Використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію

The study considers the possibility of using 3,3',5,5'-tetramethylbenzidine (TMB) as an indicator in the enzymatic analysis for the quantitative determination of quaternary ammonium compounds on the example of ethonium. The feasibility of using TMB as an indicator in the kinetic photometri...

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Published in:Журнал органічної та фармацевтичної хімії
Date:2024
Volume:22
Issue:4
Pages:36-42
ISSN:2518-1548
Author Affiliations:
  • Olena V. Kovalska — National University of Pharmacy of the Ministry of Health of Ukraine
  • Mykola Ye. Blazheyevskiy — National University of Pharmacy of the Ministry of Health of Ukraine
  • Vladyslav V. Diadchenko — Military Institute of Armored Forces of the National Technical University “Kharkiv Polytechnic Institute”
Main Authors: Kovalska, Olena V., Blazheyevskiy, Mykola Ye., Diadchenko, Vladyslav V.
Format: Article
Language:English
Published: National University of Pharmacy 2024
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Online Access:https://ophcj.nuph.edu.ua/article/view/321795
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Journal of Organic and Pharmaceutical Chemistry
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author Kovalska, Olena V.
Blazheyevskiy, Mykola Ye.
Diadchenko, Vladyslav V.
author_facet Kovalska, Olena V.
Blazheyevskiy, Mykola Ye.
Diadchenko, Vladyslav V.
author_institution_txt_mv [ { "author": "Olena V. Kovalska", "institution": "National University of Pharmacy of the Ministry of Health of Ukraine", "orcid": "" }, { "author": "Mykola Ye. Blazheyevskiy", "institution": "National University of Pharmacy of the Ministry of Health of Ukraine", "orcid": "" }, { "author": "Vladyslav V. Diadchenko", "institution": "Military Institute of Armored Forces of the National Technical University “Kharkiv Polytechnic Institute”", "orcid": "" } ]
author_sort Kovalska, Olena V.
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container_issue 4
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container_title Журнал органічної та фармацевтичної хімії
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description The study considers the possibility of using 3,3',5,5'-tetramethylbenzidine (TMB) as an indicator in the enzymatic analysis for the quantitative determination of quaternary ammonium compounds on the example of ethonium. The feasibility of using TMB as an indicator in the kinetic photometric method has been confirmed. Kinetic curves showing the relationship between the optical density and the ethonium concentration have been constructed. The reaction rates of acetylcholinesterase inhibition by ethonium have been estimated using the tangents of the angles of these curves with TMB as an indicator. The degree of enzyme inhibition has been calculated, and a linear relationship between the ethonium concentration and the degree of inhibition has been determined. This method was applied to determine the ethonium content in 0.1% ethonium gel. The relative standard deviation of the method does not exceed 2.5 %. The approach suggested offers a reliable and accurate method for the quantitative analysis of ethonium in dosage forms.
doi_str_mv 10.24959/ophcj.24.321795
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fulltext ISSN 2308-8303 (Print) / 2518-1548 (Online) 36 Original Research http://ophcj.nuph.edu.ua UDC 577.15:5615.2:547.2333.4 M. Ye. Blazheyevskiy1, O. V. Kovalska1, V. V. Diadchenko2 1 National University of Pharmacy of the Ministry of Health of Ukraine, 53 Hryhorii Skovoroda str., 61002 Kharkiv, Ukraine 2 Military Institute of Armored Forces of the National Technical University “Kharkiv Polytechnic Institute”, 2 Kyrpychova str., 61002 Kharkiv, Ukraine The Use of Tetramethylbenzidine as an Indicator in the Enzymatic Quantitative Determination of Ethonium Abstract The study considers the possibility of using 3,3’,5,5’-tetramethylbenzidine (TMB) as an indicator in the enzymatic analysis for the quantitative determination of quaternary ammonium compounds on the example of ethonium. The feasibility of using TMB as an indicator in the kinetic photometric method has been confirmed. Kinetic curves showing the relationship between the optical density and the ethonium concentration have been constructed. The reaction rates of acetylcholinesterase inhibi- tion by ethonium have been estimated using the tangents of the angles of these curves with TMB as an indicator. The degree of enzyme inhibition has been calculated, and a linear relationship between the ethonium concentration and the degree of inhibition has been