Inhibition effects of isoproterenol, chlorpromazine, carbamazepine, tamoxifen drugs on glutathione S-transferase, cholinesterases enzymes and molecular docking studies

Türkan, Fikret; Çalımlı, Mehmet Harbi; Kanberoğlu, Gülşah Saydan; Karaman, Muhammet

doi:10.1080/07391102.2020.1763200

Cited by 14 publications

(12 citation statements)

References 33 publications

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“…For Cpz, the decrease in GST activity was one of the most particular reactions observed in this study. The inhibition of GST was also illustrated for the effect of Cpz in vitro (Türkan et al 2020 ). Moreover, among four tested drugs, Cpz was found to be the best inhibitor for the GST enzyme (Oliveira et al 2015 ).…”

Section: Discussionmentioning

confidence: 99%

Environmental concentrations of Roundup in combination with chlorpromazine or heating causes biochemical disturbances in the bivalve mollusc Unio tumidus

Khoma

Martinyuk

Matskiv

et al. 2021

Environ Sci Pollut Res

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Graphical abstract Bivalve molluscs represent the most recognized bioindicators of freshwater pollution. However, their ability to indicate specific xenobiotics in complex exposures is unclear. In this study, we aimed to track the particular effects of the pesticide Roundup (Rnd) and the antipsychotic drug chlorpromazine (Cpz) on the mussel Unio tumidus at the simpler environmentally relevant models. We treated the mussels by Rnd (17 μg L −1 ), Cpz (18 μg L −1 ), the mixture of Rnd and Cpz at 18 °C (RndCpz), and Rnd at 25 °C (RndT) and examined their digestive glands after 14 days of exposure. We analyzed total antioxidant capacity, glutathione (GSH&GSSG) and protein carbonyls levels, total and Zn-related concentrations of metallothioneins (MT and Zn-MT, respectively), the activities of CYP450-related EROD, glutathione S -transferase, cholinesterase, caspase-3, citrate synthase (CS), lysosomal membrane integrity (NRR), and Zn level in the tissue. Shared responses were indicated as the increase of the antioxidant, Zn-MT, and EROD levels, whereas the changes of Zn concentration, NRR, and caspase-3 activity were most diverse compared to control. According to discriminant analysis, complex exposures abolished the individual response traits and intensified the harmful effects that caused a decrease in the Zn level in the RndCpz- and RndT-groups and the loss of lysosomal integrity in the RndT-group. We concluded that multi-marker expertise with the application of integrated indices had benefits when evaluating the effects of complex exposures. Supplementary Information The online version contains supplementary material available at 10.1007/s11356-021-16775-1.

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Section: Discussionmentioning

confidence: 99%

Environmental concentrations of Roundup in combination with chlorpromazine or heating causes biochemical disturbances in the bivalve mollusc Unio tumidus

Khoma

Martinyuk

Matskiv

et al. 2021

Environ Sci Pollut Res

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show abstract

“…For the Cpz, the decrease in GST activity was one of the most particular reactions observed in this study. The inhibition of GST has also been shown for the effect of Cpz in vitro (Türkan et al 2020). Moreover, among four tested drugs, Cpz has been found to be the best inhibitor for the GST enzyme (Oliveira et al 2015).…”

Section: Enzymes Of Biotransformation As the Probable Targets For Roundup And Chlorpromazinementioning

confidence: 88%

Predicted No-Effect Concentration of Roundup in the Composition with Pharmaceutical Chlorpromazine or Heating Causes Similar Biochemical Disturbances in Bivalve Mollusk Unio Tumidus

Khoma

Martinyuk

Matskiv

et al. 2021

Preprint

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The ability of bioindicators to reflect the specific impacts in complex exposures is unpredicted. This study aimed to track the particular effects of pesticide Roundup (Rn) and antipsychotic drug chlorpromazine (Cpz) on the mussel Unio tumidus at environmentally relevant mixtures. The mussels were treated by Rn (17 µg L−1), Cpz (18 µg L−1), mixture of Rn and Cpz at 18 oC (RnCpz) as well as by Rn at 25 oC (RnT). Digestive glands were examined after 14 days of exposure. The indexes of stress response (total antioxidant capacity, glutathione (GSH&GSSG), metallothioneins (MTSH and Zn-MT), protein carbonyls levels), and markers of metabolic and detoxication (CYP450 related (EROD), Glutathione S-transpherase (GST), cholinesterase, caspase-3, citrate synthase (CS) activities), lysosomal membrane integrity, and Zn level were analyzed. Mostly common responses of mussels were indicated as the increase of oxidative stress, MTSH (except Cpz-group), EROD and CS (except Rn-group) responses. Rn-group indicated almost no-effect or abnormal for expected symptoms effect. However, under the heating Rn caused the decrease of Zn accumulation and loss of lysosomal integrity. Cpz provoked major response diverseness: a decrease in Zn and GST levels and an increase in lysosomal integrity. Thus, complex exposures abolished the individual response traits. Summarising, the application of integrated indices has benefits when evaluating the effects of complex exposures.

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“…The effectiveness of the main protease inhibitors was determined by in vitro experiments and docked into the main protease using the induced-fit docking method [21]. Induced-fit docking was performed in three steps, including centroid generation, side-chain trimming and refinement of ligand pose, according to previously reported studies [22].…”

Section: Induced-fit Docking Studymentioning

confidence: 99%

Pharmacophore Analyses of SARS-CoV-2 Active Main Protease Inhibitors Using Pharmacophore Query and Docking Study

Karaman

2020

Preprint

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The coronavirus disease (COVID-19) pandemic is the most important current problem in the world. Many researchers have focused on approved drugs or new drug candidates to combat the pandemic. Structural and nonstructural proteins of SARS-CoV-2 have been detected as targets for prevention of host cell infection or blockade of vital function. The main protease that plays an essential role in the virus life cycle is the optimal target. To design new inhibitors against the enzyme, the catalytic active site and substrate-binding site should be well analyzed. In this study, we generated a pharmacophore model using the cocrystallized pose of an active SARS-CoV-2 main protease inhibitor. According to the model, the inhibitor inhibits the enzyme via three hydrogen bond donors, two hydrogen bond acceptors and two aromatic ring interactions. Moreover, we docked reported active inhibitors of the main protease into the catalytic active site and detected matches between their pharmacophore models. The results showed that two close hydrogen acceptor/donor atom pairs and an aromatic ring are essential for enzyme inhibition.

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Inhibition effects of isoproterenol, chlorpromazine, carbamazepine, tamoxifen drugs on glutathione S-transferase, cholinesterases enzymes and molecular docking studies

Cited by 14 publications

References 33 publications

Environmental concentrations of Roundup in combination with chlorpromazine or heating causes biochemical disturbances in the bivalve mollusc Unio tumidus

Environmental concentrations of Roundup in combination with chlorpromazine or heating causes biochemical disturbances in the bivalve mollusc Unio tumidus

Predicted No-Effect Concentration of Roundup in the Composition with Pharmaceutical Chlorpromazine or Heating Causes Similar Biochemical Disturbances in Bivalve Mollusk Unio Tumidus

Pharmacophore Analyses of SARS-CoV-2 Active Main Protease Inhibitors Using Pharmacophore Query and Docking Study

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