The synthesis, in vitro/in vivo antifungal evaluation and a structure-activity relationship (SAR) study of 3(2H)-pyridazinones was carried out. The results reported here may be helpful in the structural identification and understanding of the minimum structural requirements for these molecules acting as antifungal agents. In addition, the most active structure in this series was tested for its capacity of inhibiting Saccharomyces cerevisiae beta 1,3-glucan synthase and chitin synthase, enzymes that catalyze the synthesis of the major polymers of the fungal cell wall.
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http://dx.doi.org/10.1055/s-0031-1299820 | DOI Listing |
Sci Rep
January 2025
School of Pharmacy, Fudan University, 826 Zhangheng Road, Shanghai, 201203, P.R. China.
Hawthorn leave flavonoids (HLF) are widely used as an herb or dietary supplements for cardio-cerebrovascular diseases. However, its gastrointestinal absorption behavior and mechanism have not been disclosed. In this study, gastrointestinal absorption and its regulation of 4''-O-glucosylvitexin (GLV), 2''-O-rhamnosylvitexin (RHV), vitexin (VIT), rutin (RUT) and hyperoside (HP) in HLF were investigated using in vitro, in situ and in vivo models.
View Article and Find Full Text PDFAlzheimers Dement
December 2024
University of Virginia, Charlottesville, VA, USA.
Background: Tau phosphorylated at threonine-217 (tau), which can be measured in plasma and CSF using antibodies, is one of the most promising early biomarkers for Alzheimer's disease (AD). Little was known, however, about the cellular and subcellular distributions of tau, how those levels change during disease progression, the factor(s) that provoke tau accumulation, or functional consequences of tau phosphorylation at T217. This study addressed all of those issues.
View Article and Find Full Text PDFAlzheimers Dement
December 2024
Indiana University School of Medicine, Indianapolis, IN, USA.
Background: Alzheimer's disease (AD) and other neurodegenerative diseases are typified by a robust microglial-mediated immune response. Genetic studies have demonstrated that variants in microglial genes are linked to risk for AD. Genome-wide association studies (GWAS) originally identified Phospholipase C gamma 2 (PLCγ2) as a novel risk gene of Alzheimer's disease (AD).
View Article and Find Full Text PDFPLoS One
December 2024
Department of Applied Mathematics, University of California, Santa Cruz, Santa Cruz, CA, United States of America.
The motility of macrophages in response to microenvironment stimuli is a hallmark of innate immunity, where macrophages play pro-inflammatory or pro-reparatory roles depending on their activation status during wound healing. Cell size and shape have been informative in defining macrophage subtypes. Studies show pro and anti-inflammatory macrophages exhibit distinct migratory behaviors, in vitro, in 3D and in vivo but this link has not been rigorously studied.
View Article and Find Full Text PDF3 Biotech
January 2025
Faculty of Industrial Sciences and Technology, Universiti Malaysia Pahang Al-Sultan Abdullah, Lebuhraya Persiaran Tun Khalil Yaakob, Gambang, 26300 Kuantan, Pahang Malaysia.
Diabetes mellitus (DM) is a metabolic disease marked by an excessive rise in blood sugar (glucose) levels caused by a partial or total absence of insulin production, combined with alterations in the metabolism of proteins, lipids, and carbohydrates. The International Diabetes Federation estimates that 425 million individuals globally had diabetes in 2017 which will be 629 million by 2045. Several medications are used to treat DM, but they have limitations and side effects including weight gain, nausea, vomiting, and damage to blood vessels and kidneys.
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