18F-硼氨酸细胞摄取机制研究

doi:10.3969/j.issn.1006-7795.2021.01.003

首都医科大学学报 ›› 2021, Vol. 42 ›› Issue (1): 15-20.doi: 10.3969/j.issn.1006-7795.2021.01.003

¹⁸F-硼氨酸细胞摄取机制研究

李詝¹, 李囡¹, 刘志博², 杨志^1*

1.北京大学肿瘤医院暨北京市肿瘤防治研究所核医学科恶性肿瘤发病机制及转化研究教育部重点实验室,北京 100142;
2.北京大学化学与分子工程学院,北京 100871

收稿日期:2020-11-30 出版日期:2021-02-21 发布日期:2021-02-02
基金资助:
国家自然科学基金(81871386)。

Research on glycine cell uptake mechanisms

Li Zhu¹, Li Nan¹, Liu Zhibo², Yang Zhi^1*

1. Key Laboratory of Carcinogenesis and Translational Research (Ministry of Education/Beijing), Department of Nuclear Medicine, Peking University Cancer Hospital & Institute, Beijing 100142, China;
2. College of Chemistry and Molecular Engineering, Peking University, Beijing 100871, China

Received:2020-11-30 Online:2021-02-21 Published:2021-02-02
Contact: ^*E-mail:pekyz@163.com
Supported by:
National Natural Science Foundation of China(81871386).

摘要/Abstract

摘要： 目的本研究采用半自动方法对¹⁸F标记的苯丙硼氨酸(¹⁸F-BF₃-Phe)进行标记,通过系统的细胞实验,建立¹⁸F-硼氨酸细胞摄取与L型氨基酸转运体-1(large-neutral amino acid transporter-1,LAT-1)表达的定量关系,初步阐述¹⁸F-硼氨酸在癌细胞中的摄取机制。方法制备LAT-1转染细胞,用不同浓度LAT-1转染细胞进行¹⁸F-BF₃-Phe放射性摄取实验。培养PC9、 BXPC3、PC3、HEPG2细胞,进行不同时间点¹⁸F-BF₃-Phe放射性摄取实验。结果 LAT-1转染细胞放射性摄取实验中,细胞的放射性摄取随着LAT-1转染细胞比例的增加而逐渐增加,基本呈线性正相关。¹⁸F-BF₃-Phe在PC9、BXPC3、PC3、HEPG2 4种肿瘤细胞中均有摄取,并随时间推移呈逐渐增加趋势。其中PC9及BXPC3细胞对¹⁸F-BF₃-Phe的摄取更为显著。结论通过LAT-1转染细胞摄取实验明确了¹⁸F-BF₃-Phe摄取与LAT-1转运体表达之间呈正相关,为进一步的体内实验提供了重要的理论依据。¹⁸F-BF₃-Phe在多种肿瘤细胞中均有高摄取,显示该探针在肿瘤显像方面进行临床转化的良好前景。

关键词: 硼氨酸, 氨基酸转运体, 肿瘤, 放射性标记

Abstract: Objective To study the quantitative relationship between the uptake of ¹⁸F-BF₃-Phe and the expression of large-neutral amino acid transporter-1(LAT-1), and to elucidate the uptake mechanism of ¹⁸F-BF₃-Phe in cancer cells. Methods ¹⁸F-BF₃-Phe uptake experiments was performed with different levels of LAT-1 transfected cells. The ¹⁸F-BF₃-Phe uptake by PC9, BXPC3, PC3, HEPG2 cells was assayed at different time points. Results The uptake of ¹⁸F-BF₃-Phe in LAT-1 transfected cells was linearly correlated with the increase in the proportion of LAT-1 transfection. The uptake of ¹⁸F-BF₃-Phe in PC9, BXPC3, PC3, and HepG2 tumor cells showed an increasing trend over time. The uptake of ¹⁸F-BF₃-Phe by PC9 and BXPC3 cells was significantly higher than the other two cell lines. Conclusion The uptake of ¹⁸F-BF₃-Phe by LAT-1 transfected cells was positively correlated with the expression of LAT-1 transporter, which provided an important theoretical basis for further in vivo experiments. ¹⁸F-BF₃-Phe was highly uptaken by a variety of tumor cells, showing potential in clinical translation of this probe in tumor imaging.

Key words: boramino acid, amino acid transporter, tumor, radiolabelling

中图分类号:

R817.1

李詝, 李囡, 刘志博, 杨志. ¹⁸F-硼氨酸细胞摄取机制研究[J]. 首都医科大学学报, 2021, 42(1): 15-20.

Li Zhu, Li Nan, Liu Zhibo, Yang Zhi. Research on glycine cell uptake mechanisms[J]. Journal of Capital Medical University, 2021, 42(1): 15-20.

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¹⁸F-硼氨酸细胞摄取机制研究

Research on glycine cell uptake mechanisms

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