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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...
Autores principales: | , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2015
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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. |
format | Online Article Text |
id | pubmed-6272169 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2015 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
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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