“Crossbreeding” NIR‐II flavchromene for PSMA‐positive prostate cancer detection and image‐guided surgery

Jialiang Huang, Yongkang Yao, Liao Zhang, Chenxu Yan, Zhiqian Guo
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Abstract

Prostate‐specific membrane antigen (PSMA) is known to be overexpressed in prostate cancer (PCa). The development of precise and rapid imaging technologies to monitor PSMA is crucial for early diagnosis and therapy. Fluorescence imaging in the second near‐infrared window (NIR‐II) has emerged as a powerful tool for real‐time tracking and in vivo visualization, offering high sensitivity and resolution. However, there is a lack of stable, bright and easy‐to‐implement NIR‐II fluorescent probes for PSMA targeting. Herein, we presented a PSMA‐targeting NIR‐II fluorescent probe FC‐PSMA based on π‐conjugated crossbreeding dyed strategy that affords high stability, large extinction coefficient, and good brightness. As demonstrated, FC‐PSMA displayed a high fluorescence quantum yield in fetal bovine serum (FBS). Following intravenous injection of FC‐PSMA, the tumor‐to‐normal ratio of fluorescence intensity steadily increased over time, reaching a peak at 48 h (tumor‐to‐leg ratio = 12.16 ± 0.90). This advancement enables precise identification of PC through NIR‐II fluorescence imaging, facilitating high‐performance guidance for prostate cancer resection surgery.

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"杂交 "近红外-II 黄色素用于 PSMA 阳性前列腺癌检测和图像引导手术
众所周知,前列腺特异性膜抗原(PSMA)在前列腺癌(PCa)中过度表达。开发精确、快速的成像技术来监测 PSMA 对早期诊断和治疗至关重要。第二近红外窗口(NIR-II)的荧光成像技术具有高灵敏度和高分辨率,已成为实时跟踪和体内可视化的有力工具。然而,目前还缺乏稳定、明亮且易于实现的用于 PSMA 靶向的 NIR-II 荧光探针。在此,我们提出了一种基于π-共轭杂交染色策略的PSMA靶向近红外-II荧光探针FC-PSMA,它具有高稳定性、大消光系数和良好的亮度。实验证明,FC-PSMA 在胎牛血清(FBS)中具有很高的荧光量子产率。静脉注射 FC-PSMA 后,肿瘤与正常人的荧光强度比值随着时间的推移稳步上升,并在 48 小时后达到峰值(肿瘤与腿的比值 = 12.16 ± 0.90)。这项研究成果可通过近红外-II荧光成像精确识别PC,为前列腺癌切除手术提供高效指导。
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