determined. This method was applied to determine the ethonium content in 0.1 % ethonium gel. The relative standard deviation of the method does not exceed 2.5  %. The approach suggested offers a reliable and accurate method for the quantitative analysis of ethonium in dosage forms. Keywords: ethonium; quaternary ammonium compounds; cholinesterase; acetylcholine M. Є. Блажеєвський1, O. В. Ковальська1, В. В. Дядченко2 1 Національний фармацевтичний університет Міністерства охорони здоров’я України, вул. Григорія Сковороди, 53, м. Харків, 61002, Україна 2 Національний технічний університет «Харківський політехнічний iнститут», вул. Кирпичова, 2, м. Харків, 61002, Україна Використання тетраметилбензидину як індикатора в ензиматичному методі кількісного визначення етонію Анотація У дослідженні розглянуто можливість використання 3,3’,5,5’-тетраметилбензидину (ТМБ) як індикатора в ензиматично- му аналізі для кількісного визначення четвертинних амонієвих сполук на прикладі етонію. Підтверджено можливість застосування ТМБ як індикатора в кінетичному фотометричному методі. Побудовано кінетичні криві, що демонстру- ють залежність між оптичною густиною та концентрацією етонію. Швидкість реакції інгібування ацетилхолінестерази етонієм було оцінено за тангенсами кутів цих кривих, із цим ТМБ використано як індикатор. Розраховано ступінь інгібу- вання ферменту, а також визначено лінійну залежність між концентрацією етонію та ступенем інгібування. Цей метод за- стосовували для визначення вмісту етонію в 0,1 % гелі етонію. Відносне стандартне відхилення методу не перевищує 2,5 %. Запропонований підхід забезпечує надійний та точний метод кількісного аналізу етонію в лікарських формах. Ключові слова: етоній; холінестераза; ацетилхолін; четвертинні амонієві сполуки Citation: Blazheyevskiy, M. Ye.; Kovalska, O. V.; Diadchenko, V. V. The Use of Tetramethylbenzidine as an Indicator in the Enzymatic Quantitative Determination of Ethonium. Journal of Organic and Pharmaceutical Chemistry 2024, 22 (4), 36 – 42. https://doi.org/10.24959/ophcj.24.321795 Received: 15 August 2024; Revised: 25 November 2024; Accepted: 11 December 2024 Copyright© 2024, M. Ye. Blazheyevskіy, O. V. Kovalska, V. V. Diadchenko. This is an open access article under the CC BY license (http://creativecommons.org/licenses/by/4.0). Funding: The authors received no specific funding for this work. Conflict of interests: The authors have no conflict of interests to declare. ISSN 2308-8303 (Print) / 2518-1548 (Online) 37 Journal of Organic and Pharmaceutical Chemistry 2024, 22 (4) ■ Introduction 3,3′,5,5′-Tetramethylbenzidine (TMB) is a wi- dely used chromogen that is valued for its non- carcinogenic nature and, upon oxidation, gives pro- ducts with high absorption coefficients. This ma- kes TMB a key component in enzyme-based as- says, offering superior sensitivity and low de- tection limits compared to many commercially available chromogenic reagents. Notably, TMB is the most widely used chromogenic substrate in ELISA procedures that use horseradish per- oxidase conjugates. The TMB substrate develops a soluble blue reaction product that can be read at 370 or 655 nm [1]. Additionally, many recent reports support and justify the wide incorporation of TMB into ana- lytical practice [2]. Thus, Sil et al. proposed a one- step simple method for nanolevel detection of as- corbic acid based on the inhibitory activity of ascor- bic acid on horseradish peroxidase and hydrogen peroxide supported by redox properties of TMB [3]. TMB was also used for the uric acid detection with MnO2 nanosheets. In mildly acidic condi- tions, MnO2 oxidizes TMB to its blue oxidation product applied to human urine samples, achiev- ing recovery rates of 93.1 – 102.4 % with a rela- tive standard deviation below 3 % [4]. In 2022, Zhang et al. developed a colorimetric detection system for Cu2+ ions based on TMB and Ag(S2O3)2 3– in an aqueous solution. Unlike Ag nanoparticles, which could not oxidize TMB, Ag(S2O3)2 3– cata- lyzed the reaction effectively, with optimal con- ditions achieved at 800 μM for TMB, 400 μM for Na2S2O3, for 40 min, and at 25 °C. This system, with a detection range of 1 – 100 μM and a limit of 100 nM, shows promise for monitoring the wa- ter quality [5]. Important biogenic thiols, such as glutathione (GSH), cysteine (CySH), and ho- mocysteine (HcySH), were analyzed using TMB as a chromogen in a simple spectrophotometric method. Detection limits for GSH, CySH, and HcySH were 1.04, 0.82, and 2.09 μM, respective- ly, with successful application of the method to human serum samples, achieving recovery rates of 97 – 112 % [6]. Chandra and colleagues report- ed the synthesis