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Preliminary Biological Evaluation of (18)F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent

A novel annexin V derivative (Cys-Annexin V) with a single cysteine residue at its C-terminal has been developed and successfully labeled site-specifically with (18)F-FBEM. (18)F-FBEM was synthesized by coupling (18)F-fluorobenzoic acid ((18)F-FBA) with N-(2-aminoethyl)maleimide using optimized reac...

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Autores principales: Lu, Chunxiong, Jiang, Quanfu, Hu, Minjin, Tan, Cheng, Yu, Huixin, Hua, Zichun
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2015
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272169/
https://www.ncbi.nlm.nih.gov/pubmed/25789822
http://dx.doi.org/10.3390/molecules20034902
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author Lu, Chunxiong
Jiang, Quanfu
Hu, Minjin
Tan, Cheng
Yu, Huixin
Hua, Zichun
author_facet Lu, Chunxiong
Jiang, Quanfu
Hu, Minjin
Tan, Cheng
Yu, Huixin
Hua, Zichun
author_sort Lu, Chunxiong
collection PubMed
description A novel annexin V derivative (Cys-Annexin V) with a single cysteine residue at its C-terminal has been developed and successfully labeled site-specifically with (18)F-FBEM. (18)F-FBEM was synthesized by coupling (18)F-fluorobenzoic acid ((18)F-FBA) with N-(2-aminoethyl)maleimide using optimized reaction conditions. The yield of (18)F-FBEM-Cys-Annexin V was 71.5% ± 2.0% (n = 4, based on the starting (18)F-FBEM, non-decay corrected). The radiochemical purity of (18)F-FBEM-Cys-Annexin V was >95%. The specific radioactivities of (18)F-FBEM and (18)F-FBEM-Cys-Annexin V were >150 and 3.17 GBq/µmol, respectively. Like the 1st generation (18)F-SFB-Annexin V, the novel (18)F-FBEM-Cys-Annexin V mainly shows renal and to a lesser extent, hepatobiliary excretion in normal mice. In rat hepatic apoptosis models a 3.88 ± 0.05 (n = 4, 1 h) and 10.35 ± 0.08 (n = 4, 2 h) increase in hepatic uptake of (18)F-FBEM-Cys-Annexin V compared to normal rats was observed after injection via the tail vein. The liver uptake ratio (treated/control) at 2 h p.i. as measured via microPET correlated with the ratio of apoptotic nuclei in liver observed using TUNEL histochemistry, indicating that the novel (18)F-FBEM-Cys-Annexin V is a potential apoptosis imaging agent.
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spelling pubmed-62721692018-12-31 Preliminary Biological Evaluation of (18)F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent Lu, Chunxiong Jiang, Quanfu Hu, Minjin Tan, Cheng Yu, Huixin Hua, Zichun Molecules Article A novel annexin V derivative (Cys-Annexin V) with a single cysteine residue at its C-terminal has been developed and successfully labeled site-specifically with (18)F-FBEM. (18)F-FBEM was synthesized by coupling (18)F-fluorobenzoic acid ((18)F-FBA) with N-(2-aminoethyl)maleimide using optimized reaction conditions. The yield of (18)F-FBEM-Cys-Annexin V was 71.5% ± 2.0% (n = 4, based on the starting (18)F-FBEM, non-decay corrected). The radiochemical purity of (18)F-FBEM-Cys-Annexin V was >95%. The specific radioactivities of (18)F-FBEM and (18)F-FBEM-Cys-Annexin V were >150 and 3.17 GBq/µmol, respectively. Like the 1st generation (18)F-SFB-Annexin V, the novel (18)F-FBEM-Cys-Annexin V mainly shows renal and to a lesser extent, hepatobiliary excretion in normal mice. In rat hepatic apoptosis models a 3.88 ± 0.05 (n = 4, 1 h) and 10.35 ± 0.08 (n = 4, 2 h) increase in hepatic uptake of (18)F-FBEM-Cys-Annexin V compared to normal rats was observed after injection via the tail vein. The liver uptake ratio (treated/control) at 2 h p.i. as measured via microPET correlated with the ratio of apoptotic nuclei in liver observed using TUNEL histochemistry, indicating that the novel (18)F-FBEM-Cys-Annexin V is a potential apoptosis imaging agent. MDPI 2015-03-17 /pmc/articles/PMC6272169/ /pubmed/25789822 http://dx.doi.org/10.3390/molecules20034902 Text en © 2015 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Lu, Chunxiong
Jiang, Quanfu
Hu, Minjin
Tan, Cheng
Yu, Huixin
Hua, Zichun
Preliminary Biological Evaluation of (18)F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent
title Preliminary Biological Evaluation of (18)F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent
title_full Preliminary Biological Evaluation of (18)F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent
title_fullStr Preliminary Biological Evaluation of (18)F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent
title_full_unstemmed Preliminary Biological Evaluation of (18)F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent
title_short Preliminary Biological Evaluation of (18)F-FBEM-Cys-Annexin V a Novel Apoptosis Imaging Agent
title_sort preliminary biological evaluation of (18)f-fbem-cys-annexin v a novel apoptosis imaging agent
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6272169/
https://www.ncbi.nlm.nih.gov/pubmed/25789822
http://dx.doi.org/10.3390/molecules20034902
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