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COX-2-targeted fluorescent probe for ClO monitoring in precise cancer detection.
Bioorg Chem
January 2025
Department of Radiology, the Affiliated Hospital of Southwest Medical University, Luzhou 646000 China; Precision Imaging and Intelligent Analysis Key Laboratory of Luzhou City, Luzhou 646000 China. Electronic address:
Hypochlorite anion (ClO) is closely associated with cancer development and progression, necessitating precise monitoring of ClO in tumor sites, and Cyclooxygenase-2 (COX-2 is highly expressed in tumor cells. So we rationally designed two ClO-specific responsive fluorescent probes COX2-ClO1 and COX2-ClO2, using indomethacin (IMC) as the COX-2 targeting moiety and methylene blue as fluorophore unit. Both probes exhibited high selectivity and sensitivity towards ClO in the in vitro solution assays and possess excellent biocompatibility in cellular experiments.
View Article and Find Full Text PDFPET Quantification in Healthy Humans of Cyclooxygenase-2, a Potential Biomarker of Neuroinflammation.
J Nucl Med
January 2025
Intramural Research Program, National Institute of Mental Health, Bethesda, Maryland;
Cyclooxygenase-2 (COX-2) is present in a healthy brain at low densities but can be markedly upregulated by excitatory input and by inflammogens. This study evaluated the sensitivity of the PET radioligand [C]-6-methoxy-2-(4-(methylsulfonyl)phenyl)--(thiophen-2-ylmethyl)pyrimidin-4-amine ([C]MC1) to detect COX-2 density in a healthy human brain. The specificity of [C]MC1 was confirmed using lipopolysaccharide-injected rats and transgenic mice expressing the human gene, with 120-min baseline and blocked scans using COX-1 and COX-2 selective agents.
View Article and Find Full Text PDFApproximately 800,000 total knee arthroplasties and 450,000 total hip arthroplasties are performed annually in the United States. These procedures provide significant pain relief and restore function in patients with advanced osteoarthritis, rheumatoid arthritis, and other degenerative joint conditions. Patient evaluation before surgery includes a history, physical examination, laboratory tests, and imaging.
View Article and Find Full Text PDFOral supplementation of curcumin-encapsulated chitosan nanoconjugates as an innovative strategy for mitigating nickel-mediated hepatorenal toxicity in rats.
Naunyn Schmiedebergs Arch Pharmacol
January 2025
Nanotechnology and Advanced Materials Central Lab., Agricultural Research Center, Giza, Egypt.
Nickel pollution adversely affects human health and causes various disorders, mainly hepatic and renal dysfunction. The present work focused on a comparative evaluation of the pure form of curcumin (CU) with curcumin-encapsulated chitosan nanoconjugates (CS/CU NCs), on mitigation of the delirious effects of Ni on hepatorenal tissue. Forty-two male rats were allocated into 6 groups (n = 7 for each) as follows: (1) control, (2) CU, (3) CS/CU NCs, (4) Ni, (5) Ni + CU, (6) Ni + CS/CU NCs.
View Article and Find Full Text PDFProtein kinase A suppresses anti-proliferative effect of interferon-α in hepatocellular carcinoma by activation of protein tyrosine phosphatase SHP2.
J Biol Chem
January 2025
Center for Natural Products Research, Chengdu Institute of Biology, Chinese Academy of Sciences, Chengdu, China. Electronic address:
Src homology-2-containing protein tyrosine phosphatase 2 (SHP2) plays a dual role in cancer initiation and progression. Identifying signals that modulate the function of SHP2 can improve current therapeutic approaches for IFN-α/β in HCC. We showed that cAMP-dependent protein kinase A (PKA) suppresses IFN-α/β-induced JAK/STAT signaling by increasing the phosphatase activity of SHP2, promoting the dissociation of SHP2 from the receptor for activated C-kinase 1 (RACK1) and binding to STAT1.
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