of fluorescent carbon quantum dots (M-CQDs) through a simple hydrothermal treatment of mustard seeds [7]. M-CQDs demon- strated peroxidase-like activity, catalyzing the oxidation of TMB in the presence of H2O2, thus mimicking the natural horseradish peroxidase activity. The process enabled the colorimetric detection of H2O2 in the range of 0.02 – 0.20 mM with a detection limit of 0.015 mM. Additional- ly, reduction of oxidized TMB with ascorbic acid allowed for a selective and sensitive detection of ascorbic acid in the range of 10 – 70 μM, with a detection limit of 3.26 μM. The method was suc- cessfully applied to the ascorbic acid detection in fresh fruits. Further advancements in TMB- based systems include the application of oxidized TMB nanobelts enhancing the colorimetric and paper-based sensing of H2O2 [8], peroxidase-like nanoenzymes, such as Fe3O4 nanoparticles [9], CoFe2O4 nanoparticles [10], single-atom iron na- nozyme [11], MOF-818 nanozyme containing tri- nuclear copper centers [12], Ce2(WO4)3 nano- sheets [13], Fe3O4@AuNPs [14], etc., all enhanc- ing the H2O2 detection sensitivity through the for- mation of oxidized TMB. The versatility of TMB is reflected in its increasing popularity, with 2,889 publications between 2015 and 2024 in the Scopus® database (www.scopus.com). Notably, the number of publications surged by 1.5 times bet- ween 2019 and 2024, demonstrates the growing impact of TMB on analytical chemistry (Figure 1). Previously, our laboratory developed a novel biochemical kinetic-spectrophotometric method for detecting cholinesterase inhibitors from the group of quaternary ammonium compounds (QACs) using the oxidation of p-phenetidine by hydro- gen peroxide as the indicator reaction [15], in- cluding a recent paper reporting the quantifica- tion of Ethonium [16]. Considering all the advan- tages that TMB can provide for the quantifica- tion of this group of pharmaceuticals and its cen- tral role in the development of sensitive and ef- fective analytical methods, in this study we pre- sent the results of using TMB as a chromogen for the quantitative analysis of the QAC Etho- nium in a 0.5 % gel formulation. The enzyme- kinetic method based on the inhibition of cho- linesterase activity and the use of oxidation of TMB with hydrogen peroxide as an indicator re- action was applied. ■ Materials and methods Reagents and equipment The following reagents were used in the study: • ETONIY® (Aethonium) powder (substance) produced by OJSC Farmak, Kyiv, Ukraine. C30H62Cl2N2O4; CAS: 21954-74-5; MW 585.736 g mol–1; • 0.5 % Ethonium gel, 50 mL, batch No. 74 (Apr 2023) manufactured by APTEKA PAVLOVA ISSN 2308-8303 (Print) / 2518-1548 (Online) 38 Журнал органічної та фармацевтичної хімії 2024, 22 (4) Ltd (Odesa, Ukraine) with the composition of ethonium (active pharmaceutical ingredi- ent) 0.5 g; glycerol – 20.0 g; propylene glycol – 20.0 g; PEG 400 – 50.0 g; PEG 1500 – 10.0 g; purified water – 10.0 ml. The content of the active substance, according to the certificate, is 4.4525 % (w/w); • 3,3’,5,5’-Tetramethylbenzidine dihydrochlo- ride (TMB), C16H20N2·2HCl; 98.5  % (Sigma- Aldrich); MW 313.27 g mol–1; • Disodium hydrogen phosphate dodecahydra- te (Na2HPO4∙12H2O), puriss. p.a. (“ReaChem”, Kharkiv, Ukraine); • Stabilized hydrogen peroxide, 30 – 40  % solution, puriss. p.a., (LLC Inter-Synthes, Boryslav, Uk- raine) with the content of hydrogen peroxide de- termined using permanganatometry according to the State Pharmacopoeia of Ukraine [17]; • Acetylcholine chloride (Pharm Grade), 0.2 g per amp/5 mL, manufactured by the State Science Center of Virology and Biotechnolo- gy “Vector”; • A dry cholinesterase (EC 3.1.1.8) powder from horse serum (SMU “Biomed”), 80 mg in an ampoule (VI class, activity 28 AU mg–1). The catalytic activity of 1 activity unit (AU) is manifested in such an amount of this en- zyme preparation that converts 1 μmol of the substrate in 1 min under specified reaction conditions. • Ethanol 96 % v/v (USP, BP, Ph.Eur.) pure, pharma grade. • High-purity double distilled water was used throughout the experiment. The pH measurements were performed with a combined glass electrode (SP20B) together with an EAL-1М3.1 reference standard silver chloride electrode. The absorbance measurements were perfor- med on an SF-26 spectrophotometer (λ = 420 nm, l = 10 mm). Preparation of solutions 0.2 M Phosphate buffer solution (pH 8.35) Disodium hydrogen phosphate dodecahydra- te (35.75 g) was dissolved in a 500 mL flask us- ing double-distilled water. 0.1 M Solution of hyd- rochloric acid (19 mL) was then added. The pH of the final solution was controlled potentiomet- rically. 