Volume 26, Issue 140 (9-2016)                   J Mazandaran Univ Med Sci 2016, 26(140): 15-23 | Back to browse issues page

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Hasankhah M, Emrarian I, Sadeghzade N, Abedi S M. In vitro/In vivo Study of a New Bombesin Derivative with Tripeptide (Gly-Gly-Gly) Spacer as Potential Targeted Tumor Imaging Agent. J Mazandaran Univ Med Sci. 2016; 26 (140) :15-23
URL: http://jmums.mazums.ac.ir/article-1-8372-en.html
Abstract:   (2810 Views)

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.

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Type of Study: Research(Original) | Subject: Pharmacy

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