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    Home > Chemicals Industry > Chemical Technology > Shanghai Institute of Medicine and others develop PET/fluorescence bimodal small molecule imaging probes targeting myocardial mitochondria

    Shanghai Institute of Medicine and others develop PET/fluorescence bimodal small molecule imaging probes targeting myocardial mitochondria

    • Last Update: 2022-01-09
    • Source: Internet
    • Author: User
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    X-ray, CT, magnetic resonance, ultrasound and radionuclide imaging are commonly used clinically as diagnostic methods for cardiovascular diseases


    In previous research, the Molecular Imaging Center of Shanghai Institute of Materia Medica, Chinese Academy of Sciences discovered that indole ethylene quinoline salts F16 compounds are a promising diagnostic and therapeutic compound targeting tumor mitochondria (Chemical Science 2019, 10 (34), 7946- 7951), has a high degree of hydrophobicity, can cross the hydrophobic barrier of cell membrane and mitochondrial membrane, highly enriched in tumor cells with higher mitochondrial membrane potential (the membrane potential of cardiomyocyte mitochondria is also higher)


    Recently, researchers from the Molecular Imaging Center of Shanghai Institute of Pharmaceuticals published research papers online in the Journal of Medicinal Chemistry under the title Development of mitochondria targeted small molecule dyes for myocardial PET and fluorescence bimodal imaging.


    Researchers designed and synthesized a series of F16 derivative compounds based on the small molecule compound F16 (Figure 2a), and screened out the preferred compound 5MEF through the fluorescence imaging experiment of small animal tissues in vitro (Figure 2b)


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    The researchers used a two-step method to label the preferred compound 5MEF with 18 F.


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    In small animal PET/CT imaging, 18 F-5MEF also showed good cardiac imaging effects.


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    In summary, the probe 5MEF, developed based on the mitochondrial membrane potential targeting mechanism, has certain advantages in the early diagnosis of heart failure and the accurate assessment of myocardial survival in various cardiovascular diseases


    Figure 1 Myocardial PET/fluorescence dual-modal probe 5MEF

    Figure 2a The structure of a series of F16 derivative compounds; b F16 derivative mouse tissue fluorescence imaging results; c Myocardial cell mitochondria 5MEF and mitochondrial dye co-localization imaging

    Figure 3 Small animal PET/CT imaging of radioactive probe 18 F-5MEF and time activity curve of each organ

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