0.02 M TMB solution The substance of TMB (0.6265 g) was dissol- ved in 40 % (v/v) ethanol solution in a 100 mL vo- lumetric flask and diluted to the volume with the same solvent. The mixture was heated to 45 °C for complete dissolution and was stored in a tight- ly closed dark glass bottle in a cool place. 10 % Hydrogen peroxide solution The solution was prepared from a 30 – 40 % so- lution of hydrogen peroxide by dilution with the re- quired amount of double distilled water. The con- tent of hydrogen peroxide in a 10 % working so- lution was determined by permanganatometry. Cholinesterase (ChE) solution The accurately weighed content of an ampoule containing the cholinesterase powder (80 mg) was dissolved in double-distilled water (20.0 mL) when heating gently on a water heater. The shelf life of the solution was 1 day. Acetylcholine chloride (ACh) solution The solution with the initial concentration of 5.4·10–3 mol L–1 was prepared by dissolving the ampoule content (0.2 g of acetylcholine) in 200 mL of double-distilled water. For this purpose, the ampoule was opened, and 4.0 mL of water was pi- petted and added to the ampoule, and then shak- en until acetylcholine was completely dissolved. 41 44 74 64 113 127 166 207 296 314 310 388 453 515 118 2010 2011 2012 2013 2014 2015 2016 2017 2018 2019 2020 2021 2022 2023 2024 2025 P a p e rs N o . Year 24 Figure 1. The number of papers per year for the query “3,3’,5,5’-tetramethylbenzidine” (title, abstract, keywords) according to the Scopus® database (2010-2025) ISSN 2308-8303 (Print) / 2518-1548 (Online) 39 Journal of Organic and Pharmaceutical Chemistry 2024, 22 (4) Then the solution was transferred into a 200 mL volumetric flask and diluted to the volume with double-distilled water. 0.1 % Ethonium solution 1.0000 g of the Ethonium substance was dis- solved in a 1 L flask using double-distilled wa- ter, the solution was heated to 40 – 45°C, 9.0 g of sodium chloride was added to the solution, and diluted to the volume. Stock Solution of Ethonium (ET), 1×10–4 M The accurately weighed powder of the Etho- nium substance (0.058574 g) was dissolved in 500 mL of double-distilled water in a 1000 mL volumetric flask. The solution was diluted to the volume with the same solvent at +20 °C and mixed thoroughly. Ethonium Work Standard (WS) solution, 1·10–5 M The accurately weighed powder of the etho- nium substance (0.58574 g) was dissolved in 500 mL of ethanol solution in double-distilled water (EtOH/H2O 30:70 v/v) in a 1 L volumetric flask and diluted to the volume at +20 °C and mixed thoroughly. Using a pipette, 10 mL of the result- ing solution was taken and transferred to a 1 L volumetric flask and diluted to the volume with double-distilled water. Ethonium WS Solution, 1×10–6 M A 10 mL aliquot of Stock Solution of the drug (1×10–4 mol L–1) was transferred into a 1 L volu- metric flask and diluted to the volume with dou- ble-distilled water at +20 °C. The procedure for constructing the ki- netic curves Part 1 – working experiments «ACh + (ChE + ET)» The buffer solution (2.00 mL, pH 8.35) was added to each of the five 20 mL graduated test tubes with a ground joint stopper. Then 0.50, 1.50, 3.00, 4.50, and 6.00 mL of the ethonium 1×10–6 M WS solution was added to the test tu- bes, followed by 0.50 mL of the cholinesterase so- lution. The content was thoroughly shaken, and the test tubes were kept in a thermostat at +38 ºС for 10 min. After that 1.0 mL of acetylcholine so- lution and 5.90, 4.90, 1.90, 0.40 mL, and 5.4 mL of double-distilled water were added to the five test tubes, respectively. The content was mixed thor- oughly and incubated again for 10 min at 38 ºС. Then, a 10 % hydrogen peroxide solution (3.20 mL) was added to each of the test tubes, and the latter were incubated for 10 min at +38 ºС. After that 3.0 mL of 96 % ethanol and 0.50 mL of the TMB solution were added, and the solution was shak- en thoroughly and scanned photometrically on a spectrophotometer at a wavelength of 420 nm in a 1 cm cuvette over a 15-minute period. The phos- phate buffer was used as a reference solution. The relative rate of the reaction [[(ChE + ET) + ACh] +H2O2 + TMB] (tgα (Inh), min–1) was deter- mined as the slope of a linear section of the “op- tical density (A) vs time (t, min)” kinetic curve. Part 2 – control experiments #1 “ACh” The buffer solution (2.00 mL, pH 8.35) was added to a 20 mL graduated test tube, followed by 6.9 mL of double-distilled water, 1.0 mL of the acetylcholine solution, and 3.2 mL of the hy- drogen peroxide solution. The solution was in- cubated at 38 ºС for 10 min. After that 3.0 mL of 96 % ethanol and 0.5 mL of the TMB solution were added to the