In vivo imaging of β-galactosidase stimulated activity in hepatocellular carcinoma using ligand-targeted fluorescent probe
Abstract
Development of targeted, selective, and noninvasive fluorescent probes for in vivo visualization of tumor-associated overexpressed enzymes are highly anticipated for cancer diagnosis and therapy. Herein, we developed a noninvasive fluorescent probe (DCDHF-βgal) for the sensitive detection, and in vivo visualization of β-galactosidase in hepatocyte HepG2 cells and its xenograft model. As a model system for in vivo targeted imaging, DCDHF-βgal possessing galactose unit selectively target hepatocyte and monitor the β-galactosidase activity with deep tissue penetration, and low background interference. DCDHF-βgal was activated by intracellular β-galactosidases as the driving force for the release of NIR fluorophore, thereby exhibiting ratiometric optical response. Initial fluorescence emission measured at 615 nm was changed to fluorescence at 665 nm upon activation of DCDHF-βgal with β-galactosidase. Ratiometric fluorescence detection of β-galactosidase was also observed in hepatocellular carcinoma cells and tumor xenograft. The noninvasive in vivo optical imaging facilitated by targeted and enzyme-activated imaging agent would be useful in various biomedical and diagnostic applications.
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Hyaluronidase, γ-Glutamyltranspeptidase, prostate-specific antigen, Trysin, β-galactosidase, Azoreductase, etc. are also used in enzyme-stimulated response smart nano-delivery systems.
“In addition, hyaluronidase, γ-Glutamyltranspeptidase, prostate-specific antigen, Trysin, β-galactosidase, Azoreductase, etc. are also used in enzyme-stimulated response smart nano-delivery systems.157–162”
From Smart nanoparticles for cancer therapy (2023) · cites this paper as [161]
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- Authors
- Kim, E.-J., Kumar, R., Sharma, A., Yoon, B., Kim, H. M., Lee, H., Hong, K. S., & Kim, J. S.
- Affiliations
- Korea Basic Science Institute (KR)
- Korea University (KR)
- Corresponding author
- Hong, Kwan Soo
- Kim, Jong Seung
- Venue
- Biomaterials
- Publisher
- Elsevier BV
- Published
- 2017-04
- Volume
- 122
- Pages
- 83-90
- ISSN
- 0142-9612 (ISSN-L)
- OpenAlex
- W2579265611
- Cited by
- 129
- References
- 55
- Citations by year
- 2026: 5 · 2025: 8 · 2024: 13 · 2023: 8 · 2022: 13 · 2021: 20 · 2020: 22 · 2019: 13 · 2018: 19 · 2017: 8
- FWCI
- 8.36
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Biomaterials (publishedVersion)
- PubMed (publishedVersion)
- KRIBB Repository (submittedVersion)
- Funders
- National Research Foundation of Korea
- National Research Council of Science and Technology
- Ministry of Science, ICT and Future Planning
- KAIST Creative Research Initiatives (2009–0081566)
- Korea Basic Science Institute (CRC-15-02-KRIBB, D36401)
- Topics
- Physical Sciences › Chemistry › Spectroscopy › Molecular Sensors and Ion Detection
- Physical Sciences › Engineering › Biomedical Engineering › Nanoplatforms for cancer theranostics
- Physical Sciences › Materials Science › Materials Chemistry › Luminescence and Fluorescent Materials
- Keywords
- beta-galactosidase, hepatocellular carcinoma, fluorescent probes, ratiometric fluorescence, tumor xenografts, HepG2 cells, in vivo optical imaging, deep tissue penetration
- MeSH terms
- Animals, beta-Galactosidase, Enzyme Activation, Fluorescent Dyes, Galactose, Carcinoma, Hepatocellular, Humans, Ligands, Male, Mice, Inbred BALB C, Mice, Nude, Microscopy, Fluorescence, Sensitivity and Specificity, Biomarkers, Tumor, Reproducibility of Results, Molecular Probe Techniques, Mice, Hep G2 Cells, Molecular Imaging
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