Molar absorption coefficients for the reduced Ellman reagent: reassessment

Eyer, Peter; Worek, Franz; Kiderlen, Daniela; Šinko, Goran; Štuglin, Anita; Simeon-Rudolf, Vera; Reiner, Elsa

doi:10.1016/s0003-2697(02)00506-7

Cited by 452 publications

(311 citation statements)

References 10 publications

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“…Absorption spectra of the reduced Ellman reagent have been studied with respect to the effect of temperature on the absorbance maxima. Molar absorption coefficients have been reassessed and wavelengths for the assay suggested with respect to the interference of haemoglobin absorption on the assay (46) ) inhibits only 5 % to 10 % of the erythrocyte AChE, while the BChE U-variant is inhibited 98 % and the A-variant 74 %. Using ethopropazine as a selective inhibitor, an improved determination of AChE activities in whole blood was suggested, that is suitable for measuring low AChE activities in the whole blood of an OP-poisoned individual (48).…”

Section: Methods For Detecting Organophosphates By Means Of Cholinestmentioning

confidence: 99%

Mechanisms of Organophosphate Toxicity and Detoxication with Emphasis on Studies in Croatia

Reiner

Radić

Simeon-Rudolf

2007

Archives of Industrial Hygiene and Toxicology

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This review comprises studies on the mechanisms of toxicity and detoxication of organophosphorus (OP) compounds done in Croatia in different research areas. One area is the synthesis of antidotes against OP poisoning and their in vivo testing in experimental animals. In vitro studies included in this review focus on the mechanisms of reversible inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), protection of cholinesterases from inhibition by OPs, and reactivation of phosphylated cholinesterases. The third area comprises distribution profiles of BChE and paraoxonase (PON) phenotypes in selected population groups and the detection of OPs and metabolites in humans. Finally, methods are described for the detection of OP compounds in human blood and other media by means of cholinesterase inhibition.

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Section: Methods For Detecting Organophosphates By Means Of Cholinestmentioning

confidence: 99%

Mechanisms of Organophosphate Toxicity and Detoxication with Emphasis on Studies in Croatia

Reiner

Radić

Simeon-Rudolf

2007

Archives of Industrial Hygiene and Toxicology

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“…Spectrophotometric detection of 5-thio-2-nitrobenzoate (TNB 2-) was performed at the wavelength of 412 nm using the molar extinction coefficient of TNB 2-of 14150 M -1 cm -1 [28]. Before the in vitro study the inhibitor was dissolved in dimethyl sulfoxide.…”

Section: In Vitro Study Of Ache and Bche Inhibitionmentioning

confidence: 99%

Synthesis and the activity assessment of adamantylcontaining thiazolium inhibitors of butyrylcholinesterase

Ocheretniuk

Kobzar

Kozachenko

et al. 2017

J. org. pharm. chem.

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Cholinesterase inhibitors can be used for treatment of neuropsychiatric symptoms and functional impairments in neurodegenerative pathologies such as Alzheimer's and Parkinson's diseases.Aim. To synthesize and assess the inhibitory activity of adamantyl-containing 5-substituted N-benzyl and N-phenacylthiazolium salts against butyrylcholinesterase and acetylcholinesterase.Results and discussion. The synthesis of 3-aroylmethyl-and 3-arylmethyl-5-(2-acyloxyethyl)-4-methylthiazolium salts included preparation of 5-acyloxyethyl thiazole derivatives by the reaction of 5-(2-hydroxyethyl)-4-methyl-1,3-thiazole with the corresponding adamantoyl-or adamantylacetyl chlorides. The derivatives of 5-acyloxyethyl thiazole were quaternized in the reaction with benzyl or phenacyl halides. The studies in vitro have shown that the compounds synthesized inhibit butyrylcholinesterase with IC 50 values in the micromolar range. Some of them exhibited selectivity over acetylcholinesterase. The molecular docking was performed for understanding the mechanisms of the enzyme-inhibitor complex formation.Experimental part. The synthesis of the intermediate and target compounds was carried out by the classical methods. The structures of compounds were proven by NMR 1 H-spectroscopy and elemental analysis. The methods of enzymatic kinetics were used for determination of the inhibitory effects of the compounds synthesized. Calculations by molecular docking were carried out using Autodock 4.2 program.Conclusions. 3-Aroylmethyl-and 3-arylmethyl-5-(2-acyloxyethyl)-4-methylthiazolium salts with adamantylcontaining substituents in position 5 can selectively inhibit butyrylcholinesterase compared to their effect on acetylcholinesterase.Key words: butyrylcholinesterase; acetylcholinesterase; adamantan; inhibitor; thiazolium salt; molecular docking А. Д. Очеретнюк, О. Л. Кобзар, О. П. Козаченко, В. С. Броварець, А. І. Вовк Синтез та оцінка активності адамантиловмісних тіазолієвих інгібіторів бутирилхолінестеразиВідомо, що інгібітори холінестераз можуть використовуватись для лікування нейродегенеративних захво-рювань, таких як хвороба Альцгеймера і хвороба Паркінсона.Мета роботи. Метою роботи був синтез та оцінка активності адамантиловмісних 5-заміщених N-бензильних та N-фенацильних солей тіазолію як інгібіторів бутирилхолінестерази і ацетилхолінестерази.Результати та їх обговорення. Синтези 3-ароїлметил-і 3-арилметил-5-(2-ацилоксіетил)-4-метилтіазолієвих солей включали одержання 5-ацилоксіетильних похідних тіазолу при взаємодії 5-(2-гідроксіетил)-4-метил-1,3-тіазолу з відповідними адамантоїл-чи адамантилацетилхлоридами, які надалі кватернізували в реак-ції з бензил-або фенацилгалогенідами. Результати дослідження in vitro показали, що синтезовані сполуки інгібують бутирилхолінестеразу зі значеннями ІС 50 в мікромолярному діапазоні. Деякі з них демонструва-ли селективність дії у порівнянні з інгібуванням ацетилхолінестерази. Для з'ясування механізмів форму-вання комплексів інгібіторів з бутирилхолінестеразою було проведено молекулярний докінг.Експеримента...

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“…V 0 was calculated using the DTNB extinction coefficient of 1.38 × 10 -4 M -1 cm -1 at 37 °C. 50 The background hydrolysis (K uncat ) was determined by initial rate analysis and extrapolated to zero-buffer concentration. When inhibitors were soluble in solvent different from phosphate buffer, blank kinetics with solvent instead drug solution were added in the experimental protocol.…”

Section: Insertion Of Scfv Gene Construct In a New Vector And Cell Hostsmentioning

confidence: 99%

Selection of a human butyrylcholinesterase-like antibody single-chain variable fragment resistant to AChE inhibitors from a phage library expressed inE. coli

Podestà¹,

Rossi²,

Massarelli³

et al. 2014

mAbs

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Molar absorption coefficients for the reduced Ellman reagent: reassessment

Cited by 452 publications

References 10 publications

Mechanisms of Organophosphate Toxicity and Detoxication with Emphasis on Studies in Croatia

Mechanisms of Organophosphate Toxicity and Detoxication with Emphasis on Studies in Croatia

Synthesis and the activity assessment of adamantylcontaining thiazolium inhibitors of butyrylcholinesterase

Selection of a human butyrylcholinesterase-like antibody single-chain variable fragment resistant to AChE inhibitors from a phage library expressed inE. coli

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