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Novel Benzimidazole Derivatives as Potent Inhibitors of Microsomal Prostaglandin E Synthase 1 for the Potential Treatment of Inflammation, Pain, and Fever.
J Med Chem
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Gazi University, 06560 Ankara, Turkey.
Article Synopsis
- mPGES-1 is highlighted as a key target for developing treatments for inflammation and pain, with the study introducing new benzimidazole compounds that effectively inhibit this enzyme.
- One of the compounds, AGU654, showed exceptional selectivity for mPGES-1 over other related enzymes, with a low inhibition concentration (IC = 2.9 nM) and promising bioavailability.
- AGU654 was able to reduce PGE production from activated immune cells without affecting other prostaglandins, and it also demonstrated success in alleviating fever and pain in guinea pig models, indicating its potential for managing inflammatory diseases.
Dietary Walnuts Prevented Indomethacin-Induced Gastric Damage via AP-1 Transcribed 15-PGDH, Nrf2-Mediated HO-1, and n-3 PUFA-Derived Resolvin E1.
Int J Mol Sci
June 2024
CHA Cancer Preventive Research Center, CHA Bio Complex, Seongnam 13488, Republic of Korea.
Non-steroidal anti-inflammatory drugs (NSAIDs), the most highly prescribed drugs in the world for the treatment of pain, inflammation, and fever, cause gastric mucosal damage, including ulcers, directly or indirectly, by which the development of GI-safer (-sparing) NSAIDs relates to unmet medical needs. This study aimed to document the preventive effects of walnut polyphenol extracts (WPEs) against NSAID-induced gastric damage along with the molecular mechanisms. RGM-1 gastric mucosal cells were administered with indomethacin, and the expressions of the inflammatory mediators between indomethacin alone or a combination with WPEs were compared.
View Article and Find Full Text PDFInhibition of endogenous nitric oxide activity impairs the colonic sparing effect of rofecoxib, the cyclooxygenase-2 inhibitor and resveratrol, the preferential cyclooxygenase-1 inhibitor in the course of experimental colitis. Role of oxidative stress biomarkers and proinflammatory cytokines.
J Physiol Pharmacol
October 2023
Jagiellonian University Medical College, Faculty of Medicine, Department of Physiology, Cracow, Poland.
The gut mucosal barrier plays a key role in the physiology of gastrointestinal (GI) tract, preventing under homeostatic conditions, the epithelial cells of the gastric mucosa from hydrochloric acid and intestinal mucosa from alkaline secretion, food toxins and pathogenic microbiota. Previous studies have documented that blockade of both isoforms of cyclooxygenase (COX): constitutive (COX-1) and inducible (COX-2), as well NO synthase in the stomach exacerbated the gastric damage induced by various ulcerogens, however, such as effects of non-selective and selective inhibition of COX-1, COX-2 and NOS enzymes on colonic damage have been little studied. The supplementation of NO by intragastric (i.
View Article and Find Full Text PDFThe anti-inflammatory and vasoprotective properties of mPGES-1 inhibition offer promising therapeutic potential.
Expert Opin Ther Targets
December 2023
Division of Rheumatology, Department of Medicine, Solna, Karolinska Institutet and Karolinska University Hospital, Stockholm, Sweden.
Introduction: Prostaglandin E (PGE) is produced by cyclooxygenases (COX-1/2) and the microsomal prostaglandin E synthase 1 (mPGES-1). PGE is pro-inflammatory in diseases such as rheumatoid arthritis, cardiovascular disorders, and cancer. While Nonsteroidal anti-inflammatory drugs (NSAIDs) targeting COX can effectively reduce inflammation, their use is limited by gastrointestinal and cardiovascular side effects resulting from the blockade of all prostanoids.
View Article and Find Full Text PDFDual synergistic inhibition of COX and LOX by potential chemicals from Indian daily spices investigated through detailed computational studies.
Sci Rep
May 2023
Pediatric Research Institute, Children's Hospital Affiliated to Shandong University, Jinan, 250022, People's Republic of China.
Cyclooxygenase (COX) and Lipoxygenase (LOX) are essential enzymes for arachidonic acid (AA) to eicosanoids conversion. These AA-derived eicosanoids are essential for initiating immunological responses, causing inflammation, and resolving inflammation. Dual COX/5-LOX inhibitors are believed to be promising novel anti-inflammatory agents.
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