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Synthesis and characterization of F-18-labeled hydrazinocurcumin derivatives for tumor imaging

机译：用于肿瘤成像的F-18标记的肼酰胺蛋白蛋白衍生物的合成与表征

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摘要

Fluorine-substituted hydrazinocurcumin derivative 1 and its dimethyl-substituted form at the C2 and C6 positions (2) were synthesized and their radiolabeled forms, [F-18]1 and [F-18]2, were evaluated for tumor imaging. In vitro and in vivo metabolism studies showed that the two radioligands were resistant to reductive metabolism, probably due to the presence of a pyrazole ring. In cellular uptake studies, [F-18]1 and [F-18]2 exhibited comparable uptake by human umbilical vascular endothelial cells and rat C6 glioma cells. Inhibition of radioligand uptake to a similar extent by HC and curcumin suggests that these radioligands may share the same binding sites as those for HC and curcumin. Positron emission tomography imaging of C6 glioma xenografted mice acquired 30 and 60 min after radioligand injection showed that [F-18]2 had markedly higher tumor uptake than [F-18]1, which was consistent with biodistribution data (3.20 +/- 0.35% ID per g vs. 0.98 +/- 0.31% ID per g, respectively). However, the two radioligands showed similar levels of tumor-to-background uptake ratio, except for the significantly higher uptake of [F-18]1 by the small intestine, indicating its more rapid clearance. The results of this study will guide further structural modifications of these radioligands to enhance tumor-to-background uptake ratios.
机译：合成C2和C6位置（2）处的氟取代的肼蛋白蛋白蛋白衍生物1及其二甲基取代的形式，并评价其放射性标记的形式，[F-18] 1和[F-18] 2，用于肿瘤成像。体外和体内代谢研究表明，两种放射性配体对还原性代谢耐药，可能是由于吡唑环的存在。在蜂窝摄取性研究中，[F-18] 1和[F-18] 2对人脐血管内皮细胞和大鼠C6胶质瘤细胞的相当摄取。通过HC和姜黄素对放射性剂吸收的抑制在相似程度上表明这些放射性配体可以与HC和姜黄素的相同的结合位点与HC和姜黄素共享相同的结合位点。在放射性配体注射液后获得30和60分钟的C6胶质瘤异种移植小鼠的正电子发射断层摄影成像表明[F-18] 2显着高于[F-18] 1的肿瘤摄取，这与生物分布数据一致（3.20 +/- 0.35每G的％ID与0.98 +/- 0.31％ID，分别为每G）。然而，除了小肠的[F-18] 1显着更高的[F-18] 1，表明其更快的间隙外，两个放射性配体显示出类似的肿瘤到背景吸收比率。本研究的结果将引导这些放射性配体的进一步结构修饰，以增强肿瘤到背景的吸收比率。

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  • 来源
    《RSC Advances》 |2015年第117期|共13页
  • 作者

    Shin Sarah; Koo Hyun-Jung; Lee Iljung; Choe Yearn Seong; Choi Joon Young; Lee Kyung-Han; Kim Byung-Tae;

  • 作者单位

    Sungkyunkwan Univ Sch Med Samsung Med Ctr Dept Nucl Med Seoul 06351 South Korea;

    Sungkyunkwan Univ Sch Med Samsung Med Ctr Dept Nucl Med Seoul 06351 South Korea;

    Sungkyunkwan Univ Sch Med Samsung Med Ctr Dept Nucl Med Seoul 06351 South Korea;

    Sungkyunkwan Univ Sch Med Samsung Med Ctr Dept Nucl Med Seoul 06351 South Korea;

    Sungkyunkwan Univ Sch Med Samsung Med Ctr Dept Nucl Med Seoul 06351 South Korea;

    Sungkyunkwan Univ Sch Med Samsung Med Ctr Dept Nucl Med Seoul 06351 South Korea;

    Sungkyunkwan Univ Sch Med Samsung Med Ctr Dept Nucl Med Seoul 06351 South Korea;

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  • 正文语种 eng
  • 中图分类 化学;
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