Short-term hypothermia, caused by cooling of rats down to 20 degrees, decreased distinctly the Na+, K+-ATPase activity in brain homogenates incubated at 37 degrees and did not affect the enzyme activity in the homogenates incubated at 20 degrees. The longer hypothermia (2 hrs at 20 degrees) did not affect the Na+, K+-ATPase activity at 37 degrees (during incubation) and decreased the enzymatic activity in homogenates of middle brain and diencephalon at 20 degrees during the incubation. Contrary to Na+, K+-ATPase, the activity of acetylcholinesterase was markedly increased in brain tissues of rats with hypothermia (irrespective of the temperature of incubation) as compared with control animals.
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J Membr Biol
January 2025
Laboratório de Bioquímica Celular, Universidade Federal de São João del-Rei (UFSJ), Divinópolis, Brazil.
Cancer is a leading cause of death worldwide and its treatment is hampered by the lack of specificity and side effects of current drugs. Cardiotonic steroids (CTS) interact with Na/K-ATPase (NKA) and induce antineoplastic effects, but their narrow therapeutic window is key limiting factor. The synthesis of digitoxigenin derivatives with glycosidic unit modifications is a promising approach to develop more selective and effective antitumor agents.
View Article and Find Full Text PDFJ Nat Prod
January 2025
Division of Medicinal Chemistry and Pharmacognosy, College of Pharmacy, The Ohio State University, Columbus, Ohio 43210, United States.
(-)-Cryptanoside A () was identified previously as a major cytotoxic component of the stems of collected in Laos, which mediates its activity by targeting Na/K-ATPase (NKA), with hydrogen bonds formed between its 11- and 4'-hydroxy groups and NKA being observed in its docking profile. In a continuing investigation, and its 17-epimer, (-)-17--cryptanoside A (), and the new (+)-2-hydroxyandrosta-4,6-diene-3-one-17-carboxylic acid () and the known (+)-2,21-dihydroxypregna-4,6-diene-3,20-dione or 2-hydroxy-6,7-didehydrocortexone () pregnane-type steroids were isolated from . In addition, (-)-11,4'-di--acetylcryptanoside A () has been synthesized from the acetylation of .
View Article and Find Full Text PDFGenes Brain Behav
February 2025
Laboratory of Addiction Genetics, Department of Pharmaceutical Sciences and Center for Drug Discovery, Northeastern University, Boston, Massachusetts, USA.
Opioid use disorder is heritable, yet its genetic etiology is largely unknown. C57BL/6J and C57BL/6NJ mouse substrains exhibit phenotypic diversity in the context of limited genetic diversity which together can facilitate genetic discovery. Here, we found C57BL/6NJ mice were less sensitive to oxycodone (OXY)-induced locomotor activation versus C57BL/6J mice in a conditioned place preference paradigm.
View Article and Find Full Text PDFJ Biosci Bioeng
January 2025
Department of Chemical Engineering, Faculty of Engineering, Kyushu University, 744 Motooka, Nishi-ku, Fukuoka 819-0395, Japan.
Polarized epithelial cells are compartmentalized into apical and basement membranes with asymmetrically distributed proteins. This study aimed to establish a method for culturing epithelial cells at the fluorinated oil (Novec-7500) microdroplet surface for the formation of epithelial polarity, which is desirable for regenerative medicine and drug discovery research. Microdroplet surfaces treated with fibronectin, which regulates a variety of cell behaviors through direct interactions with cell surface integrin receptors, were prepared for culturing epithelial cells.
View Article and Find Full Text PDFEpilepsia
January 2025
Division of Pediatric Neurology and Developmental Medicine, Department of Pediatrics, Duke University, Durham, North Carolina, USA.
Objective: This study was undertaken to test the following hypotheses in the Atp1a3 mouse (which carries the most common human ATP1A3 (the major subunit of the neuronal Na/K-adenosine triphosphatase [ATPase]) mutation, D801N): sudden unexpected death in epilepsy (SUDEP) occurs during seizures and is due to terminal apneas in some and due to lethal cardiac arrhythmias in others; and Atp1a3 mice have central cardiorespiratory dysregulation and abnormal respiratory drive.
Methods: Comparison was made of littermate wild-type and Atp1a3 groups using (1) simultaneous in vivo video-telemetry recordings of electroencephalogram, electrocardiogram, and breathing; (2) whole-body plethysmography; and (3) hypoglossal nerve recordings.
Results: In Atp1a3 mice, (1) SUDEP consistently occurred during seizures that were more severe than preterminal seizures; (2) seizure clustering occurred in periods preceding SUDEP; (3) slowing of breathing rate (BR) and heart rate was observed preictally before preterminal and terminal seizures; and (4) the sequence during terminal seizures was as follows: bradypnea with bradycardia/cardiac arrhythmias, then terminal apnea, followed by terminal cardiac arrhythmias.
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