In an extensive analysis of the antiviral and interferon-induction structure-activity relationship of 6-arylpyrimidinones we found that modifications at positions 1-4 of the pyrimidine ring resulted in a loss of activity. However, we uncovered interesting hypotensive and antiinflammatory activity with a series of N-substituted analogues, the results of which we report herein.
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http://dx.doi.org/10.1021/jm00158a030 | DOI Listing |
J Microbiol Biotechnol
January 2025
Department of Pharmaceutical Engineering & Biotechnology, Sunmoon University, Chungnam 31460, Republic of Korea.
is a lactic acid bacteria found in fermented products. In our previous study, was isolated from flowers, and its acid tolerance and antibacterial properties were thoroughly investigated. This study focuses on the inhibition of melanin synthesis and inflammation of exosomes derived from .
View Article and Find Full Text PDFEur J Pharm Biopharm
January 2025
Department of Chemistry, State University of Londrina, Londrina, PR, Brazil; Department of Pharmaceutical Sciences, State University of Londrina, Londrina, PR, Brazil. Electronic address:
This study aimed to develop patches containing quercetin-loaded microcapsules and to evaluate their in vitro and in vivo safety and efficacy in preclinical surveys. A set of in vitro experiments evidenced the virucidal activity of quercetin against the HSV-1-KOS (sensitive to acyclovir) and HSV-1-AR (resistant to acyclovir) strains, with improved outcomes upon the first. The patches presented a homogeneous aspect, were easily handled, had a suitable bioadhesion, and possessed mechanical properties of soft and weak material, besides a pH compatible with human skin.
View Article and Find Full Text PDFPsychopharmacology (Berl)
January 2025
Department of Pharmacology and Toxicology, Faculty of Pharmacy, Ain Shams University, Cairo, Egypt.
Rationale: One of the most debilitating drawbacks of cisplatin chemotherapy is neurotoxicity which elicits memory impairment and cognitive dysfunction (chemobrain). This is primarily triggered by oxidative stress and inflammation. Captopril, an angiotensin-converting enzyme inhibitor, has been reported as a neuroprotective agent owing to its antioxidant and anti-inflammatory effects.
View Article and Find Full Text PDFSemin Liver Dis
January 2025
Hepatology, University of Pennsylvania, Philadelphia, United States.
Critically ill patients with cirrhosis and liver failure not uncommonly have hypotension due to multifactorial reasons, that include hyperdynamic state with increased cardiac index, low systemic vascular resistance due to portal hypertension, following the use of beta blocker or diuretic therapy, and severe sepsis. These changes are mediated by microvascular alterations in the liver, systemic inflammation, activation of renin angiotensin aldosterone system, and vasodilatation due to endothelial dysfunction. Hemodynamic assessment includes measuring inferior vena cava indices, cardiac output and systemic vascular resistance using point-of-care ultrasound (POCUS), in addition to arterial waveform analysis, or pulmonary artery pressures, and lactate clearance to guide fluid resuscitation.
View Article and Find Full Text PDFProc Biol Sci
January 2025
Laboratory for Integrative Neuroscience and Endocrinology, University of Bristol, Bristol BS1 3NY, UK.
Cortisol is released upon activation of the hypothalamic-pituitary-adrenal axis, varies across the day, possesses an underlying diurnal rhythm and is responsive to stressors. The endogenous circadian peak of cortisol occurs in the morning, and increases in cortisol observed post-awakening have been named the cortisol awakening response (CAR) based on the belief that the act of waking up stimulates cortisol secretion. However, objective evidence that awakening induces cortisol secretion is limited.
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