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Sulfated polysaccharides from red algae have a variety of biological activities, especially antitumor activities. Matrix metalloproteinase-9 (MMP-9) is a proteolytic metalloenzyme that degrades the central part of the extracellular matrix (ECM) and promotes tumor metastasis. In this research, we have investigated the influence and mechanism of GNP (sulfated polysaccharide from ) on tumor metastasis and MMP-9 expression of human fibrosarcoma (HT1080) cells. The results inflected that the concentration of GNP below 100 μg/mL has no toxicity to HT1080 cells, but showed excellent activity in inhibiting cells migration and invasion. In addition, GNP effectively inhibits the mRNA of MMP-9 and reduces its expression and activity by regulating nuclear factor-kappa B (NF-κB), mitogen-activated protein kinases (MAPK) and mTOR/PI3K/Akt signaling pathways. GNP has great potential as MMP-9 inhibitor and could be developed as a functional food or drug to prevent tumor metastasis.
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http://dx.doi.org/10.3390/foods11152360 | DOI Listing |
Eur J Med Chem
August 2025
Forschungszentrum Jülich GmbH, Institute of Neuroscience and Medicine, Nuclear Chemistry (INM-5), Wilhelm-Johnen-Straße, Jülich, 52428, Germany; University of Cologne, Faculty of Medicine and University Hospital Cologne, Institute of Radiochemistry and Experimental Molecular Imaging, Kerpener Str
Fibroblast activation protein (FAP) is almost exclusively expressed on cancer-associated stromal cells, making it a promising target for tumor imaging by positron emission tomography (PET). While Ga- or Al[F]F-labeled FAP inhibitors (FAPIs) have been characterized in detail, the potential advantages of FAPIs containing a covalently bound F-label remain largely unknown. The aim of the present work was to address this gap by comparing two FAPIs with a covalently bound F-label and the chelator-based radioligand Al[F]F-FAPI-42.
View Article and Find Full Text PDFThe precision of photothermal therapy (PTT) is often hindered by the challenge of achieving selective delivery of thermoplasmonic nanostructures to tumors. Active targeting, which leverages synthetic molecular complexes to address receptors overexpressed by malignant cells, enables such specificity and facilitates the combination of the PTT with other anticancer therapies. In this study, we developed thermoplasmonic nanoconjugates consisting of (i) 20 nm spherical gold nanoparticles (AuNPs) or gold nanostars (AuNSs) as nanocarriers, and (ii) surface-passivated antibody-based fibroblast activation protein (FAP)-targeting modules, used in adaptive chimeric antigen receptor T-cells immunotherapy.
View Article and Find Full Text PDFNano Lett
August 2025
Nanomaterials in Health Laboratory, Department of Materials Meet Life, Swiss Federal Laboratories for Materials Science and Technology (Empa), Lerchenfeldstrasse 5, 9014 St. Gallen, Switzerland.
Hypoxia, a common feature in solid tumors, induces cellular radioresistance and reduces radiotherapy efficacy. Nanoparticles present a promising radiosensitizing approach providing localized dose enhancement through physical or chemical mechanisms. While many preclinical studies have shown nanoparticle radiosensitization, most have focused on normoxic conditions, leaving the impact of hypoxia on nanoparticle-mediated dose enhancement unclear.
View Article and Find Full Text PDFEur J Med Chem
August 2025
School of Pharmaceutical Sciences, Chongqing Key Laboratory of Natural Product Synthesis and Drug Research, Chongqing University, Chongqing, 401331, PR China. Electronic address:
Mutations at arginine 132 in isocitrate dehydrogenase 1 (IDH1) are prevalent in various cancers, making them attractive therapeutic targets. Here, we report the discovery and optimization of a novel dual inhibitor. Initial screening of an in-house library identified lead compound 1-1, which inhibited IDH1 R132H by 73.
View Article and Find Full Text PDFAnticancer Res
August 2025
Department of Bioengineering, Division of Bioscience and Bioindustry, Graduate School of Technology, Industrial and Social Sciences, Tokushima University Graduate School, Tokushima, Japan.
Background/aim: Matrix metalloproteinases (MMPs) are important for extracellular matrix (ECM) degradation with MMP inhibition possibly leading to new antitumor therapies. To examine this possibility, UTX-121, in which the celecoxib sulfonamide was replaced with a methyl ester, was designed to examine the influence of UTX-121 derivatives on MMPs.
Materials And Methods: HT-1080 cells were incubated with UTX-121 derivatives over 48 h, and antitumor activities (IC) were examined using WST-8 assay.