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Silibinin, a PLC-β3 inhibitor, inhibits mast cell activation and alleviates OVA-induced asthma.
Mol Immunol
January 2025
Chinese Medicine Research and Development Center, China Medical University Hospital, Taichung, Taiwan; Graduate Institute of Integrated Medicine, College of Chinese Medicine, China Medical University, Taichung, Taiwan; Master Program of Pharmaceutical Manufacture, College of Pharmacy, China Medical University, Taichung, Taiwan; Department of Medical Laboratory Science and Biotechnology, College of Medical and Health Science, Asia University, Taichung, Taiwan. Electronic address:
The immunoglobulin E (IgE) receptor FcεRI (Fc epsilon RI) plays a crucial role in allergic reactions. Recent studies have indicated that the interaction between FcεRIβ and the downstream protein phospholipase C beta 3 (PLCβ3) leads to the production of inflammatory cytokines. The aim of this study was to develop small molecules that inhibit the protein-protein interactions between FcεRIβ and PLCβ3 to treat allergic inflammation.
View Article and Find Full Text PDFNew Insights into Aspirin's Anticancer Activity: The Predominant Role of Its Iron-Chelating Antioxidant Metabolites.
Antioxidants (Basel)
December 2024
Postgraduate Research Institute of Science, Technology, Environment and Medicine, Limassol 3021, Cyprus.
Epidemiological studies have suggested that following long-term, low-dose daily aspirin (LTLDA) administration for more than 5 years at 75-100 mg/day, 20-30% of patients (50-80 years old) had a lower risk of developing colorectal cancer (CRC) and about the same proportion in developing iron deficiency anemia (IDA). In cases of IDA, an increase in iron excretion is suspected, which is caused by aspirin chelating metabolites (ACMs): salicylic acid, salicyluric acid, 2,5-dihydroxybenzoic acid, and 2,3-dihydroxybenzoic acid. The ACMs constitute 70% of the administered aspirin dose and have much longer half-lives than aspirin in blood and tissues.
View Article and Find Full Text PDFRepurposing eugenol and cinnamaldehyde as potent antimicrobial agents: A comprehensive in-vitro and in-silico study.
Bioorg Chem
January 2025
Division of Biological and Environmental Sciences and Engineering (BESE), King Abdullah University of Science and Technology (KAUST), Thuwal 23955, Saudi Arabia. Electronic address:
Multi-drug-resistant (MDR) pathogens represent a critical global health threat, necessitating the development of novel antimicrobial agents with broad-spectrum activity and minimal toxicity. This study investigates the antimicrobial and anti-biofilm properties of 4-Allyl-2-methoxyphenol (eugenol, EU) and (E)-3-Phenylprop-2-enal (cinnamaldehyde, CN) against 19 clinically significant pathogens through a combination of in-vitro assays and in-silico analyses. EU displayed remarkable activity, particularly against Aspergillus niger (20.
View Article and Find Full Text PDFRepeated Amphetamine Exposure Blunted Angiotensin II-Induced Responses Mediated by AT Receptors.
Discov Med
January 2025
Department of Pharmacology "Otto Orsingher", Institute of Experimental Pharmacology of Córdoba (IFEC-CONICET), Faculty of Chemical Sciences, National University of Córdoba, X5000 Córdoba, Argentina.
Background: Angiotensin II, is critical in regulating the sympathetic and neuroendocrine systems through angiotensin II type 1 receptors (AT-R). Angiotensin II intracerebral administration increases water and sodium intake, as well as renal sodium excretion. Previously, our group has shown that AT-R is involved in behavioral and neurochemical sensitization induced by amphetamine.
View Article and Find Full Text PDFIdentification of promising SARS-CoV-2 main protease inhibitor through molecular docking, dynamics simulation, and ADMET analysis.
Sci Rep
January 2025
Department of Biophysics and Pharmacology, Bioscience Center, Federal University of Rio Grande do Norte, Natal, 59064-741, RN, Brazil.
The COVID-19 pandemic caused by SARS-CoV-2 continues to pose a major challenge to global health. Targeting the main protease of the virus (Mpro), which is essential for viral replication and transcription, offers a promising approach for therapeutic intervention. In this study, advanced computational techniques such as molecular docking and molecular dynamics simulations were used to screen a series of antiviral compounds for their potential inhibitory effect on the SARS-CoV-2 Mpro.
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