to label it easily by 99mTc and to evaluate it as a potential agent for imaging the tumors that have GRP receptors.
Materials And Methods
In this experimental study, the prepared derivative Bombesin was radiolabelled by 99mTc at 100°C in 10 minutes using the exchange method and radiolabelling analysis was applied by TLC and HPLC. Specific absorption test and specific internalization using prostate cancer cells PC-3 was done by blocking and unblocking the receptors. Biodistribution were determined in normal mice.
Results
More than 95% radiolabelling was obtained. Specific absorption and internalization after 4 hours were 17.9% and 9.5%, respectively in PC-3 cancer cells. Biodistribution data showed rapid clearance from blood with major renal excretion and specific binding to tissues that have GRP receptors such as pancreas.
Conclusion
Conjugated peptide radiolabelled with 99mTc has promising characteristics as potential agent for imaging the tumors that overexpress the GRP receptors.
Language:
Persian
Published:
Journal of Mazandaran University of Medical Sciences, Volume:26 Issue: 140, 2016
Pages:
15 to 23
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