645 results match your criteria tested butyrylcholinesterase


Novel Sulfonamide-Based Carbamates as Selective Inhibitors of BChE.

Int J Mol Sci 2021 Aug 31;22(17). Epub 2021 Aug 31.

Institute of Organic Chemistry and Technology, Faculty of Chemical Technology, University of Pardubice, Studentska 573, 532 10 Pardubice, Czech Republic.

A series of 14 target benzyl [2-(arylsulfamoyl)-1-substituted-ethyl]carbamates was prepared by multi-step synthesis and characterized. All the final compounds were tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in vitro, and the selectivity index (SI) was determined. Except for three compounds, all compounds showed strong preferential inhibition of BChE, and nine compounds were even more active than the clinically used rivastigmine. Read More

View Article and Full-Text PDF

Effect of N-acetylcysteine on attenuation of chlropyrifos and its methyl analogue toxicity in male rats.

Toxicology 2021 Sep 20;461:152904. Epub 2021 Aug 20.

Laboratory of Cellular and Molecular Genetics, Department of Genetics, Faculty of Agriculture, Alexandria University, P.O Box 21545, Alexandria, Egypt.

The attenuating effect of 150 mg/kg of N-acetylcysteine (NAC) against the oral administration of 7.88 and 202.07 mg/kg/day for 14 days of either chlropyrifos-ethyl (CPE-E) or chlropyrifos-methyl (CPF-M), respectively, in male rat was investigated using biochemical and genetic markers. Read More

View Article and Full-Text PDF
September 2021

Thiourea Derivatives, Simple in Structure but Efficient Enzyme Inhibitors and Mercury Sensors.

Molecules 2021 Jul 27;26(15). Epub 2021 Jul 27.

Department of Pharmacology and Therapeutics, Faculty of Veterinary Medicine, Damanhour University, Damanhour 22511, Egypt.

In this study six unsymmetrical thiourea derivatives, 1-isobutyl-3-cyclohexylthiourea (), 1-butyl-3-cyclohexylthiourea (), 1-(3-chlorophenyl)-3-cyclohexylthiourea (), 1-(1,1-dibutyl)-3-phenylthiourea (), 1-(2-chlorophenyl)-3-phenylthiourea () and 1-(4-chlorophenyl)-3-phenylthiourea () were obtained in the laboratory under aerobic conditions. Compounds and are crystalline and their structure was determined for their single crystal. Compounds is monoclinic system with space group P2/n while compound is trigonal, space group . Read More

View Article and Full-Text PDF

Discovery of sustainable drugs for Alzheimer's disease: cardanol-derived cholinesterase inhibitors with antioxidant and anti-amyloid properties.

RSC Med Chem 2021 Jul 5;12(7):1154-1163. Epub 2021 May 5.

Department of Pharmacy, Health Sciences Faculty, University of Brasília, Campus Universitário Darcy Ribeiro 70910-900 Brasília DF Brazil

As part of our efforts to develop sustainable drugs for Alzheimer's disease (AD), we have been focusing on the inexpensive and largely available cashew nut shell liquid (CNSL) as a starting material for the identification of new acetylcholinesterase (AChE) inhibitors. Herein, we decided to investigate whether cardanol, a phenolic CNSL component, could serve as a scaffold for improved compounds with concomitant anti-amyloid and antioxidant activities. Ten new derivatives, carrying the intact phenolic function and an aminomethyl functionality, were synthesized and first tested for their inhibitory potencies towards AChE and butyrylcholinesterase (BChE). Read More

View Article and Full-Text PDF

Identification of plant-based multitargeted leads for Alzheimer's disease: In-vitro and in-vivo validation of Woodfordia fruticosa (L.) Kurz.

Phytomedicine 2021 Oct 21;91:153659. Epub 2021 Jul 21.

