Published in Fish Physiology and Biochemistry
Brain cholinesterases from four fish (Arapaima gigas, Colossoma macropomum, Rachycentron canadum and Oreochromis niloticus) were characterized using specific substrates and selective inhibitors. Parameters of catalytic efficiency such as activation energy (AE), kcat and kcat/km as well as rate enhancements produced by these enzymes were estimated b...
Published in Rendiconti Lincei
Acetylcholinester ase (AChE) generally known to be sensitive toward insecticides but its sensitivity toward heavy metals was least reported. Herein, a sensitive assay for heavy metals has been pursued using AChE in a rapid and economic manner. The AChE from a mudskipper, Periophthalmodon schlosseri has been found to be sensitive toward copper > mer...
Published in Toxicology letters
Highly toxic organophosphorus (OP) nerve agents are well characterized regarding chemical, biological and toxicological properties and the effectiveness of standard atropine and oxime therapy. Open literature data on the key nerve agent precursor methylphosphonic difluoride (DF) are scarce. To fill this gap the reactions of DF and its main degradat...
Published in Monatshefte für Chemie - Chemical Monthly
AbstractAn efficient synthetic route for the synthesis of novel oxoisoindoline derivatives was described through Ugi reaction of 2-formylbenzoic acids, amines, and isocyanides. All compounds were evaluated for their acetylcholinesterase inhibitory activity and among them, 2 of 12 tested compounds showed good activity as compared to other derivative...
Published in Molecular and Cellular Biochemistry
Methionine is the only endogenous precursor of homocysteine, sulfur—containing amino acid and well known as risk factor for various brain disorders. Acetylcholinesterase is a serine protease that rapidly hydrolyzes neurotransmitter acetylcholine. It is widely distributed in different brain regions. The aim of this study was to elucidate the effects...
Published in Neurochemical Research
It is well known that the principal biomolecules involved in Alzheimer’s disease (AD) are acetylcholinesterase (AChE), acetylcholine (ACh) and the amyloid beta peptide of 42 amino acid residues (Aβ42). ACh plays an important role in human memory and learning, but it is susceptible to hydrolysis by AChE, while the aggregation of Aβ42 forms oligomers...
Published in NeuroImage
The cholinergic system plays a central role in episodic memory-related processes in health and disease. Cerebral acetylcholinesterase (AChE) activity, a measure of the integrity of the cholinergic system, can be assessed in vivo using positron emission tomography (PET) and [(11)C]N-methyl-4-piperidyl acetate (MP4A). A close relationship between the...
Published in Theoretical Biology and Medical Modelling
BackgroundOne of the leading causes of death and illness within the agriculture industry is through unintentionally ingesting or inhaling organophosphate pesticides. OP intoxication directly inhibits acetylcholinesterase, resulting in an excitatory signaling cascade leading to fasciculation, loss of control of bodily fluids, and seizures.MethodsOur...
Published in Molecular Neurobiology
Mild hyperhomocysteinemia is considered to be a risk factor for cerebral and cardiovascular disorders and can be modeled in experimental rats. Inflammation has been implicated in the toxic effects of homocysteine. Cholinergic signaling controls cytokine production and inflammation through the “cholinergic anti-inflammatory pathway,” and brain acety...
Published in Archiv der Pharmazie
Gypsogenin (1) was obtained by acidic hydrolysis from its saponin. While the parent compound 1 acted as a selective inhibitor for butyrylcholinesterase (from equus) possessing a moderate mixed-type inhibition of the enzyme, Ki values as low as 2.67 ± 0.59 μM were determined for (3β,4α) 3-O-acetyl-olean-12-ene-23,28-dinitrile (11) and acetylcholines...
