Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet

Martı́n-Biosca, Yolanda; Asensi-Bernardi, Lucía; Villanueva-Camañas, R.M.; Sagrado, S.; Medina-Hernández, M.J.

doi:10.1002/jssc.200800701

Cited by 24 publications

(14 citation statements)

References 24 publications

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“…Yolanda et al. adopted CZE with the 30 mM borax‐phosphate solution as background buffer (pH 8.0) and applied on‐line enzyme microreactor to screen the inhibitors of acetylcholin esterase. Obviously, the simple formation of the buffer applied in CZE resulted in the enhancement of the stability and repeatability of results.…”

Section: Screening Active Compounds Using Cementioning

confidence: 99%

Screening bioactive compounds from natural product and its preparations using capillary electrophoresis

Bai

et al. 2017

Electrophoresis

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Screening bioactive compounds from natural product and its preparations using capillary electrophoresisBioactive ingredients of natural products can protect human body from harm, as well as prevent and treat disease. Screening bioactive compounds from natural products is attracting particular attention. It is a great challenge to separate and detect the active compounds from complex matrix natural products. CE plays a vital role in screening active compounds because of its unique features such as high-efficiency separation, short-analysis time, minimal sample consumption, and ease to realize automatization etc. Additionally, CE has been developed various modes owing to its abundant advantages in analysis and separation of compounds. The purpose of this work is to review previous developments and applications of CE in screening bioactive compounds derived from natural products from 2007 to 2017. This review does not only summarize the traditional methods of detecting active ingredients but also briefly introduces some novel assays. The trends in the application of CE in active compounds screening are addressed in the article.

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Section: Screening Active Compounds Using Cementioning

confidence: 99%

Screening bioactive compounds from natural product and its preparations using capillary electrophoresis

Bai

et al. 2017

Electrophoresis

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“…16 The most frequently employed solution enzyme assays rely on a colorimetric method using Ellman´s reagent 17 or the Fast Blue B salt reagent, and also on radiochemical, spectrometric, and chromatographic methods 16,18 and capillary electrophoresis. [19][20] Other methods involve an interesting approach: the immobilization of the target enzyme and its inclusion in a chromatographic system. Such methods can provide a shorten analysis and more reliable results, besides furnishing information about the affinity of the tested molecule for the target protein.…”

Section: -9mentioning

confidence: 99%

A Comparative Evaluation of Acetylcholinesterase Inhibition by AChE-ICER and in vitro Ellman's Modified Method of Simplified Analogs 3-O-Acetyl-N-Benzyl-Piperidine of Donepezil

Silva¹,

Nicastro²,

Oliveira³

et al. 2015

Revista Virtual De Química

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Resumo: Inibidores de Acetilcolinesterase (AChEI) ainda são os melhores fármacos usados para a terapêutica da doença de Alzheirmer (DA). Dentre os IAChEs disponíveis, o donepezil apresenta a maior meia-vida, os efeitos colaterais mais brandos, além de segurança e tolerância satisfatórias; portanto, este tem sido utilizado como medicamento de primeira escolha no tratamento de DA leve a moderada. A triagem bem sucedida de novos AChEI depende de métodos rápidos e eficientes. Os ensaios empregados mais frequentemente são baseados no uso do reagente de Ellman (ensaio colorimétrico) ou do reagente Fast Blue B, além de métodos radioquímicos, espectrométricos ou cromatográficos. Uma abordagem mais recente utiliza a enzima imobilizada em reator capilar, acoplada a um sistema cromatográfico, que é conhecido como ICER (do inglês immobilized capillary enzyme reactor). Como parte de um projeto que visa à identificação de novos IAChEs, este artigo descreve a avaliação comparativa da atividade inibitória da AChE de uma série de derivados 3-O-acetil-N-benzilpiperidínicos substituídos por duas diferentes abordagens: método de Ellman modificado in vitro e uma metodologia de ICER. Embora nenhum dos compostos da série tenha apresentado alta atividade inibitória, todos os ensaios revelaram resultados consistentes, demostrando que é possível aplicar diferentes metodologias confiáveis para a busca e idendificação de novos inibidores de AChE.Palavras-chave: Química Medicinal; análogos N-benzil-piperidinícos; inibidores de acetilcolinesterase; doença de Alzheimer; enzima imobilizada; enzima imobilizada em reator capilar. AbstractAcetylcholinesterase inhibitors (AChEI) remain the best pharmacotherapy for Alzheimer´s disease (AD). Among the currently available AChEI drugs, Donepezil has longer half-life, fewer clinical side interactions, and satisfactory safety and tolerability; therefore, it is the first choice medicine to treat mild to moderate AD. Successful screening for new AChEIs relies on effective and fast assays. The ost f e ue tly e ployed assays a e ased o the use of Ell a 's eage t olo i et i ethod o the Fast Blue B salt reagent, despite of other radiochemical, spectrometric, or chromatographic methods. A more recent and interesting approach is to immobilize the target enzyme in a chromatographic system, which is known as immobilized capillary enzyme reactors (ICERs). As part of a current project aiming to search for novel AChEIs, in this paper we have reported a comparative evaluation of AChE inhibitory activity of a series of substituted 3-O-acetyl-N-benzylpiperidine derivatives by two different approaches: in vitro Ell a 's odified ethod a d a ICER-based methodology. Although none of the compounds has shown high activity, all different assays revealed consistent results, showing that is possible to apply different reliable methodologies for the screening of new AChEIs.Keywords: N-benzyl-pipe idi e a alogs; A etyl holi este ase i hi itio ; Alzhei e 's Disease; e zy e i o ilizatio ; i o ilized capillary enzyme reactor.

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“…Among them, the at‐inlet technology is relatively simple and more easily operated, because the analytes are mixed by free diffusion. At‐inlet technology has been successfully used in the screening of enzyme inhibitors and enzyme kinetics and other fields.…”

Section: Introductionmentioning

confidence: 99%

Establishment and development of a CZE–UV method for rapid measurement of aprotinin potency

Zhang

Dong

et al. 2019

Electrophoresis

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A new method for the measurement of aprotinin potency by CZE-UV detector was established for the first time. The on-line mixing of substrate, trypsin and aprotinin using at-inlet technology was realized by the established method. Enzymatic reaction, separation, and detection of substrate and product can be performed simultaneously online. The aprotinin potency can be measured within 4 min. The response surface methodology was used to optimize the incubation conditions of trypsin and substrate, and the optimized conditions were obtained under 17.39 mM phosphate buffer at pH 7.6, 1.40 min of incubation time. The repeatability of proposed method was evaluated in three different systems of capillary zone electrophoresis: (i) only substrate; (ii) trypsin and substrate; (iii) aprotinin, trypsin and substrate, and the RSDs of migration times and peak areas of substrate were less than 2.7 and 3.1%, respectively. The RSDs of migration times and peak areas of product were less than 2.1 and 3.0%, respectively. A formula was also developed to calculate the aprotinin potency in this method. In a word, the established CZE-UV method was convenient, fast, and environmentally friendly for the measurement of aprotinin potency.

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Screening of acetylcholinesterase inhibitors by CE after enzymatic reaction at capillary inlet

Cited by 24 publications

References 24 publications

Screening bioactive compounds from natural product and its preparations using capillary electrophoresis

Screening bioactive compounds from natural product and its preparations using capillary electrophoresis

A Comparative Evaluation of Acetylcholinesterase Inhibition by AChE-ICER and in vitro Ellman's Modified Method of Simplified Analogs 3-O-Acetyl-N-Benzyl-Piperidine of Donepezil

Establishment and development of a CZE–UV method for rapid measurement of aprotinin potency

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