Natural Products & Medicinal Chemistry Division, CSIR-Indian Institute of Integrative Medicine, Canal Road, Jammu-180001, India; Academy of Scientific & Innovative Research (AcSIR), Ghaziabad-201002, India. Electronic address:

Background: Alzheimer's disease (AD) is a complex neurodegenerative disease with no availability of disease-modifying therapeutics. The complex etiology and recent failures in clinical trials indicate the need for multitargeted agents.

Purpose: The present study aims to discover new plant-based multitargeted anti-AD leads. Read More

View Article and Full-Text PDF
October 2021

Identification of Compounds for Butyrylcholinesterase Inhibition.

SLAS Discov 2021 Jul 16:24725552211030897. Epub 2021 Jul 16.

Division for Pre-Clinical Innovation, National Center for Advancing Translational Sciences, National Institutes of Health, Rockville, MD, USA.

Butyrylcholinesterase (BChE) is a nonspecific cholinesterase enzyme that hydrolyzes choline-based esters. BChE plays a critical role in maintaining normal cholinergic function like acetylcholinesterase (AChE) through hydrolyzing acetylcholine (ACh). Selective BChE inhibition has been regarded as a viable therapeutic approach in Alzheimer's disease. Read More

View Article and Full-Text PDF

Butyrylcholinesterase as a perioperative complication marker in patients after transcatheter aortic valve implantation: a prospective observational study.

BMJ Open 2021 07 6;11(7):e042857. Epub 2021 Jul 6.

Department of Anesthesiology, University Hospital Regensburg, Regensburg, Germany

Objectives: Transcatheter aortic valve implantation (TAVI) is performed in elderly patients with severe aortic valve stenosis and increased operative risks. We tested the hypothesis that acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) have a predictive value for prevalent complications after TAVI and could serve as indicators of systemic inflammation in the early postoperative period.

Design: Prospective observational study. Read More

View Article and Full-Text PDF

Isolation and characterization of chemical constituents from roots and their enzyme inhibitory and antioxidant effects.

Z Naturforsch C J Biosci 2021 Jul 5. Epub 2021 Jul 5.

Department of Chemistry, Faculty of Science, Muğla Sıtkı Koçman University, 48000, Muğla, Turkey.

Isolation and bioactive effects of the roots of L. were firstly investigated herein. Enzyme (acetylcholinesterase, butyrylcholinesterase, urease, α-amylase, α-glucosidase, and tyrosinase) inhibitory effects of root extracts were tested. Read More

View Article and Full-Text PDF

Biphenylalkoxyamine Derivatives-Histamine H Receptor Ligands with Butyrylcholinesterase Inhibitory Activity.

Molecules 2021 Jun 11;26(12). Epub 2021 Jun 11.

Department of Technology and Biotechnology of Drugs, Jagiellonian University Medical College, Medyczna Str. 9, 30-688 Kraków, Poland.

Neurodegenerative diseases, e.g., Alzheimer's disease (AD), are a key health problem in the aging population. Read More

View Article and Full-Text PDF

Chemical Profiling and Biological Evaluation of Extracts and Essential Oil: An Endemic Plant from Turkey.

Plants (Basel) 2021 Jun 9;10(6). Epub 2021 Jun 9.

Department of Health Sciences, Faculty of Medicine and Health Sciences, University of Mauritius, Réduit 80837, Mauritius.

is a poorly studied, endemic species () of Turkey. For the first time, the biological activities (antioxidant, enzyme inhibition, and cytotoxicity properties) of the hexane, ethyl acetate, methanol, water/methanol, and water extracts and essential oil prepared from aerial parts were assessed. Hydro-methanol (41. Read More

View Article and Full-Text PDF

Release of protein-bound nerve agents by excess fluoride from whole blood: GC-MS/MS method development, validation, and application to a real-life denatured blood sample.

J Chromatogr B Analyt Technol Biomed Life Sci 2021 Aug 15;1179:122693. Epub 2021 Apr 15.

