Tang Yongjia, Xu Haoran, Dai Yaxue, Wang Fang, Huang Wenjing, Liu Peifei, Gu Yueqing
State Key Laboratory of Natural Medicine, Department of Biomedical Engineering, School of Engineering, China Pharmaceutical University, No. 24 Tongjia Lane, Gulou District, Nanjing 211198, China.
J Mater Chem B. 2021 Jun 2;9(22):4577-4586. doi: 10.1039/d1tb00408e.
Hepatocellular carcinoma (HCC) is one of the most common malignant tumors with limited diagnosis. Mesenchymal epithelial transition factor (c-Met) has become a hot target for cancer diagnosis and therapy, which is overexpressed in HCC. In this study, we labeled a novel c-Met targeting peptide YQ-M3 with a near-infrared fluorescent dye MPA and a radionuclide technetium-99m for HCC detection. YQ-M3-MPA showed high affinity for c-Met positive HepG2 tumor in vitro and higher tumor uptake and higher T/N ratio than GE137-MPA (a positive tracer for c-Met) in HepG2 tumor-bearing mice in vivo by fluorescence imaging. In addition, 99mTc-HYNIC-YQ-M3 also showed significant tumor uptake in vivo through SPECT imaging. These results indicated that c-Met positive tumors were successfully detected via fluorescence and SPECT imaging using YQ-M3-MPA and 99mTc-HYNIC-YQ-M3, respectively, and further suggested that YQ-M3-MPA and 99mTc-HYNIC-YQ-M3 have some possibly potential clinical applications for HCC diagnosis.
肝细胞癌（HCC）是诊断手段有限的最常见恶性肿瘤之一。间充质上皮转化因子（c-Met）已成为癌症诊断和治疗的热门靶点，其在HCC中过表达。在本研究中，我们用近红外荧光染料MPA和放射性核素锝-99m标记了一种新型的靶向c-Met肽YQ-M3用于HCC检测。YQ-M3-MPA在体外对c-Met阳性的HepG2肿瘤显示出高亲和力，并且通过荧光成像在体内荷HepG2肿瘤小鼠中比GE137-MPA（一种c-Met阳性示踪剂）具有更高的肿瘤摄取和更高的T/N比值。此外，99mTc-HYNIC-YQ-M3通过SPECT成像在体内也显示出显著的肿瘤摄取。这些结果表明，分别使用YQ-M3-MPA和99mTc-HYNIC-YQ-M3通过荧光和SPECT成像成功检测到了c-Met阳性肿瘤，并进一步表明YQ-M3-MPA和99mTc-HYNIC-YQ-M3在HCC诊断方面具有一些潜在的临床应用价值。
