Abstract
In this study, we synthesized a novel fluorescein isothiocyanate (FITC)-labeled prostate-specific membrane antigen (PSMA) ligand (PSMA-FITC) via the Fmoc solid-phase synthesis method, and the application value of PSMA-FITC in targeted fluorescence imaging of PSMA-positive prostate cancer was evaluated. The PSMA ligand developed based on the Glu-urea-Lys structure was linked to FITC by aminocaproic acid (Ahx) to obtain PSMA-FITC. The new probe was evaluated in vitro and in vivo. Fluorescence microscopy examination of PSMA-FITC in PSMA(+) LNCaP cells, PSMA(−) PC3 cells, and blocked LNCaP cells showed that the binding of PSMA-FITC with PSMA was target-specific. For in vivo optical imaging, PSMA-FITC exhibited rapid 22Rv1 tumor targeting within 30 min of injection, and the highest tumor-background ratio (TBR) was observed 60 min after injection. The TBR was 3.45 ± 0.31 in the nonblocking group and 0.44 ± 0.13 in the blocking group, which was consistent with the in vitro results. PSMA-FITC is a promising probe and has important reference value for the development of PSMA fluorescent probes. In the future, it can be applied to obtain accurate tumor images for radical prostatectomy.
Highlights
In recent years, optical imaging technology has been widely used in basic biomedical research, clinical diagnosis and treatment in various fields
prostate-specific membrane antigen (PSMA)-fluorescein isothiocyanate (FITC) and LNCaP cells were incubated at 37 °C for 1 h, and confocal fluorescence microscopy imaging was performed
Confocal fluorescence microscopy results indicate that PSMA-FITC can bind to PSMA
Summary
Optical imaging technology has been widely used in basic biomedical research, clinical diagnosis and treatment in various fields. Fluorescent labeling technology, combined with a variety of microscopic imaging techniques, can be used in neurology, oncology, and pharmacy at the cellular and subcellular levels. Biocompatible organic smallmolecule fluorescent dyes have been rapidly developed and gradually used in clinical diagnosis and treatment (Han et al 2017). The combination of ICG with an optical imager can provide fluorescence imaging navigation during surgery to guide the removal of primary and metastatic tumor lesions (Shah et al 2019). FITC, an organic small-molecule fluorescent dye, has a maximum absorption wavelength of 490–495 nm and a maximum emission wavelength of 520–530 nm, emitting bright yellow-green fluorescence. FITC has become one of the most commonly used fluorescein dyes in biomedical research (Hu et al 2020)
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