Bundeswehr Institute of Pharmacology and Toxicology, Neuherbergstraße 11, D-80937 Munich, Germany. Electronic address:

In analogy to the fluoride-induced regeneration of butyrylcholinesterase (BChE) inhibited by nerve agents a method was developed and optimized for whole blood samples. Compared to the plasma method, regeneration grade was found to be higher for cyclosarin (GF), i-butylsarin from VR, and n-butylsarin from CVX, but lower for sarin (GB), fluorotabun from tabun (GA), and ethylsarin from VX. Regeneration grade of soman (GD) is the same for both matrices because it is released from serum albumin and not from cholinesterases. Read More

View Article and Full-Text PDF

Selective Pseudo-irreversible Butyrylcholinesterase Inhibitors Transferring Antioxidant Moieties to the Enzyme Show Pronounced Neuroprotective Efficacy In Vitro and In Vivo in an Alzheimer's Disease Mouse Model.

J Med Chem 2021 07 21;64(13):9302-9320. Epub 2021 Jun 21.

Pharmaceutical and Medicinal Chemistry, Institute of Pharmacy and Food Chemistry, Julius Maximilian University of Würzburg, Am Hubland, 97074 Würzburg, Germany.

A series of multitarget-directed ligands (MTDLs) was designed by functionalizing a pseudo-irreversible butyrylcholinesterase (BChE) inhibitor. The obtained hybrids were investigated in vitro regarding their BChE and AChE inhibition, their enzyme kinetics, and their antioxidant physicochemical properties (DPPH, ORAC, metal chelating). In addition, in vitro assays were applied to investigate antioxidant effects using murine hippocampal HT22 cells and immunomodulatory effects on the murine microglial N9 cell line. Read More

View Article and Full-Text PDF

A comprehensive phytochemical, biological, toxicological and molecular docking evaluation of Suaeda fruticosa (L.) Forssk.: An edible halophyte medicinal plant.

Food Chem Toxicol 2021 Aug 16;154:112348. Epub 2021 Jun 16.

School of Pharmacy, Monash University, Jalan Lagoon Selatan, 47500 Bandar Sunway Selangor Darul Ehsan, Malaysia.

Suaeda fruticosa is an edible medicinal halophyte known for its traditional uses. In this study, methanol and dichloromethane extracts of S. fruticosa were explored for phytochemical, biological and toxicological parameters. Read More

View Article and Full-Text PDF

"Clicking" fragment leads to novel dual-binding cholinesterase inhibitors.

Bioorg Med Chem 2021 Jul 7;42:116269. Epub 2021 Jun 7.

National Medicines Institute, Chełmska 30/34, 00-725 Warsaw, Poland; National Centre for Nuclear Research, 05-400 Otwock-Świerk, Poland.

Cholinesterase inhibitors are potent therapeutics in the treatment of Alzheimer's disease. Among them, dual binding ligands have recently gained a lot of attention. We discovered novel dual-binding cholinesterase inhibitors, using "clickable" fragments, which bind to either catalytic active site (CAS) or peripheral anionic site (PAS) of the enzyme. Read More

View Article and Full-Text PDF

Aryl -[ω-(6-Fluoroindol-1-yl)alkyl]carbamates as Inhibitors of Fatty Acid Amide Hydrolase, Monoacylglycerol Lipase, and Butyrylcholinesterase: Structure-Activity Relationships and Hydrolytic Stability.

ACS Omega 2021 May 14;6(20):13466-13483. Epub 2021 May 14.

Institute of Pharmaceutical and Medicinal Chemistry, University of Münster, Corrensstrasse 48, 48149 Münster, Germany.

A series of aryl -[ω-(6-fluoroindol-1-yl)alkyl]carbamates with alkyl spacers of varying lengths between the indole and the carbamate group and with differently substituted aryl moieties at the carbamate oxygen were synthesized and tested for inhibition of the pharmacologically interesting serine hydrolases fatty acid amide hydrolase (FAAH), monoacylglycerol lipase (MAGL), butyrylcholinesterase (BuChE), and acetylcholinesterase (AChE). Furthermore, the chemical stability in an aqueous solution and the metabolic stability toward esterases in porcine liver homogenate and porcine blood plasma were determined. While most of the synthesized derivatives were potent inhibitors of FAAH, a considerable inhibition of MAGL and BuChE was elicited only by compounds with a high carbamate reactivity, as evidenced by a significant hydrolysis of these compounds in an aqueous solution. Read More

View Article and Full-Text PDF

Design and synthesis of garlic-related unsymmetrical thiosulfonates as potential Alzheimer's disease therapeutics: In vitro and in silico study.

