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

YAO Shaobo; HU Kongzhen; TANG Ganghua; LIANG Xiang; JIANG Shende

doi:10.11889/j.0253-3219.2014.hjs.37.030301

您当前的位置：

首页 >

文章列表页 >

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

更新时间：2021-03-03

- Automated synthesis of novel cell death imaging tracer 18F-FPDuramycin
- NUCLEAR TECHNIQUES Vol. 37, Issue 3, Article number: 030301(2014)
- 作者机构：
  
  1. 天津大学药物科学与技术学院,天津,300072
  2. 中山大学附属第一医院核医学科,广州,510080
- 作者简介：
- 基金信息：
- DOI：10.11889/j.0253-3219.2014.hjs.37.030301
  CLC：
- Published：14 March 2014
- 稿件说明：
移动端阅览
YAO Shaobo, HU Kongzhen, TANG Ganghua, et al. Automated synthesis of novel cell death imaging tracer 18F-FPDuramycin[J]. Nuclear techniques, 2014, 37(3): 030301
DOI：

YAO Shaobo, HU Kongzhen, TANG Ganghua, et al. Automated synthesis of novel cell death imaging tracer 18F-FPDuramycin[J]. Nuclear techniques, 2014, 37(3): 030301 DOI： 10.11889/j.0253-3219.2014.hjs.37.030301.

摘要

通过引入氟标记辅助基团尝试多肽耐久霉素(Duramycin)的18F标记，探索其放化标记的自动化合成过程。使用国产PET-MF-2V-IT-I合成模块，先通过三步简单的反应，合成辅助基团4-nitrophenyl 2-[18F]fluoropropionate (18F-NFP)；随后将18F-NFP与耐久霉素反应生成18F-FPDuramycin，产物通过固相萃取的方法进行纯化，并对相应反应条件(溶剂、碱和反应时间)做了正交试验以确定其最佳条件。从18F离子起始合成18F-NFP共需80 min，未经衰变矫正，放化收率为(25±5)% (n=10)；以18F-NFP为原料合成至18F-FPDuramycin共需20 min，未经衰变矫正，放化收率为(70±3)% (n=8)，终产物18F-FPDuramycin的放化纯度大于99%，比活度为(23.7±13.7)GBq??mol?1 (n=10)。通过使用“二锅法”自动化合成18F-FPDuramycin，操作简便，收率稳定，质量控制检测满足放射性药物质量管理条例规定，能满足科研和临床正电子断层显像的要求。

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.Cited

关键词

Keywords

references

Views

下载量

CSCD

Alert me when the article has been cited

提交

Tools

Publicity Resources

Fully automated synthesis of ¹⁸F-FDG by acidic hydrolysis on domestic module

Automated synthesis of ¹⁸F-fluorothymidine via Sep-Pak purification

Automated synthesis of 16α-[¹⁸F]fluoro-17β-estrogen as estrogen receptor imaging probe of breast cancer

A simple and rapid automated synthesis of ¹⁸F-FHBG as a reporter gene expression PET imaging agent

Automated synthesis of 3’-deoxy-3’-[¹⁸F]fluorothymidine and O-(2-¹⁸F-fluoroethyl)-L-tyrosine as tumor imaging agents

Related Author

Jinming ZHANG

Yungang LI

Xiaojun ZHANG

Haifeng LI

WEN Fuhua DENG Huaifu TANG Ganghua YI Chang WU Kening

邓怀福

唐刚华

易畅

Related Institution

Department of Nuclear Medicine, The People's Liberation Army(PLA) General Hospital

Department of Nuclear Medicine, Jiang Xi Cancer Hospital

PET-CT Center,Department of Nuclear Medicine,The First Affiliated Hospital,Sun Yat-Sen University

复旦大学上海医学院肿瘤学系

PET Center,Shanghai Cancer Hospital Affiliated to Fudan University,and Department of Oncology,Medical College,Fudan University

AI问答

Address：2019 Jialuo Road, Jiading, Shanghai, China Postal code：201800
Tel：021-39194977 Email：LHB@sinap.ac.cn
Technical support is provided by Beijing Founder electronics co., LTD 沪ICP备05005479号-1 京公网安备11010802024621
It is recommended to read the content of this site in Chrome&IE9+. Please switch to extreme mode in browser 360.
Cookies We use cookies to help provide and enhance our service and tailor content. By continuing, you agree to the use of cookies.
Total Visits：881246 Visits Today：773

⁰