The purpose of this study was to investigate the protective effect Beta vulgaris leaf extract (BVLE) on Fe2+-induced oxidative testicular damage via experimental and computational models. Oxidative induced incubation tissue supernatant with 0.1 mM FeSO4 for 30 min at 37 °C. Treatment achieved by incubating tissues BVLE under same conditions. catalase (CAT), superoxide dismutase (SOD), glutathio...

To elucidate the mechanism whereby distigmine, an underactive bladder remedy, potentiates urinary bladder contractions long-lastingly, the inhibition of recombinant human acetylcholinesterase (rhAChE) by distigmine was investigated. A centrifugal ultrafiltration device, Nanosep® 10K, was used to separate rhAChE and a bound inhibitor from an unbound inhibitor, reaction substrate, and reaction pr...

The short and long term effects of chromium toxicity on brain catecholamines and acetylcholinesterase levels were investigated. Rats were injected daily with varying amounts of chromium. The short term (2 h) administration of chromium (8 mmol/kg) reduced catecholamines level of cerebellum, mid-brain and brain-cortex by 22.8, 19.4 and 21.2% respectively. Acetylcholinesterase activity was also re...

Generic Name: Galantamine Brand Name: Reminyl® Manufacturer: Shire Pharmaceuticals and Janssen Cilag (http://www.janssenpharmaceutica.be/index_N.asp) Summary: Galantamine hydrobromide, a phenanthrene alkaloid, is a reversible, competitive acetylcholinesterase inhibitor that is structurally unrelated to other acetylcholinesterase inhibitors (e.g, donepezil, rivastigmine, tacrine). Galantamine hy...

The regulation of the rat heart muscarinic acetylcholine receptor by injection of paraoxon (an acetylcholinesterase inhibitor) was characterized. No changes in receptor density in the four cardiac chambers were seen after two days. After three daily injections, however, significant decreases (20-25%) were observed in both atria and ventricles. These changes were associated with a 50% decrease i...

We report herein that a variety of isosorbide di-esters, previously reported to be novel substrates for butyrylcholinesterase (BuChE, EC 3.1.1.8), are in fact inhibitors of the homologous enzyme acetylcholinesterase (AChE), with IC(50) values in the micromolar range. In vitro studies show that they are mixed inhibitors of the enzyme, and thus the ternary enzyme-inhibitor-substrate complex can f...

Two novel mechanisms of organophosphate resistance were isolated and characterized from a population of Culex pipiens L. from Cyprus. Two strains, one expressing the novel, highly active esterases A5 and B5 (strain A5B5-R), and one expressing insensitive acetylcholinesterase (strain Ace-R), were developed by single pair crosses and selection with temephos and propoxur, respectively. The A5B5-R ...

To delineate the role of peptide backbone flexibility and rapid molecular motion in acetylcholinesterase catalysis and inhibitor association, we investigated the decay of fluorescence anisotropy at three sites of fluorescein conjugation to cysteine-substitution mutants of the enzyme. One cysteine was placed in a loop at the peripheral site near the rim of the active center gorge (H287C); a seco...

The X-ray crystal structure of Torpedo californica acetylcholinesterase (TcAChE) complexed with BW284C51 [CO[-CH(2)CH(2)-pC(6)H(4)-N(CH(3))(2)(CH(2)-CH=CH(2))](2)] is described and compared with the complexes of two other active-site gorge-spanning inhibitors, decamethonium and E2020. The inhibitor was soaked into TcAChE crystals in the trigonal space group P3(1)21, yielding a complex which dif...