Bioorg Med Chem 2021 06 1;40:116194. Epub 2021 May 1.

Department of Chemistry, Agri Ibrahim Cecen University, Agri, Turkey.

Garlic contains a wide range of organosulfur compounds, which exhibit a broad spectrum of biological activities. Amongst the sulfur-containing compounds in garlic, the thiosulfonates are considerably popular in various fields. In light of this, we decided to investigate the enzyme inhibition ability of thiosulfonates. Read More

View Article and Full-Text PDF

Design, synthesis, and evaluation of N-benzylpyrrolidine and 1,3,4-oxadiazole as multitargeted hybrids for the treatment of Alzheimer's disease.

Bioorg Chem 2021 06 17;111:104922. Epub 2021 Apr 17.

Pharmaceutical Chemistry Research Laboratory, Department of Pharmaceutical Engineering & Technology, Indian Institute of Technology (Banaras Hindu University), Varanasi 221005, India. Electronic address:

Novel N-Benzylpyrrolidine hybrids were designed, synthesized, and tested against multiple in-vitro and in-vivo parameters. Among all the synthesized molecules, 8f and 12f showed extensive inhibition against beta-secretase-1 (hBACE-1), human acetylcholinesterase (hAChE) & human butyrylcholinesterase (hBuChE). These molecules are also endowed with significant AChE-peripheral anionic site (PAS) binding capability, blood-brain barrier permeability, potential disassembly of Aβ aggregates along with neuroprotection ability on SHSY-5Y cell lines. Read More

View Article and Full-Text PDF

Bioactive stigmastadienone from Isodon rugosus as potential anticholinesterase, α-glucosidase and COX/LOX inhibitor: In-vitro and molecular docking studies.

Steroids 2021 08 1;172:108857. Epub 2021 May 1.

Department of Pharmaceutical Chemistry, College of Pharmacy, Najran University, Najran, Saudi Arabia.

Natural product is a well-known source of bioactive compounds. Herein, a steroidal compound stigmasta-7,22-diene-3-one (stigmastadienone) has been isolated from Isodon rugosus. The potency of isolated compound has been tested for several in-vitro targets. Read More

View Article and Full-Text PDF

Synthesis of New Biscoumarin Derivatives, In Vitro Cholinesterase Inhibition, Molecular Modelling and Antiproliferative Effect in A549 Human Lung Carcinoma Cells.

Int J Mol Sci 2021 Apr 7;22(8). Epub 2021 Apr 7.

Department of Biochemistry, Faculty of Science, Pavol Jozef Šafárik University in Košice, Šrobárova 2, 041 54 Košice, Slovakia.

A series of novel C4-C7-tethered biscoumarin derivatives (-) linked through piperazine moiety was designed, synthesized, and evaluated biological/therapeutic potential. Biscoumarin was found to be the most effective inhibitor of both acetylcholinesterase (AChE, IC = 6.30 µM) and butyrylcholinesterase (BChE, IC = 49 µM). Read More

View Article and Full-Text PDF

Permeability of Extract Component-Physodic Acid through the Blood-Brain Barrier as an Important Argument for Its Anticancer and Neuroprotective Activity within the Central Nervous System.

Cancers (Basel) 2021 Apr 5;13(7). Epub 2021 Apr 5.

Department of Pharmacognosy, Poznan University of Medical Sciences, Święcicki 4 Str, 60-781 Poznań, Poland.

