<i>In vitro</i> inhibition effect of some coumarin compounds on purified human serum paraoxonase 1 (PON1)

In this study, we investigated the effects of certain respiratory drugs, which are mainly used on human serum paraoxonase‐1 (hPON1; EC 3.1.8.1). hPON1 was purified from human serum, with 354.91 fold and 45% yield by using two simple step procedures including, first, ammonium sulfate precipitation, then, Sepharose‐4B‐l‐tyrosine‐1‐naphthylamine hydrophobic interaction chromatography. SDS‐polyacrylamide gel electrophoresis showed a single protein band belonging to hPON1 with 43 kDa. All the pharmaceutical compounds inhibited the PON1 enzyme highly at the micromolar level. The obtained IC50 values for nine different pharmaceutics ranged from 0.219 μM (salbutamol sulfate) to 67.205 μM (montelukast sodium). So, all drugs could be considered as potent hPON1 inhibitors. Ki values and inhibition types were determined by Lineweaver‐Burk graphs. While varenicline tartrate and moxifloxacin hydrochloride inhibited the enzyme in a noncompetitive manner, others inhibited it in a mixed manner.

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“…However, there are very few studies investigating the interaction between PON activity and pharmaceutical products …”

Section: Resultsmentioning

confidence: 99%

Association of human serum paraoxonase‐1 with some respiratory drugs

Gökçe

Sarıoğlu

Gençer

et al. 2019

J Biochem & Molecular Tox

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“…Several studies reported the effects of some drugs on PON1 (Arslan et al, 2012; Gokce et al, 2016; Kiranoglu et al, 2007; Sinan et al, 2006). In the literature, there are few studies investigating the interactions between pharmaceutical products and PON1 activity.…”

Section: Discussionmentioning

confidence: 99%

“…These enzymes have been purified from different sources. Drug interaction studies of these essential enzymes have made significant contributions to the academic literature in the field of drug metabolism (Arslan et al, 2012; Gokce et al, 2016; Karatas, Uslu, Alıcı, Gokce, Gencer, & Arslan, 2016; Karatas Uslu, Alıcı, Gokce, Gencer, Arslan, Arslan, et al, 2016; Kiranoglu et al, 2007; Sinan et al, 2006). However, there are not enough studies about the impact of cardiac drugs on PON1 activity.…”

Section: Introductionmentioning

confidence: 99%

In vitro effects of thirty‐eight cardiac drugs on human serum paraoxonase

et al. 2022

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In this study, the effects of 38 commonly used cardiac drugs on the human paraoxonase (PON1) were investigated. PON1 was purified from human serum blood by ammonium sulfate precipitation (60%–80%) and hydrophobic interaction chromatography (Sepharose‐4B~L‐tyrosine~1‐napthylamine gel). All of the cardiac drugs inhibited PON1 at the micro molar level. IC50 and Ki values were determined for each drug. The tested drugs displayed potent PON1 inhibitory activity. It was found that the weakest PON1 inhibitors are Irbesartan (Ki: 421.73 µM), Glyceryl Trinitrate (Ki: 351.48 µM), and Apixaban (Ki: 333.27 µM). Bisoprolol hemifumarate (Ki: 269.31 µM) is also other weak PON1 inhibitor. Therefore, these drugs, having weak PON1 inhibitory activity, may be preferred primarily in patients with atheroclerotic heart disease compared to other drugs due to the protective effect of PON1 on atherosclerosis. Conversely, the most potent inhibitors against PON1 were propafenone (Ki: 0.35 µM), Lacidipine (Ki: 0.78 µM), Lidocaine HCl (Ki: 1.78 µM), and Propranolol (Ki: 1.86 µM). Molecular docking was also applied to confirm the activity of some cardiac drugs on PON1.

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“…Respecto a las actividades enzimáticas PON1, existen varios estudios en la literatura que refieren una menor actividad AREasa en poblaciones ocupacionalmente expuestas a OF (Zhang et al 2014, Gokce et al 2016 con respecto a poblaciones control, lo cual coincide con los resultados obtenidos en este trabajo. En cuanto a la actividad CMPAasa, hasta donde sabemos sólo existe un estudio realizado por Bernal-Hernández et al (2014) en agricultores indígenas de México, en el que reportaron tendencias de una disminución en la actividad CMPAasa en el grupo expuesto con respecto al grupo no expuesto.…”

Section: Discussionunclassified

Patrón De Uso De Plaguicidas Y Biomarcadores Bioquímicos en Una Población De Fumigadores Urbanos

Benítez-Trinidad

Herrera-Moreno

Xotlanihua-Gervacio

et al. 2018

Rev. Int. Contam. Ambie.

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Palabras clave: plaguicidas, colinesterasas, paraoxonasa RESUMEN Nayarit es uno de los estados con las tasas más altas de intoxicación por plaguicidas en México. Los fumigadores son una población vulnerable por el alto riesgo de exposición que conlleva su trabajo. El objetivo de este estudio fue evaluar el patrón de uso de estos compuestos, así como las actividades de colinesterasas y paraoxonasa 1 en fumigadores urbanos, en dos periodos de tiempo. Se realizó un estudio descriptivo y analítico, se aplicaron cuestionarios estructurados para conocer las características antropométricas de los trabajadores que se dedican a la fumigación, la frecuencia del uso de equipo de protección, la percepción del riesgo y el patrón de plaguicidas utilizados. La determinación de las actividades acetilcolinesterasa (AChE), butirilcolinesterasa (BuChE) y paraoxonasa 1 (AREasa y CMPAasa) se realizó por métodos espectrofotométricos. Los resultados indican que el género masculino es el que mayormente desempaña estas labores y que el 95.1 % no utilizan el equipo de protección recomendado. Los insecticidas organofosforados, piretroides y carbamatos son los más utilizados. En cuanto a las actividades enzimáticas, se observó una menor actividad de BuChE y AREasa en el primer periodo del estudio. Sobre la base de los resultados obtenidos, es necesario implementar estrategias de educación ambiental encaminadas a disminuir la exposición a plaguicidas y por ende los efectos adversos ocasionados por un mal uso y manejo de los mismos.Key words: pesticides, cholinesterases, paraoxonases ABSTRACT Nayarit is among the states with the highest rates of pesticide poisoning in Mexico. Sprayers are a vulnerable population due to the high risk of exposure that their job entails. The aim of this study was to gain insight into the current usage pattern of pesticides in fumigation activities, cholinesterases and paraoxonase activities in urban sprays in two different period of times. A descriptive and analytical study was conducted, structured questionnaires were applied to evaluate the anthropometric characteristics

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In vitro inhibition effect of some coumarin compounds on purified human serum paraoxonase 1 (PON1)

Cited by 9 publications

References 30 publications

Association of human serum paraoxonase‐1 with some respiratory drugs

Association of human serum paraoxonase‐1 with some respiratory drugs

In vitro effects of thirty‐eight cardiac drugs on human serum paraoxonase

Patrón De Uso De Plaguicidas Y Biomarcadores Bioquímicos en Una Población De Fumigadores Urbanos

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