Department of Nuclear Medicine, The First Affiliated Hospital of Chongqing Medical University, Chongqing, 400016, P. R. China.
Department of Nuclear Medicine, Shanghai Sixth People's Hospital, Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, 200235, P. R. China.
J Nanobiotechnology. 2024 Oct 10;22(1):614. doi: 10.1186/s12951-024-02879-6.
Hepatocellular cancer (HCC) remained a life-threatening carcinoma. Agents for HCC imaging and therapy were expected to possess different intratumoral retention time. To construct an agent with different intratumoral retention time when applied for tumor imaging or therapy remained great values. A lasialoglycoprotein receptor (ASGPR) targeted lactobionic acid derivative (LABO) was constructed for fluorescent imaging and photodynamic therapy of HCC. F labeled LABO (F-LABO) was developed for PET imaging of HCC. LABO and F-LABO showed similar molecular structure. LABO exhibited characteristic of viscosity and concentration-induced intratumoral in-situ self-assembly to expand the intratumoral retention. LABO was non-fluorescent at free stage, but emitted NIR fluorescence and generated irradiation-induced ROS after self-assembly for fluorescent imaging and photodynamic therapy. ASGPR specificity of LABO and F-LABO was confirmed using HepG2 cell. Biodistribution and fluorescent imaging confirmed the different tumor retention time of LABO and F-LABO when used for photodynamic therapy and PET imaging. PET imaging and photodynamic therapy were performed on HepG2 tumor bearing mice, which revealed that F-LABO/LABO could specifically accumulated in the HepG2 tumor for tumor location/inhibition. LABO/F-LABO with excellent HCC specificity but different intratumoral behaviors showed great values for the PET/NIR imaging and photodynamic therapy for HCC.
肝细胞癌（HCC）仍然是一种危及生命的癌。用于 HCC 成像和治疗的试剂预计具有不同的肿瘤内保留时间。构建用于肿瘤成像或治疗的具有不同肿瘤内保留时间的试剂仍然具有很大的价值。构建了一种用于 HCC 的荧光成像和光动力治疗的去唾液酸糖蛋白受体（ASGPR）靶向乳糖酸衍生物（LABO）。开发了用于 HCC 的正电子发射断层扫描（PET）成像的 F 标记的 LABO（F-LABO）。LABO 和 F-LABO 具有相似的分子结构。LABO 表现出粘度和浓度诱导的肿瘤内原位自组装的特征，以扩大肿瘤内保留。LABO 在游离状态下是非荧光的，但在自组装后会发出近红外荧光并产生辐射诱导的 ROS，用于荧光成像和光动力治疗。使用 HepG2 细胞证实了 LABO 和 F-LABO 的 ASGPR 特异性。生物分布和荧光成像证实了 LABO 和 F-LABO 在用于光动力治疗和 PET 成像时的不同肿瘤保留时间。在荷 HepG2 肿瘤的小鼠上进行了 PET 成像和光动力治疗，结果表明 F-LABO/LABO 可以特异性地聚集在 HepG2 肿瘤中，用于肿瘤定位/抑制。LABO/F-LABO 具有出色的 HCC 特异性，但具有不同的肿瘤内行为，对于 HCC 的 PET/NIR 成像和光动力治疗具有很大的价值。