test tube. The solution was shaken thoroughly and scanned photometrically on a spec- trophotometer at a wavelength of 420 nm in a 1 cm cuvette over a 15-minute period. The phosphate buffer was used as a reference solution. According to the plotted “optical density (A) vs time (t, min)” kinetic curve, the relative rate of the reaction [(ACh + H2O2) + TMB] was determined as a slo- pe of a linear section of the curve (tgα (ACh), min–1). Part 3 – control experiments #2 “Ach+ChE” 2.0 mL of the buffer solution, 6.4 mL of double- distilled water, 0.5 mL of the cholinesterase so- lution, and 1.0 mL of the acetylcholine solution were successively added to a 20 mL test tube with a ground joint stopper and then thermostated at 38 ºС for 10 min. Further 3.2 mL of the hydro- gen peroxide solution was added, and the mix- ture was thoroughly shaken and thermostated again at 38 ºС for 10 min. After that 3.0 mL of 96 % ethanol and 0.5 mL of the TMB solution were added. Then the solution was scanned photomet- rically on a spectrophotometer at a wavelength of 420 nm in a 1 cm cuvette over a 15 min period. The phosphate buffer was used as a reference solution. According to the plotted “optical den- sity (A) vs time (t, min)” kinetic curve, the rela- tive rate of the reaction [(ChE + ACh) + H2O2 + TMB] was determined as a slope of a linear sec- tion of the curve (tgα (ACh + ChE), min–1). The relative rates of the reactions (expressed as tangents of the angles of slope) were used to calculate the inhibition degree of the enzymatic hydrolysis of ACh (U,  %) in the presence of etho- nium according to the following equation: U(%) = [tg�(Inh) – Ach + ChE)tg�� ] × 100 % [tg�� ) – Ach + ChE)tg�� ]Ach where tgα (Inh) (min–1) is the relative reac- tion rate of the TMB oxidation by peroxyacetic ISSN 2308-8303 (Print) / 2518-1548 (Online) 40 Журнал органічної та фармацевтичної хімії 2024, 22 (4) acid formed during the perhydrolysis of unre- acted ACh in the working experiment at various concentrations of the inhibitor (ET); tgα (Ach) (min–1) is the relative reaction rate of the TMB oxidation by peroxyacetic acid for- med in the reaction of the ACh perhydrolysis in the absence of the inhibitor and ChE (control ex- periment #1); tgα (Ach + ChE) (min–1) the relative reaction rate of the TMB oxidation by peroxyacetic acid formed in the reaction of the perhydrolysis of unreacted ACh in the presence of ChE and in the absence of the inhibitor (ET) (control experi- ment #2). The calculated values of U ( %) were used to plot the “inhibition degree (U,  %) vs ethonium concentration (c, ng mL–1)” calibration graph (Figure 3). ■ Results and discussion Previously, a study was conducted to analyze the parameters that may affect the effectiveness of the approach proposed [18]. This allowed us to determine the optimal working conditions and concentrations of the reagents used in this study. Kinetic curves were plotted using experimen- tal data showing the relationship between the op- tical density and time, as presented in Figure 2. The calibration graph (Figure 3) was con- structed in the coordinates of the inhibition de- gree (U,  %) vs the concentration (c, ng mL–1). From Figure 3, the linear dependence of the inhibition degree on the concentration of the in- hibitor was observed in the interval of 4 – 60 % (R = 0.9) corresponding to the concentration of the inhibitor 17 – 200 ng mL–1. The LOQ was defined as the concentration corresponding to a 4 % de- gree of inhibition, i.e., 17 ng mL–1. The method for the quantitative deter- mination of ethonium with TMB as an indi- cator in a “Ethonium 0.5 % gel” formulation 0.1 g (accurate weight) of the ethonium gel was dissolved in 1000 mL of double-distilled wa- ter. Then 2.0 mL of the phosphate buffer solution, 5.0 mL of the gel solution, and 0.5 mL of the ChE solution were successively added to a 20 mL test tube. The mixture was thoroughly shaken and incubated for 10 min at 38 ºС. After that 1.0 mL of the ACh solution and 1.4 mL of double-distilled water were added, and the content was carefully mixed and incubated again for 10 min at 38 ºС. Then, 3.2 mL of the hydrogen peroxide solution was added, and the mixture was incubated again at 38 ºС for 10 min. After that 3.0 mL of 96 % etha- nol and 0.5 mL of the TMB solution were added to the test tube. The optical density of the solu- tion was measured at 420 nm in a 1 cm cuvette for 15 min. According to the plot of the “optical density vs time” dependence, the tangent of the angle of slope for the linear section tgα (Inh) was found in min–1. In parallel, two more experiments were carried out. One of them involved acetyl- choline and cholinesterase