(±)-Dispirocochlearoids A-C (-), meroterpenoids with a 6/6/5/6/6/6 ring system, were isolated from . - are selective COX-2 inhibitors with an IC value of (-)- at 386 nM. Site-directed mutagenesis identified His351 as a COX-2 active site. In vivo anti-inflammatory activities of (-)- were performed against acute lung injury in mice.
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http://dx.doi.org/10.1021/acs.orglett.0c00452 | DOI Listing |
Sci Rep
January 2025
Department of Biochemistry and Food Chemistry, University of Life Sciences, Skromna Str. 8, Lublin, 20-704, Poland.
Polyphenolic plant compounds possess nutritional and pro-healthy potential, reducing the risk of auto-inflammatory and neoplastic diseases. However, their interference with the progression of thyroid gland dysfunctions has remained largely unaddressed. For this purpose, we combined the analyses of phenolic content and antioxidative activity with the thyroid peroxidase (TPO), lipoxygenase (LOX), xanthine oxidase (XO) and cyclooxygenase-2 (COX-2) activity assays, isobolographic approach and the estimation of thyroid cancer cells' proliferation and motility in vitro.
View Article and Find Full Text PDFSci Rep
January 2025
State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao SAR, China.
Brain microvascular endothelial cells are connected by tight junction (TJ) proteins and interacted by adhesion molecules, which participate in the selective permeability of the blood-brain barrier (BBB). The disruption of BBB is associated with the progression of cerebral diseases. Pterostilbene is a natural compound found in blueberries and grapes with a wide range of biological activities, including anti-inflammatory, antioxidant, and anti-diabetic effects.
View Article and Find Full Text PDFJ Trace Elem Med Biol
January 2025
Department of Pathology, College of Medicine, King Khalid University, Asir 61421, Saudi Arabia; Department of Forensic Medicine and Clinical Toxicology, Mansoura University, Egypt.
Background: Vanadium (VAN) is a significant trace element, but its higher exposure is reported to cause severe organ toxicity. Tectochrysin (TEC) is a naturally derived flavonoid which demonstrates a wide range of pharmacological properties.
Aim: The current study was planned to assess the cardioprotective potential of TEC against VAN induced cardiotoxicity in rats via regulating biochemical, and histological profile.
Alzheimers Dement
December 2024
All India Institute of Medical Sciences, AIIMS, New Delhi, Delhi, India.
Background: Alzheimer's disease (AD) is a progressive brain disorder which leads to gradual decline in memory, thinking, behaviour and social skills. The current scenario for drug development is based on neuro-inflammation and oxidative stress. Amyloid-β (Aβ) deposition, a major hallmark of the disease activates microglia leading to neuro-inflammation and neuro-degeneration induced by activation of COX-2 via NFkB p50 in glioblastoma cells.
View Article and Find Full Text PDFBiomed Chromatogr
February 2025
Department of Pharmacy, Lianyungang Affiliated Hospital of Nanjing University of Chinese Medicine, Lianyungang, China.
Choerospondias axillaris is a medicinal plant used for treating coronary heart disease (CHD) due to its broad spectrum of anti-inflammatory activities. Cyclooxygenase 2 (COX-2) and lipoxygenase 5 (5-LOX) were immobilized on magnetic nanoparticles for selective ligand-extraction of these two enzymes present in C. axillaris.
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