Lichen secondary metabolites are characterized by huge pharmacological potential. Our research focused on assessing the anticancer and neuroprotective activity of acetone extract (HP extract) and physodic acid, its major component. The antitumor properties were evaluated by cytotoxicity analysis using A-172, T98G, and U-138 MG glioblastoma cell lines and by hyaluronidase and cyclooxygenase-2 (COX-2) inhibition. Read More

View Article and Full-Text PDF

Metabolomic profiling and biological properties of six species: novel perspectives for nutraceutical purposes.

Food Funct 2021 Apr;12(8):3443-3454

Department for Sustainable Food Process, Università Cattolica del Sacro Cuore, Via Emilia Parmense 29122, Piacenza, Italy.

The genus Limonium includes important halophyte plants containing a variety of bioactive compounds of therapeutic interest. In the present work, the untargeted phytochemical profiles of both aerial part and root extracts from six Limonium species namely, L. bellidifolium, L. Read More

View Article and Full-Text PDF

Structure-activity relationships of dually-acting acetylcholinesterase inhibitors derived from tacrine on N-methyl-d-Aspartate receptors.

Eur J Med Chem 2021 Jul 20;219:113434. Epub 2021 Apr 20.

Biomedical Research Center, University Hospital Hradec Kralove, Sokolska 581, 500 05, Hradec Kralove, Czech Republic. Electronic address:

Tacrine is a classic drug whose efficacy against neurodegenerative diseases is still shrouded in mystery. It seems that besides its inhibitory effect on cholinesterases, the clinical benefit is co-determined by NMDAR-antagonizing activity. Our previous data showed that the direct inhibitory effect of tacrine, as well as its 7-methoxy derivative (7-MEOTA), is ensured via a "foot-in-the-door" open-channel blockage, and that interestingly both tacrine and 7-MEOTA are slightly more potent at the GluN1/GluN2A receptors when compared with the GluN1/GluN2B receptors. Read More

View Article and Full-Text PDF

Green toxicology approach involving polylactic acid biomicroplastics and neotropical tadpoles: (Eco)toxicological safety or environmental hazard?

Sci Total Environ 2021 Aug 9;783:146994. Epub 2021 Apr 9.

Post-Graduate Program in Conservation of Cerrado Natural Resources, Goiano Federal Institute, Urutaí, GO, Brazil; Post-Graduate Program in Biodiversity and Biotechnology, Federal University of Goiás, Goiânia, Brazil.

Different and alternative renewable-source materials, commonly called bioplastics, have been proposed due to the high production and consumption of petroleum-derived plastics and to their high toxicity in the biota. However, their toxicological safety has not yet been assessed in a comprehensive way; therefore, their effects on several animal groups remain completely unknown. Thus, we aimed at testing the following hypothesis: the exposure of Physalaemus cuvieri tadpoles to polylaic acid biomicroplastic (PLA BioMP) at environmentally relevant concentrations (760 and 15,020 μg/L) induces physiological changes in them. Read More

View Article and Full-Text PDF

Polyethylene glycol acute and sub-lethal toxicity in neotropical Physalaemus cuvieri tadpoles (Anura, Leptodactylidae).

Environ Pollut 2021 Aug 4;283:117054. Epub 2021 Apr 4.

Biological Research Laboratory, Goiano Federal Institute - Urutaí Campus, Urutaí, GO, Brazil; Post-Graduation Program in Biotechnology and Biodiversity, Federal University of Goiás, Goiânia, GO, Brazil; Graduate Program in Conservation of Cerrado Natural Resources, Goiano Federal Institute, Urutaí, GO, Brazil; Post-Graduation Program in Ecology and Natural Resources Conservation, Uberlândia, MG, Brazil. Electronic address:

Although many polymers are known by their toxicity, we know nothing about the impact of polyethylene glycol (PEG) on anurofauna. Its presence in different products and disposal in aquatic environments turn assessments about its impact on amphibians an urgent matter. Accordingly, we tested the hypothesis that short-time exposure (72 h) of tadpoles belonging to the species Physalaemus cuvieri (Anura, Leptodactylidae) to PEG induces oxidative stress and neurotoxicity on them. Read More

View Article and Full-Text PDF

Health Potential of Clery Strawberries: Enzymatic Inhibition and Anti- Activity Evaluation.