without the inhibitor, another one was performed without the use of cho- linesterase enzyme (control experiments #1 and #2 described in the previous section). As a result, the 0 0,1 0,2 0,3 0,4 0,5 0 10 20 30 40 A b s o rb a n c e Time, min Ach Ach + ChE 1 2 3 4 5 Figure 2. Kinetic curves of the conjugated oxidation of TMB with hydrogen peroxide in the presence of mixtures ACh + ChE + Inh (1 – 5). c (Ach) = 3.3×10–4 mol L–1; w(H2O2) =1.92 %; c (AChE) = 0.24 mg mL–1. w (ET): 17 ng mL–1 (1); 50 ng mL–1 (2); 100 ng mL–1 (3); 150 ng mL–1 (4); 200 ng mL–1 (5); c (ТМB) = 6.25×10–4 mol L–1; control experiments “Ach + ChE”, control experiments “ACh” ISSN 2308-8303 (Print) / 2518-1548 (Online) 41 Journal of Organic and Pharmaceutical Chemistry 2024, 22 (4) other two tangents tgα (Ach + ChE) and tgα (ACh), respectively, were determined. The content of ethonium in the gel formula- tion, (w,  %) was calculated by the formula: w (%, w/w) = 0.00059574[tg tg� ��( ) – Ach + ChE)X ]×100 % g× ][tg tg� ��(Ach) – Ach + ChE) where 0.00059574 – is the mass of Ethonium in a 10.00 mL aliquot of the Stock Solution of the drug, g; g – is the mass of the ethonium gel sample taken for the analysis, g; tgα (X) – is the relative reaction rate (the tan- gent of the angle of slope of the kinetic curve), in the working experiment with the sample solu- tion of the drug studied (the Ach – ChE – Inh (Х) + (H2O2 – TMB) system), min–1; tgα (Ach + ChE) – is the relative reaction rate in the absence of the inhibitor (ET) (the tangent of the angle of slope of the kinetic curve) in the Ach – СhЕ + (H2O2 – TMB) system, min–1; tgα (ACh) – is the relative reaction rate (the tangent of the angle of slope of the kinetic curve) in the working experiment without the use of the inhibitor and cholinesterase, (the Ach – ChE – Inh (WSS) + (H2O2 – TMB) system), min–1. ■ Conclusions This paper proves the possibility of using tetramethylbenzidine as a promising indicator substance for the quantitative determination of surface-active substances of the class of quater- nary ammonium compounds. The quantitative content of Ethonium as an active ingredient in the 0.5 % gel formulation and in the 0.1 % solution prepared ex tempore was determined by the enzyme-kinetic method using the effect of inhibiting the activity of the enzyme cholinesterase. The inhibition was es- timated by the residual acetylcholine using the indicator reaction of the 3,3’,5,5’-tetramethyl- benzidine oxidation with peracetic acid formed in the perhydrolysis of acetylcholine. As a re- sult, RSD did not exceed 2.5 % with accuracy δ = –0.45….–2.00  % (δ < RSD). The LOQ value was 17 ng mL–1. y = 0.3092x – 2.9353 R = 0.9935² 0 10 20 30 40 50 60 70 0 50 100 150 200 250 D e g re e o f in g ib it io n , % Etonium c 1 oncetration, ng mL – Figure 3. The dependence of the degree of inhibition on the concentration of Ethonium in the system (ACh + (ChE + Ethonium), determined by the indicator reaction of the conjugated oxidation of TMB with hydrogen peroxide in the presence of residual acetylcholine. c (ACh) = 3.3×10–4 mol L–1; w (H2O2) = 1.92 %; c (AChE) = 0.24 mg mL–1, c (TMB) = 6.25×10–4 mol L–1 Table. The results of the analysis of 0.5 % ethonium gel and 0.1 % solution according to the proposed procedure by the kinetic- spectrophotometric enzyme method The substance analyzed ET found (x ± Δx), %a RSD, % The quality certificate data,  % Accuracy, (δ,  %)b 0.5 % Ethonium gel, 50 mL, manufactured by APTEKA PAVLOVA Ltd (Odesa, Ukraine) 0.443 ± 0.014 2.54 0.445 –0.45 0.100 % Ethonium solution, 1000 mL, prepared ex tempore 0.098 ± 0.003 2.46 0.100 –2.00 Notes: a Mean of 5 measurements (P = 0.95); b δ = (x – μ) × 100  % × μ–1; μ is the actual content of ET according to the Certificate ISSN 2308-8303 (Print) / 2518-1548 (Online) 42 Журнал органічної та фармацевтичної хімії 2024, 22 (4) ■ References 1. 3,3′,5,5′-Tetramethylbenzidine. https://www.sigmaaldrich.com/UA/en/product/sigma/t0440 (accessed Oct 11, 2024). 2. Frey, A.; Meckelein, B.; Externest, D.; Schmidt, M. A. A stable and highly sensitive 3,3′,5,5′-tetramethylbenzidine-based substrate reagent for en- zyme-linked immunosorbent assays. Journal of Immunological Methods 2000, 233 (1), 47 – 56. https://doi.org/10.1016/S0022-1759(99)00166-0. 3. Sil, B. K.; Jamiruddin, M. R.; Haq, M. A.; Aekwattanaphol, N.; K, P. A.; Salendra, L.; Paliwal, H.; Paul, P. K.; Buatong, W.; Sricha- na, T. Nanolevel of detection of ascorbic acid using horse-radish peroxidase inhibition assay. Heliyon 2024, 10 (10), e30715. https://doi.org/10.1016/j.heliyon.2024.e30715. 