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用于坏死心肌成像的新型F标记1-羟基蒽醌衍生物

Novel F-Labeled 1-Hydroxyanthraquinone Derivatives for Necrotic Myocardium Imaging.

作者信息

Ji Ai-Yan, Jin Qiao-Mei, Zhang Dong-Jian, Zhu Hua, Su Chang, Duan Xing-Hua, Bian Li, Sun Zi-Ping, Ni Yi-Cheng, Zhang Jian, Yang Zhi, Yin Zhi-Qi

机构信息

Department of Natural Medicinal Chemistry & Jiangsu Key Laboratory of Natural Medicines, China Pharmaceutical University, Nanjing 210009, Jiangsu, China; Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, Jiangsu, China; Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, Jiangsu, China.

Laboratories of Translational Medicine, Jiangsu Province Academy of Traditional Chinese Medicine, Nanjing 210028, Jiangsu, China; Affiliated Hospital of Integrated Traditional Chinese and Western Medicine, Nanjing University of Chinese Medicine, Nanjing 210028, Jiangsu, China.

出版信息

ACS Med Chem Lett. 2016 Dec 28;8(2):191-195. doi: 10.1021/acsmedchemlett.6b00398. eCollection 2017 Feb 9.

DOI:10.1021/acsmedchemlett.6b00398
PMID:28197310
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC5304286/
Abstract

Rapid detection and precise evaluation of myocardial viability is necessary to aid in clinical decision making whether to recommend revascularization for patients with myocardial infarction (MI). Three novel F-labeled 1-hydroxyanthraquinone derivatives were synthesized, characterized, and evaluated as potential necrosis avid imaging agents for assessment of myocardial viability. Among these tracers, [F]FA3OP emerged as the most promising compound with best stability and highest targetability. Clear PET images of [F]FA3OP were obtained in rat model of myocardial infarction and reperfusion at 1 h after injection. In addition, the possible mechanisms of [F]FA3OP for necrotic myocardium were discussed. The results showed [F]FA3OP may bind DNA to achieve targetability to necrotic myocardium by intercalation. In summary, [F]FA3OP was a more promising "hot spot imaging" tracer for rapid visualization of necrotic myocardium.

摘要

快速检测和精确评估心肌活力对于辅助临床决策是否为心肌梗死（MI）患者推荐血运重建至关重要。合成了三种新型F标记的1-羟基蒽醌衍生物，对其进行了表征，并评估其作为评估心肌活力的潜在坏死亲和成像剂。在这些示踪剂中，[F]FA3OP成为最有前景的化合物，具有最佳的稳定性和最高的靶向性。在注射后1小时，在心肌梗死和再灌注大鼠模型中获得了清晰的[F]FA3OP PET图像。此外，还讨论了[F]FA3OP对坏死心肌的可能作用机制。结果表明，[F]FA3OP可能通过嵌入结合DNA以实现对坏死心肌的靶向性。总之，[F]FA3OP是一种更有前景的“热点成像”示踪剂，可快速显示坏死心肌。

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Discovery of Radioiodinated Monomeric Anthraquinones as a Novel Class of Necrosis Avid Agents for Early Imaging of Necrotic Myocardium.放射性碘化单体蒽醌作为一类新型坏死亲和剂用于坏死心肌早期成像的发现。
Sci Rep. 2016 Feb 16;6:21341. doi: 10.1038/srep21341.
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