Molecules 2021 Mar 19;26(6). Epub 2021 Mar 19.

Dipartimento di Chimica e Tecnologie del Farmaco, Università degli Studi di Roma "La Sapienza", Piazzale Aldo Moro 5, 00185 Roma, Italy.

Strawberries, belonging to cultivar Clery ( × Duchesne ex Weston) and to a graft obtained by crossing Clery and L., were chosen for a study on their health potential, with regard to the prevention of chronic and degenerative diseases. Selected samples, coming from fresh and defrosted berries, submitted to different homogenization techniques combined with thermal and microwave treatments, had been previously analyzed in their polyphenolic content and antioxidant capacity. Read More

View Article and Full-Text PDF

A Smartphone Camera Colorimetric Assay of Acetylcholinesterase and Butyrylcholinesterase Activity.

Sensors (Basel) 2021 Mar 5;21(5). Epub 2021 Mar 5.

Faculty of Military Health Sciences, University of Defense, Trebesska 1575, CZ-50001 Hradec Kralove, Czech Republic.

Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) can serve as biochemical markers of various pathologies like liver disfunction and poisonings by nerve agents. Ellman's assay is the standard spectrophotometric method to measure cholinesterase activity in clinical laboratories. The authors present a new colorimetric test to assess AChE and BChE activity in biological samples using chromogenic reagents, treated 3D-printed measuring pads and a smartphone camera as a signal detector. Read More

View Article and Full-Text PDF

Quinuclidine-Based Carbamates as Potential CNS Active Compounds.

Pharmaceutics 2021 Mar 20;13(3). Epub 2021 Mar 20.

Department of Chemistry, Faculty of Science, University of Zagreb, Horvatovac 102A, HR-10 000 Zagreb, Croatia.

The treatment of central nervous system (CNS) diseases related to the decrease of neurotransmitter acetylcholine in neurons is based on compounds that prevent or disrupt the action of acetylcholinesterase and butyrylcholinesterase. A series of thirteen quinuclidine carbamates were designed using quinuclidine as the structural base and a carbamate group to ensure the covalent binding to the cholinesterase, which were synthesized and tested as potential human acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitors. The synthesized compounds differed in the substituents on the amino and carbamoyl parts of the molecule. Read More

View Article and Full-Text PDF

Evaluation of Antioxidant and Enzyme Inhibition Properties of L'Hér. Extracts Obtained with Different Solvents.

Molecules 2021 Mar 28;26(7). Epub 2021 Mar 28.

Department of Biology, Science Faculty, Selcuk University, Campus, 42130 Konya, Turkey.

L'Hér methanol extract was studied by NMR and two different LC-DAD-MS using electrospray (ESI) and atmospheric pressure chemical ionization (APCI) sources to obtain a quali-quantitative fingerprint. Forty different phytochemicals were identified, and twenty of them were quantified, whereas the main constituents were dihydro α ionol--[arabinosil(1-6) glucoside] (133 mg/g), dihydro β ionol--[arabinosil(1-6) glucoside] (80 mg/g), β-sitosterol (49 mg/g), and isorhamnetin-3--rutinoside (26 mg/g). was extracted with different solvents-namely, water, methanol, dichloromethane, and ethyl acetate-and the extracts were assayed using different in vitro tests. Read More

View Article and Full-Text PDF

Chemical Composition and Pharmacological Evaluation and of Toddalia asiatica (Rutaceae) Extracts and Essential Oil by in Vitro and in Silico Approaches.

Chem Biodivers 2021 Apr 19;18(4):e2000999. Epub 2021 Mar 19.

Department of Health Sciences, Faculty of Medicine and Health Sciences, University of Mauritius, Moka, Réduit, 80837, Mauritius.

Toddalia asiatica (L.) Lam. is extensively used in traditional medicinal systems by various cultures. Read More

View Article and Full-Text PDF