We propose to use in vitro tests for the design of antiinflammatory drugs. These tests are inhibition of prostaglandin synthetase and binding to albumin. The antienzymic potency of a compound is a good indicator of its local antiinflammatory activity. The difference between the antienzymic and the albumin ligand potencies of a compound roughly correlates with its systemic antiinflammatory activity. We found it rewarding to use de novo models for studying structure-activity relationship within our series of prostaglandin synthetase inhibitors. It is supposed that the general chemical character of prostaglandin synthetase inhibitors inclines to a wide application of the additive mathematical model of Free and Wilson for the design of antiinflammatory drugs.
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Wiad Lek
January 2025
DEPARTMENT OF PHARMACOLOGY AND TOXICOLOGY, FACULTY OF PHARMACY, UNIVERSITY OF KUFA, KUFA, IRAQ.
Objective: Aim: Testing Cordia myxa extract on colon cancer cell line and caspase-3 gene and COX-2 protein expression.
Patients And Methods: Materials and Methods: This study used Cordia myxa ethanolic extract at various dosages on SW480 cells. Cell proliferation was measured using MTT, also examined effect of Cordia myxa extract on caspase-3 gene expression using quantitative real-time polymerase chain reaction.
Molecules
January 2025
Department of Pharmacology and Toxicology, College of Pharmacy, Qassim University, Buraydah 51452, Saudi Arabia.
Dual inhibition of cyclooxygenase-2 (COX-2) and lipoxygenase (LOX) is a recognized strategy for enhanced anti-inflammatory effects in small molecules, offering potential therapeutic benefits for individuals at risk of dementia, particularly those with neurodegenerative diseases, common cancers, and diabetes type. Alzheimer's disease (AD) is the most common cause of dementia, and the inhibition of acetylcholinesterase (AChE) is a key approach in treating AD. Meanwhile, Caspase-3 catalyzes early events in apoptosis, contributing to neurodegeneration and subsequently AD.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Shemyakin-Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Miklukho-Maklaya 16/10, 117997 Moscow, Russia.
2-arachnadoyl glycerol (2-AG) is one of the most common endocannabinoid molecules with anti-proliferative, cytotoxic, and pro-proliferative effects on different types of tumors. Typically, it induces cell death via cannabinoid receptor 1/2 (CB1/CB2)-linked ceramide production. In breast cancer, ceramide is counterbalanced by the sphingosine-1-phosphate, and thus the mechanisms of 2-AG influence on proliferation are poorly understood.
View Article and Find Full Text PDFInt J Mol Sci
January 2025
Laboratory of Nutritional Biochemistry, National Institute of Gastroenterology IRCCS "Saverio de Bellis", 70013 Castellana Grotte, Italy.
Navelina oranges () are rich in phytonutrients and bioactive compounds, especially flavonoids like hesperidin. This study investigates the anti-inflammatory and anti-fibrotic properties of hesperidin (HE) and a polyphenol mixture from Navelina oranges (OE) in human hepatocytes (Hepa-RG) and hepatic stellate cells (LX-2), in order to elucidate the underlying molecular mechanisms. In Hepa-RG cells, HE treatment increased expression of cannabinoid receptor 2 (CB2R), which was associated with down-regulation of p38 mitogen-activated protein kinases (p38 MAPK) but had minimal impact on cyclooxygenase-2 (COX-2) and transforming growth factor-β (TGF-β) levels.
View Article and Find Full Text PDFBMC Pediatr
January 2025
Medical Biochemistry Department, Medical Research and Clinical Studies Institute, National Research Centre, Cairo, Egypt.
Background: Chronic inflammation and its control are crucial to the responses of glomerular and renal tubular cells. This contributes to the pathogenic mechanisms and advancement of the disease in Alport syndrome. The study aimed to elucidate the role of cyclooxygenase-2, Interleukin 4, Plasminogen activating inhibitor 1, and Prostaglandin E2 in the development and course of Alport syndrome.
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