1. β-Galactosidase-activated near-infrared AIEgen for ovarian cancer imaging in vivo.
- Author
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Xu, Lingling, Gao, Hang, Deng, Yu, Liu, Xiaoyang, Zhan, Wenjun, Sun, Xianbao, Xu, Jing-Juan, and Liang, Gaolin
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OVARIAN cancer , *GALACTOSIDASES , *DETECTION limit , *MOLECULAR docking , *OVARIAN tumors , *CELL imaging - Abstract
Near-infrared (NIR) aggregation induced-emission luminogens (AIEgens) circumvent the noisome aggregation-caused quenching (ACQ) effect in physiological milieu, thus holding high promise for real-time and sensitive imaging of biomarkers in vivo. β-Galactosidase (β-Gal) is a biomarker for primary ovarian carcinoma, but current AIEgens for β-Gal sensing display emissions in the visible region and have not been applied in vivo. We herein propose an NIR AIEgen QM-TPA-Gal and applied it for imaging β-Gal activity in vitro and in ovarian tumor model. After being internalized by ovarian cancer cells (e.g. , SKOV3), the hydrophilic nonfluorescent QM-TPA-Gal undergoes hydrolyzation by β-Gal to yield hydrophobic QM-TPA-OH , which subsequently aggregates into nanoparticles to turn NIR fluorescence "on" through the AIE mechanism. In vitro experimental results indicate that QM-TPA-Gal has a sensitive and selective response to β-Gal with a limit of detection (LOD) of 0.21 U/mL. Molecular docking simulation confirms that QM-TPA-Gal has a good binding ability with β-Gal to allow efficient hydrolysis. Furthermore, QM-TPA-Gal is successfully applied for β-Gal imaging in SKOV3 cell and SKOV3-bearing living mouse models. It is anticipated that QM-TPA-Gal could be applied for early diagnosis of ovarian cancers or other β-Gal-associated diseases in near future. • A near-infrared AIEgen QM-TPA-Gal was designed and synthesized for the first time. • QM-TPA-Gal presented highly sensitive and selective response to β-Gal in vitro, with a limit of detection (LOD) of 0.21 U/mL. • QM-TPA-Gal was successfully applied for β-Gal imaging in vivo with superior sensitivity, specificity, and biosafety. [ABSTRACT FROM AUTHOR]
- Published
- 2024
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