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Development of 99mTc-labeled melanin-targeted probes for SPECT imaging of melanoma

文献类型：期刊论文

作者Tao, Ji3,4; Cao, Rui6; Lei, Zhe1; Wang, Xiao1; Luo, Renli4; Zhou, Yuanyuan4; Li, Yanlin3,4; Xu, Xiaoping1; Liu, Xiaosheng1; Qu, Chunrong4
刊名EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING
出版日期2025-04-21
页码14
关键词Melanoma Melanin (99m)Technetium SPECT Imaging probe
ISSN号1619-7070
DOI10.1007/s00259-025-07268-1
英文摘要Purpose: Melanoma is a highly aggressive skin cancer with poor prognosis, highlighting the need for early detection. This study aims to develop a Tc-99m-labeled single photon emission computed tomography (SPECT) probe targeting melanin to improve melanoma detection with enhanced specificity and cost-effectiveness. Methods: Six potential Tc-99m-labeled probes were synthesized by conjugating small molecules with nitrogen-rich fatty chains or cyclic structures to Tc-99m. These Tc-99m-complexes were then assessed in vitro for their lipid-water partition coefficient, radiochemical stability, and cellular uptake. In vivo studies included biodistribution, SPECT/CT imaging, pharmacokinetics, stability and biocompatibility studies were conducted in various mouse models. Results: These six probes exhibited high radiolabeling yields (> 95%) and radiochemical purities (> 95%). In vitro cell uptake and blocking experiments demonstrated their binding capability and specificity for melanin. Among these probes, Tc-99m-SMIC-4006 displayed the highest tumor uptake (5.18 +/- 1.55%ID/g at 1 h) and significantly higher uptake in B16F10 xenografts compared to non-melanotic A375 xenografts (p < 0.01). The initial tumor-to-blood ratio for Tc-99m-SMIC-4006 was 4.30 +/- 0.63 at 1 h, increasing to 10.27 +/- 5.13 at 6 h. Importantly, SPECT/CT imaging of Tc-99m-SMIC-4006 clearly delineated B16F10 tumor regions with high contrast, while A375 xenografts showed minimal uptake. Conclusion: Tc-99m-SMIC-4006 is a promising SPECT probe for melanoma imaging, offering high tumor specificity, excellent uptake, and ideal tumor-to-background contrast, with strong potential for clinical application.
WOS关键词MALIGNANT-MELANOMA ; PIGMENTED MELANOMA ; METASTASES ; TRACER ; BIODISTRIBUTION ; DETECT ; TUMORS ; MICE
资助项目Shanghai Municipal Science and Technology Major Project ; National Natural Science Foundation of China[U2267221] ; State Key Laboratory of Drug Research[SIMM0120231004] ; Gansu Science and Technology Major Project[23ZDFA014] ; Ningbo Major Research and Development Plan Project[2024Z214] ; Natural Science Foundation of Shanghai[24ZR1477300] ; Shandong Laboratory Program[SYS202205] ; [2023SHZDZX02]
WOS研究方向Radiology, Nuclear Medicine & Medical Imaging
语种英语
WOS记录号WOS:001471820500001
出版者SPRINGER
源URL[http://119.78.100.183/handle/2S10ELR8/317443]  
专题新药研究国家重点实验室
通讯作者Song, Shaoli; Tian, Mei; Cheng, Zhen
作者单位1.Fudan Univ, Shanghai Canc Ctr, Dept Nucl Med, Shanghai, Peoples R China
2.Univ Chinese Acad Sci, Sch Pharm, Beijing, Peoples R China
3.Fudan Univ, Human Phenome Inst, Shanghai, Peoples R China
4.Chinese Acad Sci, Shanghai Inst Mat Med, Mol Imaging Ctr, State Key Lab Drug Res, Shanghai, Peoples R China
5.Bohai Rim Adv Res Inst Drug Discovery, Shandong Lab Yantai Drug Discovery, Yantai, Peoples R China
6.Shanghai Jiao Tong Univ, Shanghai Peoples Hosp 6, Sch Med, Dept Nucl Med, Shanghai, Peoples R China
7.Zhejiang Univ, PET Ctr,Sch Med, Affiliated Hosp 2, Dept Nucl Med, Hangzhou, Peoples R China
8.Fudan Univ, Huashan Hosp, PET Ctr, Dept Nucl Med, Shanghai, Peoples R China
推荐引用方式
GB/T 7714		 Tao, Ji,Cao, Rui,Lei, Zhe,et al. Development of 99mTc-labeled melanin-targeted probes for SPECT imaging of melanoma[J]. EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,2025:14.
APA Tao, Ji.,Cao, Rui.,Lei, Zhe.,Wang, Xiao.,Luo, Renli.,...&Cheng, Zhen.(2025).Development of 99mTc-labeled melanin-targeted probes for SPECT imaging of melanoma.EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING,14.
MLA Tao, Ji,et al."Development of 99mTc-labeled melanin-targeted probes for SPECT imaging of melanoma".EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING (2025):14.

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来源：上海药物研究所

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