| 朱家序,蒋亚群,潘芯,李崇佼,雷萍,何勇.基于七甲川菁构建并初步评估双模态PET/近红外荧光探针[J].中国医学影像技术,2023,39(5):646~650 |
| 基于七甲川菁构建并初步评估双模态PET/近红外荧光探针 |
| Construction and preliminary evaluation on dual-modal PET/ near-infrared fluorescent probe with heptamethine |
| 投稿时间：2023-01-06 修订日期：2023-02-17 |
| DOI：10.13929/j.issn.1003-3289.2023.05.002 |
| 中文关键词: 分子探针技术 七甲川菁 镓 正电子发射断层显像 谱学,近红外线 |
| 英文关键词:molecular probe techniques heptamethine gallium positron-emission tomography spectroscopy, near-infrared |
| 基金项目:国家自然科学基金(82171986)。 |
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| 中文摘要: |
| 目的 基于七甲川菁染料MHI148构建新型PET/近红外荧光(NIRF)双模态探针,并初步评估其用于肿瘤模型小鼠成像的能力。方法 采用双功能螯合剂DOTA修饰MHI148构建MHI148-DOTA,对其光物理、光热性能进行表征;以放射性核素68Ga标记MHI148-DOTA,合成探针68Ga-MHI148,测定其放射化学纯度及稳定性。建立小鼠乳腺癌4T1及人脑胶质母细胞瘤U-87MG皮下瘤模型,以68Ga-MHI148探针对其进行小动物PET显像,观察成像效果及该探针在小鼠体内的生物分布。结果 MHI148-DOTA光物理及光热性能优异。以之构建的探针68Ga-MHI148放射化学纯度＞99%,稳定性良好;小动物PET成像可清晰显示肿瘤,肿瘤摄取随时间延长而逐渐升高,6 h时U-87MG及4T1肿瘤/肌肉摄取比值分别为4.55±0.20及8.08±2.26;68Ga-MHI148小鼠体内主要分布于血液、肺、肝及肾脏。结论 成功构建的双模态68Ga-MHI148探针标记简单、稳定性良好,肿瘤靶向潜力较好,并可在近红外激光照射下抑制小鼠肿瘤细胞生长。 |
| 英文摘要: |
| Objective To construct a novel dual-modal PET/near-infrared fluorescence (NIRF) probe based on heptamethine dye MHI148, and to preliminarily evaluate the imaging capability of this probe for tumor model mice. Methods MHI148 was modified with a bifunctional chelating agent (i.e. DOTA) to synthesize MHI148-DOTA. The photophysical and photothermal properties of MHI148-DOTA were characterized. Then probe 68Ga-MHI148 was prepared by chelating radionuclide 68Ga with MHI148-DOTA, and its radiochemical purity and stability were analyzed. Mice models of breast cancer 4T1 and human glioblastoma U-87MG subcutaneous tumor were established to evaluate the effect of 68Ga-MHI148 probe on micro-PET imaging and its biodistribution in mice. Results MHI148-DOTA had excellent photophysical and photothermal properties. The probe 68Ga-MHI148 was successfully constructed with radiochemical purity over 99% and good stability. Micro-PET scan could clearly show the subcutaneous tumors of mice, and tumor uptake gradually increased with the extension of time. The U-87MG and 4T1 tumor/muscle uptake ratios at 6 h was 4.55±0.20 and 8.08±2.26, respectively. 68Ga-MHI148 mainly distributed in blood, lung, liver and kidney of mice. Conclusion A dual-modal 68Ga-MHI148 probe was successfully constructed, which was simple to label and stable with good tumor targeting potential, and might inhibit the growth of tumor cells under near-infrared laser in mice. |
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