Nuclear Techniques ›› 2014, Vol. 37 ›› Issue (03): 30301-030301.doi: 10.11889/j.0253-3219.2014.hjs.37.030301

• NUCLEAR CHEMISTRY, RADIOCHEMISTRY, RADIOPHARMACEUTICALS AND NUCLEAR MEDICINE • Previous Articles     Next Articles

Automated synthesis of novel cell death imaging tracer 18F-FPDuramycin

YAO Shaobo1,2 HU Kongzhen2 TANG Ganghua2 LIANG Xiang2 JIANG Shende1   

  1. 1(School of Pharmaceutical Science and Technology, Tianjin University, Tianjin 300072, China) 2(Department of Nuclear Medicine, the First Af?liated Hospital, Sun Yat-Sen University, Guangzhou 510080, China)
  • Received:2013-11-11 Revised:2013-12-24 Online:2014-03-10 Published:2014-03-14

Abstract:

Background: The noninvasive imaging of cell death plays an important role in the evaluation of degenerative diseases and detection of tumor treatments. Duramycin, a peptide with 19-amino acid, is produced by Streptoverticillium cinnamoneus. It binds specifically to phosphatidylethanolamine (PE), a novel molecular target for cell death. Purpose: The aim is to develop a synthetic method to label duramycin using 18F ion. The automated synthesis was carried out by multi-step procedure on the modified PET-MF-2V-IT-I synthesizer. Methods: Firstly, the prosthetic group of 4-nitrophenyl 2-[18F]fluoropropionate (18F-NFP) was automatically synthesized by a convenient three-step procedure. Secondly, 18F-FPDuramycin was synthesized by conjunction of 18F-NFP with duramycin, which was purified by a solid-phase extraction cartridge. Orthogonal test was performed to confirm the suitable reaction conditions (solvent, base and temperature). Results: The radiochemical yields of 18F-NFP were (25±5)% (n=10, decay-uncorrected) based on [18F]fluoride in 80 min. 18F-FPDuramycin was obtained with yield of (70±3)% (n=8, decay-uncorrected) based on 18F-NFP within 20 min. The radiochemical purity of 18F-FPDuramycin was greater than 99% and the specific activity was greater than (23.7±13.7) GBq??mol?1 (n=10). Conclusion: 18F-FPDuramycin injection is easy to be prepared with “two-pot reaction” and is a promising radiotracer used for the clinical and scientific study on positron emission tomography (PET) imaging.

Key words: Automated synthesis, 18F-FPDuramycin, Cell death, Phosphatidylethanolamine, Radiolabeling