Organophosphorus and carbamate insecticides are toxic to insects and mammals by virtue of their ability to inactivate the enzyme acetylcholinesterase. This review addresses the mechanism of inhibition of acetylcholinesterase by organophosphorus and carbamate esters, focusing on structural requirements necessary for anticholinesterase activity. The inhibition of acetylcholinesterase by these com...

Background and Objective: Changes of the enzyme acetylcholinesterase are involved in pathogenesis of different nervous disorders including Alzheimer’s disease. This research work was conducted to evaluate the inhibitory effect of Pistacia lentiscus ethanolic extract on acetylcholinesterase activity. Materials and Methods: Activity of the enzyme acetylcholinesterase (AChE) was measured by Ellman...

In the symptomatic treatment of mild to moderately severe dementia associated with Alzheimer’s disease, donepezil (E2020) has been introduced for the inhibition of acetylcholinesterase activity in the human brain. However, there is no morphological evidence as to how this chemical agent affects the acetylcholinesterase-positive structures in the various areas of the human and the rat CNS. This ...

The present study aimed to investigate the essential oil composition of Liparis nervosa (Thunb.) Lindl., grown in China, and determine its antioxidant inhibitory effects on acetylcholinesterase. was obtained by hydrodistillation, chemical compounds were analyzed GC-MS GC-FID. We used 2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS), 2,2-diphenyl-1-picrylhydrazyl (DPPH), ferric redu...

New series of indole derivatives analogous to donepezil, a well known anti-Alzheimer and acetylcholinesterase inhibitor drug, was synthesized. A full chemical characterization of the new compounds is provided. Biological evaluation of the new compounds as acetylcholinesterase inhibitors was performed. Most of the compounds were found to have potent acetylcholinesterase inhibitor activity compar...

Measurement of alpha-fetoprotein concentration and acetylcholinesterase activity in amniotic fluid can be used to identify chromosomal defects as well as neural tube defects. In seven cases of trisomy 21 and one case of partial trisomy 3, alpha-fetoprotein concentrations were below the reference range but values for acetylcholinesterase activity were normal for the appropriate gestational age. ...

Crystal structures of acetylcholinesterase complexed with ligands are compared with side-chain conformations accessed by native acetylcholinesterase in molecular dynamics (MD) simulations. Several crystallographic conformations of a key residue in a specific binding site are accessed in a simulation of native acetylcholinesterase, although not seen in rotomer plots. Conformational changes upon ...

background: to evaluate the immunological properties of leishmania major excreted- secreted (e-s) products on the progress of leishmaniasis in susceptible balb/c mice. methods: promastigotes of the leishmania major were cultured and e-s products were collected during the culture preiod. groups of balb/c mice (n= 12) were immunized with e-s products or whole antigen. animals were challenged with...

Inhibition of the critical enzyme acetylcholinesterase (E.C. 3.1.1.7) with subsequent cholinergic crisis is the mechanism of acute toxicity of the organophosphorus insecticides (B. E. Mileson et al., 1998, Toxicol. Sci.41, 8-20). Consequently, measurement of acetylcholinesterase activity is important for evaluating the mammalian toxicity of this commonly used class of insecticides. While mammal...

the chemical composition of the essential oils of flower at the pre-flowering, full-flowering and post-flowering stage of a. annua was analyzed by gc and gc/ms and sixty-two components were identified. the main compounds in the pre-flowering oil were β-myrcene (37.71%), 1, 8-cineole (16.11%) and camphor (14.97%). the full-flowering oil contained predominantly caryophyllene (19.4%), germacrene d...