New freeze-dried kit for diagnosis of Bombesin receptor expressing tumors

سال انتشار: 1389
نوع سند: مقاله ژورنالی
زبان: انگلیسی
مشاهده: 309

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شناسه ملی سند علمی:

JR_IRJNM-18-2_002

تاریخ نمایه سازی: 27 فروردین 1399

چکیده مقاله:

  Introduction: It has been shown that some primary human tumors and their metastases, including prostate and breast tumors, over-express gastrin-releasing peptide (GRP) receptors. Bombesin is a neuropeptide with a high affinity for these GRP receptors. The purpose of this study was to prepare and evaluate the characteristics of a new Freeze-dried kit, [6-hydrazinopyridine-3-carboxylic acid (HYNIC)]-GABA-Bombesin [7-14] NH2 designed for the labeling with 99mTc using tricine and EDDA as coligand. Methods: Synthesis was performed on a solid phase using a standard Fmoc strategy and HYNIC precursor coupled at the N-terminus. Purified peptide conjugate was labeled with 99mTc at 100°C for 10 min. Radiochemical analysis involved ITLC and high-performance liquid chromatography methods. Peptide conjugate stability and affinity to human serum was challenged for 24 hours. The internalization rate was studied in GRP receptor expressing PC-3 cells. Biodistribution of radiopeptide was studied in rats. Results: Radiolabeling was performed at high specific activities, and radiochemical purity was > 98%. The stability of radiolabeled peptide in human serum was excellent. In vitro studies showed > 14% of activity was specific internalized into PC-3 cells up to 4 h. After injection into rat biodistribution data showed a rapid blood clearance, with renal excretion and specific binding towards GRP receptor-positive tissues such as pancreas (1.15±0.19% ID/g after 4 h). Conclusion: [99mTc-HYNIC]-GABA-Bombesin [7-14] NH2 showed favorable radiochemical and biological characteristics which make our new designed labeled peptide conjugate as a very suitable agent for diagnostic purposes in malignant tumors.

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نویسندگان

Mostafa Erfani

Nuclear Science Research School, Nuclear Science and Technology Research Institute, Atomic Energy organization of Iran, Tehran, Iran

Seyed Pezhman Shirmardi

Nuclear Science Research School, Nuclear Science and Technology Research Institute, Atomic Energy organization of Iran, Tehran, Iran

Mohammad Ghannadi Maragheh

Nuclear Science Research School, Nuclear Science and Technology Research Institute, Atomic Energy organization of Iran, Tehran, Iran

Mohammad Shafiei

Nuclear Science Research School, Nuclear Science and Technology Research Institute, Atomic Energy organization of Iran, Tehran, Iran