4. Huang, L.; Qin, Sh.; Xu, Y.; Shi, Ch.; Jin, Y.; Wang, Y. Enzyme-free colorimetric detection of uric acid on the basis of MnO2 nanosheets-mediated oxidation of 3,3′,5,5′-tetramethylbenzidine. Microchemical Journal, 2023, 190, 108719. https://doi.org/10.1016/j.microc.2023.108719. 5. Zhang, Z.; Zhao, W.; Hu, C.; Guo, D.; Liu, Y. Colorimetric copper (II) ions detection in aqueous solution based on the system of 3′3′5′5′-te- tramethylbenzidine and AgNPs in the presence of Na2S2O3. Journal of Science: Advanced Materials and Devices 2022, 7 (2), 100420. https://doi.org/10.1016/j.jsamd.2022.100420. 6. Lin, M.; Guo, Y.; Liang, Z.; Zhao, X.; Chen, J.; Wang, Y. Simple and fast determination of biothiols using Fe3+-3,3′,5,5′-tetramethylbenzidine as a colorimetric probe. Microchem. J. 2019, 147, 319 – 323. https://doi.org/10.1016/j.microc.2019.03.049. 7. Chandra, S.; Singh, V. K.; Yadav, P. K.; Bano, D.; Kumar, V.; Pandey, V. K.; Talat, M.; Hasan, S. H. Mustard seeds derived fluorescent carbon quantum dots and their peroxidase-like activity for colorimetric detection of H2O2 and ascorbic acid in a real sample. Anal. Chim. Acta 2019, 1054, 145 – 156. https://doi.org/10.1016/j.aca.2018.12.024. 8. Xu, L.; Yang, B.; Guo, L. Oxidized 3,3′,5,5′-tetramethylbenzidine nanobelts enhance colorimetric sensing of H2O2. Talanta 2024, 279, 126584. https://doi.org/10.1016/j.talanta.2024.126584. 9. Baye, A. F.; Thi Nguyen, H.; Kim, H. Fe0/Fe3C-assisted Fe3O4 redox sites as robust peroxidase mimics for colorimetric detection of H2O2. Sensors and Actuators B: Chemical 2023, 377, 133097. https://doi.org/10.1016/j.snb.2022.133097. 10. Yin, X.; Liu, P.; Xu, X.; Pan, J.; Li, X.; Niu, X. Breaking the pH limitation of peroxidase-like CoFe2O4 nanozyme via vitriolization for one-step glucose detection at physiological pH. Sensors and Actuators B: Chemical 2021, 328, 129033. https://doi.org/10.1016/j.snb.2020.129033. 11. Song, G.; Zhang, Z.; Fauconnier, M.-L.; Li, C.; Chen, L.; Zheng, X.; Zhang, D. Bimodal single-atom iron nanozyme biosensor for volatile amine and food freshness detection. Nano Today 2023, 53, 102025. https://doi.org/10.1016/j.nantod.2023.102025. 12. Yu, K.; Li, M.; Chai, H.; Liu, Q.; Hai, X.; Tian, M.; Qu, L.; Xu, T.; Zhang, G.; Zhang, X. MOF-818 nanozyme-based colorimetric and electro- chemical dual-mode smartphone sensing platform for in situ detection of H2O2 and H2S released from living cells. Chem. Eng. J. 2023, 451, 138321. https://doi.org/10.1016/j.cej.2022.138321. 13. Cao, W.; Ju, P.; Wang, Z.; Zhang, Y.; Zhai, X.; Jiang, F.; Sun, C. Colorimetric detection of H2O2 based on the enhanced peroxidase mimetic activity of nanoparticles decorated Ce2(WO4)3 nanosheets. Spectrochim. Acta, Part A 2020, 239, 118499. https://doi.org/10.1016/j.saa.2020.118499. 14. Liu, Q.; Tang, P.; Xing, X.; Cheng, W.; Liu, S.; Lu, X.; Zhong, L. Colorimetry /SERS dual-sensor of H2O2 constructed via TMB–Fe3O4@ AuNPs. Talanta 2022, 240, 123118. https://doi.org/10.1016/j.talanta.2021.123118. 15. Blazheevskiy, M. Ye.; Dyadchenko, V. V. Kinetic determination of anticholinesterase compounds by a biochemical method by oxidizing reaction of p-phenetidine as display. Farmatsevtychnyi zhurnal 2004, 2, 52-58. 16. Blazheyevskiy, M. Y.; Kovalska, O. V. The Quantitative Determination of Etonium by the Enzymatic Kinetic-Spectrophotometric Method. J. Org. Pharm. Chem. 2024, 22, 57-62. https://doi.org/10.24959/ophcj.24.304120. 17. Derzhavna farmakopeia Ukrainy: v 3 tomakh, 2 vydannia [The State Pharmacopoeia of Ukraine: in 3 volumes, 2nd ed., in Ukrainian]; State Enterprise “Ukrainian Scientific Pharmacopoeial Center for Quality of Medicines”: Kharkiv, 2015; Vol. 1. 18. Blazheevskiy, M. E.; Kovalska, O. V.; Dyadchenko, V. V. (National University of Pharmacy, Kharkiv, Ukraine). Sposib vyznachennia akty- vnosti kholinesterazy krovi [Method for determining blood cholinesterase activity, in Ukrainian]. Ukraine Patent 117474, 26.06.2017. Information about the authors: Olena V. Kovalska (corresponding author), Ph.D. in Pharmacy, Associate Professor of Organization, Economy and Pharmacy Management Department, Institute of Advanced Training of Pharmacy Specialists of the National University of Pharmacy of the Ministry of Health of Ukraine; https://orcid.org/0000-0003-0113-7060; e-mail for correspondence: lena05021985@ukr.net; tel. +380970710498. Mykola Ye. Blazheyevskіy, D.Sci. in Chemistry, Professor of the General Chemistry Department, National University of Pharmacy of the Ministry of Health of Ukraine; https://orcid.org/0000-0002-8032-347X. Vladyslav V. Diadchenko, Ph.D. in Chemistry, Associate Professor, Military Institute of Armored Forces of the National Technical University “Kharkiv Polytechnic Institute”. https://orcid.org/0000-0002-5552-3031.
