Sun Ke-Xin, Yu Zhen-Peng, Luo Jia-Lun, Yu Zhi-Qiang, Zhu Hong, Wu Tao, Dai Peng-Fei, Si Hongwei
Department of Nuclear Medicine, The First Affiliated Hospital of Anhui Medical University, Hefei, Anhui 230022, China.
Department of Respiratory and Critical Care Medicine, The First Affiliated Hospital of Anhui Medical University, Hefei, Anhui 230022, China.
Bioorg Med Chem. 2025 Aug 1;125:118221. doi: 10.1016/j.bmc.2025.118221. Epub 2025 Apr 30.
The precise diagnosis of HCC is confronted with severe challenges due to the tumor heterogeneity and insidious symptoms of hepatocellular carcinoma (HCC), and meanwhile the limitations of positron emission tomography (PET) with traditional 2-deoxy-2-[fluorine-18] fluoro-d-glucose (F-FDG) tracer. Given that angiotensin II type 1 receptor (AT1R) is significantly upregulated in HCC and closely related to its progression, we have developed a novel Ga-radiolabeled compound, Ga-DOTA-AngII (Ga-DOTA-GGDRVYIHPF), and evaluated its HCC detection capability. Ga-DOTA-AngII demonstrated acceptable stability in both human plasma and phosphate buffered saline. In vivo imaging and in vitro biodistribution analysis in tumor-bearing mice showed that Ga-DOTA-AngII demonstrate a high tumor uptake, and the tumor tissue exhibited rapid uptake. In brief, this radiotracer possesses a promising potency for imaging the expression of AT1R for further clinical application.
由于肝细胞癌（HCC）的肿瘤异质性和隐匿症状，以及正电子发射断层扫描（PET）使用传统的2-脱氧-2-[氟-18]氟-D-葡萄糖（F-FDG）示踪剂的局限性，HCC的精确诊断面临严峻挑战。鉴于血管紧张素II 1型受体（AT1R）在HCC中显著上调且与其进展密切相关，我们开发了一种新型的镓标记化合物，Ga-DOTA-血管紧张素II（Ga-DOTA-GGDRVYIHPF），并评估了其检测HCC的能力。Ga-DOTA-血管紧张素II在人血浆和磷酸盐缓冲盐水中均表现出可接受的稳定性。在荷瘤小鼠体内成像和体外生物分布分析表明，Ga-DOTA-血管紧张素II具有高肿瘤摄取，且肿瘤组织摄取迅速。简而言之，这种放射性示踪剂在成像AT1R表达方面具有良好的应用前景，可进一步用于临床。
