Correlating molecular character of NIR imaging agents with tissue-specific uptake.
Correlating molecular character of NIR imaging agents with tissue-specific uptake.
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DOI：
10.1021/acs.jmedchem.5b00475
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发表时间：
2015-05-28
影响因子：
7.3
通讯作者：
Henary M
中科院分区：
文献类型：
--
作者：
Owens EA;Hyun H;Tawney JG;Choi HS;Henary M
近红外(NIR)荧光造影剂作为目前发射有害电离辐射的试剂的敏感、经济高效和无害的替代品正在光学成像中出现。开发光谱清晰的近红外荧光团来显示敏感的重要组织，以便在手术切除病变组织时选择性地避免它们，具有重要的意义。在这里，我们报告了五甲基菁荧光团的合成变异和物理化学性质的改变，以促进组织特异性地摄取敏感组织(即内分泌腺)。组织特异性靶向和生物分布研究表明，造影剂在肾上腺和脑垂体腺、胰腺和淋巴结中的定位取决于分子特征。通过引入疏水杂环、烷基和卤素，可以微调疏水性质和偶极矩，以观察生物活性随微小结构变化而发生的扰动。这些近红外造影剂有可能被临床转化为术中成像来描绘微妙的腺体。
Near-infrared (NIR) fluorescent contrast agents are emerging in optical imaging as sensitive, cost-effective, and nonharmful alternatives to current agents that emit harmful ionizing radiation. Developing spectrally distinct NIR fluorophores to visualize sensitive vital tissues to selectively avoid them during surgical resection of diseased tissue is of great significance. Herein, we report the synthetic variation of pentamethine cyanine fluorophores with modifications of physicochemical properties toward prompting tissue-specific uptake into sensitive tissues (i.e., endocrine glands). Tissue-specific targeting and biodistribution studies revealed localization of contrast agents in the adrenal and pituitary glands, pancreas, and lymph nodes with dependence on molecular characteristics. Incorporation of hydrophobic heterocyclic rings, alkyl groups, and halogens allowed a fine-tuning capability to the hydrophobic character and dipole moment for observing perturbation in biological activity in response to minor structural alterations. These NIR contrast agents have potential for clinical translation for intraoperative imaging in the delineation of delicate glands.