Cartilage-Specific Near-Infrared Fluorophores for Biomedical Imaging.
Cartilage-Specific Near-Infrared Fluorophores for Biomedical Imaging.
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DOI：
10.1002/anie.201502287
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发表时间：
2015-07-20
期刊：
影响因子：
--
通讯作者：
Choi HS
中科院分区：
文献类型：
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作者：
Hyun H;Owens EA;Wada H;Levitz A;Park G;Park MH;Frangioni JV;Henary M;Choi HS
在这项研究中，我们报告了一类新的近红外荧光造影剂，具有高特异性靶向软骨固有的荧光团的化学结构的合成。在单次低剂量静脉注射和≤ 4 h的清除时间后，这些药物与所有三种主要类型的软骨（透明软骨、弹性软骨和纤维软骨）结合，并且在不同物种中表现同样良好。化学结构相似性的分析揭示了软骨靶向的潜在药效团。我们的研究结果为组织工程、关节手术和软骨特异性药物开发的未来改进奠定了基础。合成了软骨特异性的近红外荧光团，并在小型和大型动物模型系统中测试了它们的性能。这些试剂不仅可以结合所有测试物种中的所有类型的软骨，而且还可以与其他靶向近红外荧光团（如骨特异性荧光团）结合，以提供前所未有的生物医学光学成像。
In this study we report the synthesis of a novel class of near-infrared fluorescent contrast agents that possess high-specificity targeting to cartilage inherent to the chemical structure of the fluorophore. After a single, low-dose intravenous injection and a clearance time of ≤ 4 h, these agents bind to all three major types of cartilage (hyaline, elastic, and fibrocartilage) and perform equally well across species. Analysis of chemical structure similarities reveals a potential pharmacophore for cartilage targeting. Our results lay the foundation for future improvements in tissue engineering, joint surgery, and cartilage-specific drug development. Near-infrared fluorophores specific for cartilage were synthesized and their performance tested in small and large animal model systems. Not only do these agents bind all types of cartilage in all species tested, but they can also be combined with other targeted near-infrared fluorophores, such as those specific to bone, to provide unprecedented biomedical optical imaging.