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一种新型近红外 EGFR 靶向探针,用于临床前小鼠模型中转移性淋巴结的成像。

A novel near-infrared EGFR targeting probe for metastatic lymph node imaging in preclinical mouse models.

机构信息

Department of Oral and Maxillofacial Surgery, Affiliated Hospital of Medical School, Nanjing Stomatological Hospital, Nanjing University, Nanjing, China.

Department of Biomedical Engineering, College of Engineering and Applied Sciences, Nanjing University, Nanjing, China.

出版信息

J Nanobiotechnology. 2023 Sep 22;21(1):342. doi: 10.1186/s12951-023-02101-z.

DOI:10.1186/s12951-023-02101-z
PMID:37736720
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC10514992/
Abstract

For the treatment of patients with oral squamous cell carcinoma (OSCC), the imaging of cervical lymph nodes and the evaluation of metastastic progression are of great significance. In recent years, the development of new non-radioactive lymph node tracers has been an area of intense research. Here, we report the synthesis, good biocompatibility, and in vivo evaluation of a new small molecule near-infrared (NIR) fluorescence probe by the conjugation of Lapatinib to S0456 (LP-S). We show that like Lapatinib, LP-S binds to the epidermal growth factor receptor (EGFR) resulting in high quality fluorescence imaging of metastatic lymph nodes in OSCC mouse models. After local injection of LP-S into the tumor, the lymphatic drainage pathway and lymph nodes can be clearly identified by NIR fluorescence imaging. Further, the LP-S probe shows higher contrast and longer retention in metastatic lymph nodes, allowing them to be differentiated from normal lymph nodes, and affording a new choice for fluorescence-guided surgery. Scheme. Chemical synthesis and application of EGFR targeting probe LP-S for imaging of metastatic lymph nodes (mLNs) in OSCC.

摘要

对于口腔鳞状细胞癌(OSCC)患者的治疗,颈部淋巴结的影像学检查和转移进展的评估具有重要意义。近年来,新型非放射性淋巴结示踪剂的发展一直是研究的热点。在这里,我们通过将拉帕替尼与 S0456(LP-S)偶联,报道了一种新的小分子近红外(NIR)荧光探针的合成、良好的生物相容性及其体内评估。我们表明,与拉帕替尼一样,LP-S 与表皮生长因子受体(EGFR)结合,导致 OSCC 小鼠模型中转移性淋巴结的高质量荧光成像。将 LP-S 局部注射到肿瘤中后,通过近红外荧光成像可以清楚地识别淋巴管引流途径和淋巴结。此外,LP-S 探针在转移性淋巴结中显示出更高的对比度和更长的保留时间,使其能够与正常淋巴结区分开来,并为荧光引导手术提供了新的选择。方案。用于 OSCC 中转移性淋巴结(mLNs)成像的 EGFR 靶向探针 LP-S 的化学合成及应用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/9bbbac8346f5/12951_2023_2101_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/c6d5913db242/12951_2023_2101_Figa_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/19c644d1bb78/12951_2023_2101_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/6ff90ecf5ff9/12951_2023_2101_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/20a084059755/12951_2023_2101_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/14ba9e0f9c70/12951_2023_2101_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/0815360d068f/12951_2023_2101_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/b1085260b351/12951_2023_2101_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/9bbbac8346f5/12951_2023_2101_Fig7_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/c6d5913db242/12951_2023_2101_Figa_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/19c644d1bb78/12951_2023_2101_Fig1_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/6ff90ecf5ff9/12951_2023_2101_Fig2_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/20a084059755/12951_2023_2101_Fig3_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/14ba9e0f9c70/12951_2023_2101_Fig4_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/0815360d068f/12951_2023_2101_Fig5_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/b1085260b351/12951_2023_2101_Fig6_HTML.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/7802/10514992/9bbbac8346f5/12951_2023_2101_Fig7_HTML.jpg

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