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Discovery of novel bicyclic and tricyclic cyclohepta[b]thiophene derivatives as multipotent AChE and BChE inhibitors, in-Vivo and in-Vitro assays, ADMET and molecular docking simulation.
Eur J Med Chem
December 2024
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Sinai University, Kantara Branch, Ismailia, 41636, Egypt.
Alzheimer's disease (AD) is primarily caused by oxidative stress, hyperphosphorylated τ-protein aggregation, and amyloid-β deposition. Changes in dopaminergic and serotoninergic neurotransmitter pathways are linked to certain symptoms of AD. Derivatives of bicyclic and tricyclic cyclohepta[b]thiophene were developed to identify new potential candidates as acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors for the treatment of AD.
View Article and Find Full Text PDFSPRTN metalloprotease participates in repair of ROS-mediated DNA-protein crosslinks.
Sci Rep
December 2024
Department of Medicinal Chemistry, University of Minnesota, Minneapolis, MN, 55455, USA.
Exposure to reactive oxygen species (ROS) can induce DNA-protein crosslinks (DPCs), unusually bulky DNA lesions that block replication and transcription and play a role in aging, cancer, cardiovascular disease, and neurodegenerative disorders. Repair of DPCs depends on the coordinated efforts of proteases and DNA repair enzymes to cleave the protein component of the lesion to smaller DNA-peptide crosslinks which can be processed by tyrosyl-DNA phosphodiesterases 1 and 2, nucleotide excision and homologous recombination repair pathways. DNA-dependent metalloprotease SPRTN plays a role in DPC repair, and SPRTN-deficient mice exhibit an accelerated aging phenotype and develop liver cancer early in life.
View Article and Find Full Text PDFPhysiological relevance, localization and substrate specificity of the alternative (type II) mitochondrial NADH dehydrogenases of .
Front Microbiol
December 2024
Department of Biotechnology, Delft University of Technology, Delft, Netherlands.
Mitochondria from harbor a branched electron-transport chain containing a proton-pumping Complex I NADH dehydrogenase and three Type II NADH dehydrogenases (NDH-2). To investigate the physiological role, localization and substrate specificity of these enzymes, the growth of various NADH dehydrogenase knockout mutants was quantitatively characterized in shake-flask and chemostat cultures, followed by oxygen-uptake experiments with isolated mitochondria. NAD(P)H:quinone oxidoreduction of the three NDH-2 were individually assessed.
View Article and Find Full Text PDFTwo sides of the same coin: Weathering differences of plastic fragments in coastal environments around the globe.
J Hazard Mater
December 2024
State Key Laboratory of Estuarine and Coastal Research, East China Normal University, Shanghai 200241, China. Electronic address:
Plastic debris in coastal environments usually undergoes weathering due to various environmental conditions. However, the weathering effects on exposed and shaded sides of the same plastics are underexplored. In this study, 1573 plastic fragments were collected from 15 coastal sites worldwide between December 2021 and December 2022, and weathering experiments were conducted outdoors.
View Article and Find Full Text PDFPrenatal Exposure to Quercetin Protects Against Methimazole-Induced Reflexive Motor Behavior and Oxidative Stress Markers in Mouse Offspring.
Int J Dev Neurosci
February 2025
Department of Clinical Sciences, Faculty of Veterinary Medicine, Science and Research Branch, Islamic Azad University, Tehran, Iran.
Quercetin is a natural flavonoid and one of the most powerful antioxidants. Due to its wide range of biological properties, it may improve cognitive and physical performance by affecting nervous tissue. The current study is aimed at determining the effect of prenatal exposure to quercetin against methimazole (MMI)-induced hypothyroidism on reflexive motor behavior in mouse offspring.
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