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spelling oai:ojs.journals.uran.ua:article-3217952026-08-23T15:46:26Z The Use of Tetramethylbenzidine as an Indicator in the Enzymatic Quantitative Determination of Ethonium Використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію Kovalska, Olena V. Blazheyevskiy, Mykola Ye. Diadchenko, Vladyslav V. ethonium quaternary ammonium compounds cholinesterase acetylcholine етоній холінестераза ацетилхолін четвертинні амонієві сполуки The study considers the possibility of using 3,3',5,5'-tetramethylbenzidine (TMB) as an indicator in the enzymatic analysis for the quantitative determination of quaternary ammonium compounds on the example of ethonium. The feasibility of using TMB as an indicator in the kinetic photometric method has been confirmed. Kinetic curves showing the relationship between the optical density and the ethonium concentration have been constructed. The reaction rates of acetylcholinesterase inhibition by ethonium have been estimated using the tangents of the angles of these curves with TMB as an indicator. The degree of enzyme inhibition has been calculated, and a linear relationship between the ethonium concentration and the degree of inhibition has been determined. This method was applied to determine the ethonium content in 0.1% ethonium gel. The relative standard deviation of the method does not exceed 2.5 %. The approach suggested offers a reliable and accurate method for the quantitative analysis of ethonium in dosage forms. У дослідженні розглянуто можливість використання 3,3',5,5'-тетраметилбензидину (ТМБ) як індикатора в ензиматичному аналізі для кількісного визначення четвертинних амонієвих сполук на прикладі етонію. Підтверджено можливість застосування ТМБ як індикатора в кінетичному фотометричному методі. Побудовано кінетичні криві, що демонструють залежність між оптичною густиною та концентрацією етонію. Швидкість реакції інгібування ацетилхолінестерази етонієм було оцінено за тангенсами кутів цих кривих, із цим ТМБ використано як індикатор. Розраховано ступінь інгібування ферменту, а також визначено лінійну залежність між концентрацією етонію та ступенем інгібування. Цей метод застосовували для визначення вмісту етонію в 0,1% гелі етонію. Відносне стандартне відхилення методу не перевищує 2,5%. Запропонований підхід забезпечує надійний та точний метод кількісного аналізу етонію у лікарських формах. National University of Pharmacy 2024-12-12 Article Article application/pdf https://ophcj.nuph.edu.ua/article/view/321795 10.24959/ophcj.24.321795 Journal of Organic and Pharmaceutical Chemistry; Vol. 22 No. 4 (2024); 36-42 Журнал органической и фармацевтической химии; Том 22 № 4 (2024); 36-42 Журнал органічної та фармацевтичної хімії; Том 22 № 4 (2024); 36-42 2518-1548 2308-8303 en https://ophcj.nuph.edu.ua/article/view/321795/313392 Copyright (c) 2025 Olena V. Kovalska, Mykola Ye. Blazheyevskiy, Vladyslav V. Diadchenko http://creativecommons.org/licenses/by/4.0
spellingShingle етоній
холінестераза
ацетилхолін
четвертинні амонієві сполуки
Kovalska, Olena V.
Blazheyevskiy, Mykola Ye.
Diadchenko, Vladyslav V.
Використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію
title Використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію
title_alt The Use of Tetramethylbenzidine as an Indicator in the Enzymatic Quantitative Determination of Ethonium
title_full Використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію
title_fullStr Використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію
title_full_unstemmed Використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію
title_short Використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію
title_sort використання тетраметилбензидину як індикатора у ензиматичному методі кількісного визначення етонію
topic етоній
холінестераза
ацетилхолін
четвертинні амонієві сполуки
topic_facet ethonium
quaternary ammonium compounds
cholinesterase
acetylcholine
етоній
холінестераза
ацетилхолін
четвертинні амонієві сполуки
url https://ophcj.nuph.edu.ua/article/view/321795
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