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Synthesis and evaluation of the antifungal and antibiofilm potential of aminochalcones.
Arch Microbiol
January 2025
Department of Chemistryand Environmental Sciences, Institute of Biosciences, Humanities and Exact Sciences, São Paulo State University Júlio de Mesquita Filho, São José do Rio Preto, SP, Brazil.
Candida is a commensal fungus of clinical interest that commonly lives in oral cavity and intestine but can become an opportunist microrganism and cause severe infections. A serie of 10 aminochalcones were designed and synthetized to obtain compounds anti-Candida with potent and broad-spectrum activity. The most active compound J34 demonstrated excellent in vitro activity against Candida albicans, Candida tropicalis, Candida parapsilosis, Candida glabrata and Candida krusei with minimum inhibitory concentration between 1.
View Article and Find Full Text PDFTolterodine is a novel candidate for assessing CYP3A4 activity through metabolic volatiles to predict drug responses.
Sci Rep
January 2025
Institute for Breath Research, University of Innsbruck, Innrain 80/82, Innsbruck, 6020, Austria.
Cytochrome P450 (CYP) 3A4 plays a major role in drug metabolism. Its activity could be determined by non-invasive and cost-effective assays, such as breath analysis, for the personalised monitoring of drug response. For the first time, we identify an isotopically unlabelled CYP3A4 substrate, tolterodine that leads to the formation of a non-toxic volatile metabolite, acetone, which could potentially be applied to monitor CYP3A4 activity in humans.
View Article and Find Full Text PDFTherapeutic potential of ketone bodies on exercise intolerance in heart failure: looking beyond the heart.
Cardiovasc Res
January 2025
Cardiovascular Research Centre, University of Alberta, Edmonton, Alberta, Canada.
Recent evidence suggests that ketone bodies have therapeutic potential in many cardiovascular diseases including heart failure (HF). Accordingly, this has led to multiple clinical trials that use ketone esters to treat HF patients, which we term ketone therapy. Ketone esters, specifically ketone monoesters, are synthetic compounds which, when consumed, are de-esterified into two β-hydroxybutyrate (βOHB) molecules and increase the circulating βOHB concentration.
View Article and Find Full Text PDFA murine model of acute and prolonged abdominal sepsis, supported by intensive care, reveals time-dependent metabolic alterations in the heart.
Intensive Care Med Exp
January 2025
Clinical Division and Laboratory of Intensive Care Medicine, Department of Cellular and Molecular Medicine, KU Leuven, Herestraat 49, O&N1 Box 503, 3000, Louvain, Belgium.
Background: Sepsis-induced cardiomyopathy (SICM) often occurs in the acute phase of sepsis and is associated with increased mortality due to cardiac dysfunction. The pathogenesis remains poorly understood, and no specific treatments are available. Although SICM is considered reversible, emerging evidence suggests potential long-term sequelae.
View Article and Find Full Text PDFCognitive impairment caused by compromised hepatic ketogenesis is prevented by endurance exercise.
J Physiol
January 2025
Department of Nutrition and Exercise Physiology, University of Missouri-Columbia, Columbia, Missouri, USA.
Extensive research has demonstrated endurance exercise to be neuroprotective. Whether these neuroprotective benefits are mediated, in part, by hepatic ketone production remains unclear. To investigate the role of hepatic ketone production on brain health during exercise, healthy 6-month-old female rats underwent viral knockdown of the rate-limiting enzyme in the liver that catalyses the first reaction in ketogenesis: 3-hydroxymethylglutaryl-CoA synthase 2 (HMGCS2).
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