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Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium

Assessment of myocardial viability is deemed necessary to aid in clinical decision making whether to recommend revascularization therapy for patients with myocardial infarction (MI). Dianthraquinones such as hypericin (Hyp) selectively accumulate in necrotic myocardium, but were unsuitable for early...

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Autores principales: Wang, Qin, Yang, Shengwei, Jiang, Cuihua, Li, Jindian, Wang, Cong, Chen, Linwei, Jin, Qiaomei, Song, Shaoli, Feng, Yuanbo, Ni, Yicheng, Zhang, Jian, Yin, Zhiqi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4754898/
https://www.ncbi.nlm.nih.gov/pubmed/26878909
http://dx.doi.org/10.1038/srep21341
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author Wang, Qin
Yang, Shengwei
Jiang, Cuihua
Li, Jindian
Wang, Cong
Chen, Linwei
Jin, Qiaomei
Song, Shaoli
Feng, Yuanbo
Ni, Yicheng
Zhang, Jian
Yin, Zhiqi
author_facet Wang, Qin
Yang, Shengwei
Jiang, Cuihua
Li, Jindian
Wang, Cong
Chen, Linwei
Jin, Qiaomei
Song, Shaoli
Feng, Yuanbo
Ni, Yicheng
Zhang, Jian
Yin, Zhiqi
author_sort Wang, Qin
collection PubMed
description Assessment of myocardial viability is deemed necessary to aid in clinical decision making whether to recommend revascularization therapy for patients with myocardial infarction (MI). Dianthraquinones such as hypericin (Hyp) selectively accumulate in necrotic myocardium, but were unsuitable for early imaging after administration to assess myocardial viability. Since dianthraquinones can be composed by coupling two molecules of monomeric anthraquinone and the active center can be found by splitting chemical structure, we propose that monomeric anthraquinones may be effective functional groups for necrosis targetability. In this study, eight radioiodinated monomeric anthraquinones were evaluated as novel necrosis avid agents (NAAs) for imaging of necrotic myocardium. All (131)I-anthraquinones showed high affinity to necrotic tissues and (131)I-rhein emerged as the most promising compound. Infarcts were visualized on SPECT/CT images at 6 h after injection of (131)I-rhein, which was earlier than that with (131)I-Hyp. Moreover, (131)I-rhein showed satisfactory heart-to-blood, heart-to-liver and heart-to-lung ratios for obtaining images of good diagnostic quality. (131)I-rhein was a more promising “hot spot imaging” tracer for earlier visualization of necrotic myocardium than (131)I-Hyp, which supported further development of radiopharmaceuticals based on rhein for SPECT/CT ((123)I and (99m)Tc) or PET/CT imaging ((18)F and (124)I) of myocardial necrosis.
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spelling pubmed-47548982016-02-24 Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium Wang, Qin Yang, Shengwei Jiang, Cuihua Li, Jindian Wang, Cong Chen, Linwei Jin, Qiaomei Song, Shaoli Feng, Yuanbo Ni, Yicheng Zhang, Jian Yin, Zhiqi Sci Rep Article Assessment of myocardial viability is deemed necessary to aid in clinical decision making whether to recommend revascularization therapy for patients with myocardial infarction (MI). Dianthraquinones such as hypericin (Hyp) selectively accumulate in necrotic myocardium, but were unsuitable for early imaging after administration to assess myocardial viability. Since dianthraquinones can be composed by coupling two molecules of monomeric anthraquinone and the active center can be found by splitting chemical structure, we propose that monomeric anthraquinones may be effective functional groups for necrosis targetability. In this study, eight radioiodinated monomeric anthraquinones were evaluated as novel necrosis avid agents (NAAs) for imaging of necrotic myocardium. All (131)I-anthraquinones showed high affinity to necrotic tissues and (131)I-rhein emerged as the most promising compound. Infarcts were visualized on SPECT/CT images at 6 h after injection of (131)I-rhein, which was earlier than that with (131)I-Hyp. Moreover, (131)I-rhein showed satisfactory heart-to-blood, heart-to-liver and heart-to-lung ratios for obtaining images of good diagnostic quality. (131)I-rhein was a more promising “hot spot imaging” tracer for earlier visualization of necrotic myocardium than (131)I-Hyp, which supported further development of radiopharmaceuticals based on rhein for SPECT/CT ((123)I and (99m)Tc) or PET/CT imaging ((18)F and (124)I) of myocardial necrosis. Nature Publishing Group 2016-02-16 /pmc/articles/PMC4754898/ /pubmed/26878909 http://dx.doi.org/10.1038/srep21341 Text en Copyright © 2016, Macmillan Publishers Limited http://creativecommons.org/licenses/by/4.0/ This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/
spellingShingle Article
Wang, Qin
Yang, Shengwei
Jiang, Cuihua
Li, Jindian
Wang, Cong
Chen, Linwei
Jin, Qiaomei
Song, Shaoli
Feng, Yuanbo
Ni, Yicheng
Zhang, Jian
Yin, Zhiqi
Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium
title Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium
title_full Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium
title_fullStr Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium
title_full_unstemmed Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium
title_short Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium
title_sort discovery of radioiodinated monomeric anthraquinones as a novel class of necrosis avid agents for early imaging of necrotic myocardium
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4754898/
https://www.ncbi.nlm.nih.gov/pubmed/26878909
http://dx.doi.org/10.1038/srep21341
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