To address the problem of acute cocaine overdose, we undertook molecular engineering of butyrylcholinesterase (BChE) as a cocaine hydrolase so that modest doses could be used to accelerate metabolic clearance of this drug. Molecular modeling of BChE complexed with cocaine suggested that the inefficient hydrolysis (k(cat) = 4 min(-1)) involves a rotation toward the catalytic triad, hindered by T...

Human butyrylcholinesterase (hBChE) is currently being developed as a detoxication enzyme for stoichiometric binding and/or catalytic hydrolysis of organophosphates. Herein, we describe the use of a molecular evolution method to develop novel hBChE variants with increased resistance to stereochemically defined nerve agent model compounds of soman, sarin, and cyclosarin. Novel hBChE variants (Y3...

This study compared obese (N = 134) and unobese (N = 92) male blood donors, regarding the relative intensity (RI) and activity of different molecular forms (G1, G2, G4 and G1-ALB) of butyrylcholinesterase (BChE, EC 3.1.1.8) found in plasma, thereby searching for an association between these variables with obesity and SNPs of exons 1 and 4 of the BCHE gene. It was shown that obese and unobese in...

Acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) catalyze the hydrolysis of the neurotransmitter acetylcholine and, thereby, function as coregulators of cholinergic neurotransmission. For both enzymes, hydrolysis takes place near the bottom of a 20 Å deep active site gorge. A number of amino acid residues within the gorge have been identified as important in facilitating efficient ...

Corresponding author: Eun Sung Kim, M.D., Ph.D., Department of Anesthesiology and Pain Medicine, Seoul St. Mary’s Hospital, College of Medicine, The Catholic University of Korea, 505, Banpo-dong, Seocho-gu, 137-040, Korea. Tel: 82-2-2258-2236, Fax: 82-2-591-1592, E-mail: [email protected] This is an open-access article distributed under the terms of the Creative Commons Attribution Non-Co...

The present study reports the synthesis of a series N-substituted derivatives of brominated 2-phenitidine. First, the reaction of 2-phenitidine (1) with benzenesulfonyl chloride (2) in aqueous media yielded N-(2-ethoxyphenyl) benzenesulfonamide (3), which was then subjected to bromination with bromine in the presence of glacial acetic acid to give N-(4,5-dibromo-2-ethoxyphenyl)benzenesulfonamid...

The volatile organic compounds (VOCs) of two Coronilla species (Coronilla orientalis Miller and Coronilla varia L.) obtained by hydrodistillation (HD) and solid phase microextraction (SPME) techniques were identified by GC-FID/MS. The major compounds identified in the SPME extracts were limonene (43.4%) in C. orientalis, (Z)-β-ocimene and (E...

The volatile organic compounds (VOCs) of two Coronilla species (Coronilla orientalis Miller and Coronilla varia L.) obtained by hydrodistillation (HD) and solid phase microextraction (SPME) techniques were identified by GC-FID/MS. The major compounds identified in the SPME extracts were limonene (43.4%) in C. orientalis, (Z)-β-ocimene and (E...

Background and objectives: Variety of extraction methods coupled with definite solvents could increase the removal rate ofmajor constituents from plants. This research has been conducted to evaluate the effect of extraction methods on the main group of compounds, cytotoxicity, anti acetylcholinesterase (AChE) and antioxidant activity of Trachyspermum ammi fruits. <stro...