A series of human carbonic anhydrase (hCA) IX inhibitors conjugated to various near-infrared fluorescent dyes was synthesized with the aim of imaging hypoxia-induced hCA IX expression in tumor cells in vitro, ex vivo and in vivo. The resulting compounds were profiled for inhibition of transmembrane hCA IX showing a range of potencies from 7.5 to 116 nM and up to 50-fold selectivity over the cytosolic form hCA II. Some of the compounds also showed inhibition selectivity for other transmembrane forms hCA XII and XIV as well. Compounds incubated in vitro with HeLa cells cultured under normoxic and hypoxic conditions detected upregulation of hCA IX under hypoxia by fluorescence microscopy. A pilot in vivo study in HT-29 tumor bearing mice showed significant accumulation of a fluorescent acetazolamide derivative in tumor tissue with little accumulation in other tissues. Approximately 10% of injected dose was non-invasively quantified in tumors by fluorescence molecular tomography (FMT), demonstrating the promise of these new compounds for quantitative imaging of hCA IX upregulation in live animals.
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http://dx.doi.org/10.1016/j.bmcl.2011.10.058 | DOI Listing |
Anal Chem
January 2025
School of Life Sciences, Key Laboratory of Space Bioscience & Biotechnology, Northwestern Polytechnical University, Xi'an 710072, China.
Lymphoma is a malignant cancer characterized by a rapidly increasing incidence, complex etiology, and lack of obvious early symptoms. Efficient theranostics of lymphoma is of great significance in improving patient outcomes, empowering informed decision-making, and driving medical innovation. Herein, we developed a multifunctional nanoplatform for precise optical imaging and therapy of lymphoma based on a new photosensitizer (1-oxo-1-benzoo[de]anthracene-2,3-dicarbonitrile-triphenylamine (OBADC-TPA)).
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January 2025
Faculty of Food Science and Engineering, Kunming University of Science and Technology, Kunming 650500, China.
The use of biomass feedstocks for producing high-value-added chemicals is gaining significant attention in the academic community. In this study, near-infrared carbon dots (NIR-CDs) with antimicrobial and bioimaging functions were prepared from branches and leaves using a novel green synthesis approach. The spectral properties of the synthesized NIR-CDs were characterized by ultraviolet-visible (UV-Vis) absorption and fluorescence spectroscopy.
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January 2025
College of Chemistry and Chemical Engineering, Central South University, Changsha 410017, China.
Ratiometric lanthanide coordination polymers (Ln-CPs) are advanced materials that combine the unique optical properties of lanthanide ions (e.g., Eu, Tb, Ce) with the structural flexibility and tunability of coordination polymers.
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January 2025
Department of Hematology, Zhongnan Hospital of Wuhan University, Wuhan University School of Pharmaceutical Sciences, Wuhan 430071, China.
In recent years, the near-infrared (NIR) fluorescence theranostic system has garnered increasing attention for its advantages in the simultaneous diagnosis- and imaging-guided delivery of therapeutic drugs. However, challenges such as strong background fluorescence signals and rapid metabolism have hindered the achievement of sufficient contrast between tumors and surrounding tissues, limiting the system's applicability. This study aims to integrate the pegylation strategy with a tumor microenvironment-responsive approach.
View Article and Find Full Text PDFBiomolecules
January 2025
Department of Chemistry, Molecular Basis of Disease, Petit Science Center, Georgia State University, 100 Piedmont Avenue SE, Atlanta, GA 30303, USA.
Donor acceptor (D-π-A) fluorophores containing a donor unit and an acceptor moiety at each end connected by a conjugated linker gained attention in the last decade due to their conjugated system and ease of tunability. These features make them good candidates for various applications such as bioimaging, photovoltaic devices and nonlinear optical materials. Upon excitation of the D-π-A fluorophore, intramolecular charge transfer (ICT) occurs, and it polarizes the molecule resulting in the 'push-pull' system.
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