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正电子发射断层扫描/近红外荧光双模成像用于靶向肿瘤检测。

PET/NIR Fluorescence Bimodal Imaging for Targeted Tumor Detection.

机构信息

Department of Basic Medicine and Clinical Pharmacy, China Pharmaceutical University, Nanjing 211198, Jiangsu China.

Jiangsu Key Laboratory of Drug Design & Optimization, Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 211100, Jiangsu China.

出版信息

Mol Pharm. 2023 Dec 4;20(12):6262-6271. doi: 10.1021/acs.molpharmaceut.3c00660. Epub 2023 Nov 10.

Abstract

Cancer is one of the greatest threats to human health due to late diagnosis and incomplete resection. The bimodal probe combines positron emission tomography (PET) imaging for noninvasive whole-body scanning with intraoperative near-infrared fluorescence (NIRF) surgical guidance for preoperative tumor detection, tumor resection during surgery, and postoperative monitoring. We developed a new PET/NIRF bimodal imaging agent, [Ga]Ga-DOTA-NPC, covalently coupled to DCDSTCY and DOTA via ethylenediamine and radiolabeled with gallium-68, and investigated it and . The probe was found to be preferential for colon cancer cells due to the organic anion-transporting polypeptide1B3 (OATP1B3). PET/NIRF imaging allowed us to confirm [Ga]Ga-DOTA-NPC as a promising probe for tumor detection, as it provides good biosafety and high-contrast tumor accumulation. Orthotopic and subcutaneous colon tumors were successfully resected under real-time NIRF guidance. [Ga]Ga-DOTA-NPC provides highly sensitive and unlimited tissue-penetrating PET/NIRF imaging, helping to visualize and differentiate tumors from adjacent tissue.

摘要

癌症是对人类健康的最大威胁之一,原因是诊断较晚和切除不完全。双模态探头结合正电子发射断层扫描(PET)进行非侵入性全身扫描,以及术中近红外荧光(NIRF)手术指导,用于术前肿瘤检测、手术期间肿瘤切除和术后监测。我们开发了一种新的 PET/NIRF 双模态成像剂,[Ga]Ga-DOTA-NPC,通过乙二胺与 DCDSTCY 和 DOTA 共价偶联,并进行了放射性标记。研究了它的 。由于有机阴离子转运多肽 1B3(OATP1B3),该探针优先与结肠癌细胞结合。PET/NIRF 成像使我们能够确认 [Ga]Ga-DOTA-NPC 是一种有前途的肿瘤检测探针,因为它具有良好的生物安全性和高对比度的肿瘤积累。在实时 NIRF 引导下成功切除了原位和皮下结肠肿瘤。[Ga]Ga-DOTA-NPC 提供了高灵敏度和无限制的组织穿透性 PET/NIRF 成像,有助于可视化和区分肿瘤与相邻组织。

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