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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >PEGylated BF 2 -Azadipyrromethene (NIR-AZA) fluorophores, for intraoperative imaging
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PEGylated BF 2 -Azadipyrromethene (NIR-AZA) fluorophores, for intraoperative imaging

机译：聚乙二醇化的BF 2-唑氟甲烯（NIR-AZA）荧光团，用于术中成像

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Clinical imaging utilising near-infrared fluorescence is growing as an intraoperative aid for the decision-making processes during complex surgical procedures. Existing uses include perfusion assessment and lymph node identification with many new applications currently being proposed and developed. While imaging hardware and software have significantly progressed in recent times, suitable NIR-fluorophores remain a limiting factor. In this report, we describe the design, synthesis, photophysical characterization andin?vivoimaging assessment of new PEGylated NIR-fluorophores based on the BF2-azadipyrromethene fluorophore class. The synthetic route includes PEGylation as the final step, thereby allowing routine access to derivatives substituted with different molecular weights of PEG. Absorption and emission wavelength maxima in PBS lie at 690 and 720?nm respectively with quantum yields over 12%. They show excellent photostability and no light induced singlet oxygen production. A time-course of NIR-fluorescence imaging, post i.v. administration, in BALB/c mice showed a rapid and preferential accumulation in the renal excretion pathway within 20?min, indicative of potential clinical usage for intraoperative identification of vial structures along this pathway. Assessment with clinical imaging equipment showed the NIR-AZA fluorophores to be wavelength compatible and brighter than currently used methylene blue (MB), and that they have the ability to be imaged simultaneously with indocyanine green (ICG) offering a potential for dual colour clinical imaging.
机译：利用近红外荧光的临床成像越来越多地作为复杂外科手术过程中决策过程的术中助剂。现有用途包括灌注评估和淋巴结识别，具有当前正在提出和开发的许多新应用程序。在近期成像硬件和软件显着进行，而合适的NIR荧光团仍然是一个限制因素。在本报告中，我们描述了基于BF2-己二维硫甲烯荧光团类的新型聚乙二醇化NIR-荧光团的设计，合成，光学表征和蛋白的设计，合成，光物理表征。合成途径包括作为最终步骤的聚乙二醇化，从而允许常规接入被用不同分子量的PEG取代的衍生物。 PBS中的吸收和发射波长最大值分别在690和720℃下，量子产量超过12％。它们显示出优异的光稳定性，无光引起的单线氧产生。 NIR-荧光成像的时间过程，柱I.v.施用，在BALB / C小鼠中，在20？min内呈肾排泄途径的快速和优先积累，这表明潜在的临床用途，用于沿着该途径术中的小瓶结构的术语鉴定。与临床成像设备的评估显示NIR-AZA荧光团比目前使用的亚甲基蓝（MB）兼容，并且它们具有与吲哚菁绿（ICG）同时成像的能力，该临床成像具有潜力。 。

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