<br>用于高对比度肝细胞癌成像和分化的 GABAA 受体特异性碳点,Advanced Functional Materials

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用于高对比度肝细胞癌成像和分化的 GABAA 受体特异性碳点
Advanced Functional Materials ( IF 18.5 ) Pub Date : 2024-04-15 , DOI: 10.1002/adfm.202401744
Yifei Guo ₁ , Yuanqiang Sun ₁ , Xin Geng ₁ , Junli Wang ₁ , Jingyu Hu ₁ , Rong‐Bin Song _{1,

2} , Ran Yang ₁ , Lingbo Qu ₁ , Zhaohui Li _{1,

3}

Affiliation

从科学研究和临床应用来看，用于肝细胞癌（HCC）成像和分化的靶向荧光探针是非常需要的。然而，目前的靶向荧光探针大多聚焦于肝细胞癌化引起的细胞内微环境的变化，导致荧光强度改变，但由于缺乏进一步提高准确性的稳健参数而无法产生空间分化。在此，该研究开发了一种新的荧光碳点（CTF-CD），可以靶向细胞膜上过度表达的 GABA _A受体（GABA _A R），从而对 HCC 和分化进行准确、高对比度的成像。 CTF-CD 和典型受体结合配体之间的竞争反应揭示了它们对 GABA _A R 印防己毒素结合位点的亲和力。基于这种 GABA _A R 靶向能力，通过照亮 HCC 细胞的膜，沿着与正常肝细胞和其他癌细胞的细胞内荧光有很大差异。此外，CTF-CD 还被用于可视化抗癌药物诱导的 HCC 细胞膜变化和 HCC 组织中的荧光成像。该工作将荧光探针的靶向对象从细胞内微环境扩展到膜蛋白，为HCC的成像和分化增加了新的维度。

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GABAA Receptor-Specific Carbon Dots for High-Contrast Hepatocellular Carcinoma Imaging and Differentiation

Targeted fluorescence probes for imaging and differentiation of hepatocellular carcinoma (HCC) are highly desirable from its scientific research and clinical applications. However, most of the current targeted fluorescence probes focus on the variation of intracellular microenvironment caused by the cancerization of hepatocyte, which causes a fluorescence intensity alteration but fails to produce a spatial differentiation due to the lack of robust parameters for further improving accuracy. Herein, the study develops a new fluorescent carbon dot (CTF-CDs) that can target the overexpressed GABA_A receptor (GABA_AR) on cell membrane for accurate and high-contrast imaging of HCC and differentiation. The competition response between CTF-CDs and typical receptor-binding ligands reveals their affinity toward the picrotoxin-binding site of GABA_AR. Based on this GABA_AR-targeting ability, accurate imaging of HCC cells is realized by lighting their membranes, along with a big difference from the intracellular fluorescence of normal liver cells and other cancer cells. In addition, the CTF-CDs have also been used to visualize the anticancer drug-induced variations on HCC cell membrane and fluorescent imaging in HCC tissue. This work extends the targeting object of fluorescence probes from intracellular microenvironment to membrane protein, adding a new dimension to the imaging and differentiation of HCC.

更新日期：2024-04-15

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