Binding of Cimetidine to Balb/C Mouse Liver Catalase; Kinetics and Conformational Studies

Jahangirvand, Mahboubeh; Minai-Tehrani, Dariush; Yazdi, Fatemeh; Minai-Tehrani, Arash; Razmi, Nematollah

doi:10.2174/1574884711666160122093020

Cited by 5 publications

(3 citation statements)

References 9 publications

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“…11 Cimetidine is a H2 blocker that inhibits gastric acid secretion and is largely used in the treatment of peptic ulcers. 12 It works by binding to an H2-receptor located on the basolateral membrane of the gastric parietal cell, blocking histamine effects. 13 It has been demonstrated to cause dose-related inhibition of cytochrome P-450-mediated oxidation both in vivo and in vitro.…”

Section: Introductionmentioning

confidence: 99%

Effect of cimetidine on cyclophosphamide-induced liver toxicity in albino rats

Adikwu

Bokolo

2018

Asian J Med Sci

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Background: The clinical use of cyclophosphamide (CP) has been characterised by liver toxicity.Aims and Objectives: This research assessed the effect of cimetidine against CP-induced liver toxicity in a rat model.Material and Methods: Forty eight albino rats divided into 8 groups (A-H) of 6 rats per group gage were used for this study. Group A (control) was administered with water while groups B-D were administered with 5, 10, and 20 mg/kg/day of cimetidine intraperitoneally (ip) for 5 days respectively. Group E was administered with 150 mg/kg of CP ip on the 5th day whereas groups F-H were administered with 5 10, and 20 mg/kg/day of cimetidine for 5 days and CP ip on the 5th day. Rats were subjected to an overnight fast and sacrificed on the sixth day. Serum was extracted from blood and liver function parameters were evaluated. Liver was excised and evaluated for biochemical parameters and histology.Results: CP treatment had no significant (P>0.05) effects on body and liver weights, but significant (P<0.05) increases in alanine aminotransferase, alkaline phosphatase, aspartate aminotransferase, lactate dehydrogenase, gamma, glatamyl transferase, total bilirubin, conjugated bilirubin and malondialdehyde levels were observed when compared to control. Furthermore, significant (P<0.05) decreases in liver superoxide dismutase, catalase, glutathione and glutathione peroxidise were obtained in CP-administered rats when compared to control. The Liver of CP-treated rat shows hepatocyte necrosis around the central veins. However, CP-induced liver damage was significantly (P<0.05; 0.01) ameliorated in a dose-dependent manner in rats administered with cimetidine prior to the administration of CP.Conclusion: Cimetidine ameliorates cyclophosphamide-induced liver toxicity in albino rats.Asian Journal of Medical Sciences Vol.9(5) 2018 50-56

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Section: Introductionmentioning

confidence: 99%

Effect of cimetidine on cyclophosphamide-induced liver toxicity in albino rats

Adikwu

Bokolo

2018

Asian J Med Sci

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“…Lineweaver-Burk plots were used to determine the kinetic parameters and inhibition types. Arrhenius plots were used to compare the activation energies of the enzymes in the presence or absence of the drug by calculating Vmax of the enzymes at different temperatures 36,37 .…”

Section: Experimental Studies Sample Collectionmentioning

confidence: 99%

In silico and in vitro studies confirm Ondansetron as a novel acetylcholinesterase and butyrylcholinesterase inhibitor

Gholami

Minai-Tehrani

Eriksson

2023

Sci Rep

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Alzheimer’s disease (AD) is a progressive neurodegenerative disorder that is growing rapidly among the elderly population around the world. Studies show that a lack of acetylcholine and butyrylcholine due to the overexpression of enzymes Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE) may lead to reduced communication between neuron cells. As a result, seeking novel inhibitors targeting these enzymes might be vital for the future treatment of AD. Ondansetron is used to prevent nausea and vomiting caused by chemotherapy or radiation treatments and is herein shown to be a potent inhibitor of cholinesterase. Comparison is made between Ondansetron and FDA-approved cholinesterase inhibitors Rivastigmine and Tacrine. Molecular docking demonstrates that interactions between the studied ligand and aromatic residues in the peripheral region of the active site are important in binding. Molecular dynamics simulations and binding pose metadynamics show that Ondansetron is highly potent against both enzymes and far better than Rivastigmine. Inhibitor activities evaluated by in vitro studies confirm that the drug inhibits AChE and BChE by non-competitive and mixed inhibition, respectively, with IC50 values 33 µM (AChE) and 2.5 µM (BChE). Based on the findings, we propose that Ondansetron may have therapeutic applications in inhibiting cholinesterase, especially for BChE.

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“…Lineweaver-Burk plots were used to de ne the kinetic parameters and inhibition types. Arrhenius plots were used to compare the activation energies of the enzymes in the presence or absence of the drug by calculating Vmax of the enzymes at different temperatures [35,36].…”

Section: Enzyme Assaymentioning

confidence: 99%

In silico and in vitro Studies Confirm Ondansetron as a Novel Acetylcholinesterase and Butyrylcholinesterase Inhibitor

Gholami

Minai-Tehrani

Eriksson

2022

Preprint

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Alzheimer’s disease (AD) is a progressive neurodegenerative disorder that is growing rapidly among the elderly population around the world. Studies show that a lack of acetylcholine and butyrylcholine due to the overexpression of enzymes Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE) may lead to reduced communication between neuron cells. As a result, seeking novel inhibitors targeting these enzymes might be vital for future treatment of AD. Ondansetron is used to prevent nausea and vomiting caused by chemotherapy or radiation treatments, and is herein shown to be a potent inhibitor of cholinesterase. Comparison is made between Ondansetron and FDA-approved cholinesterase inhibitors Rivastigmine and Tacrine. Molecular docking demonstrates that interactions between the studied ligand and aromatic residues in the peripheral region of the active site are important in binding. Molecular dynamics simulations and binding pose metadynamics show that Ondansetron is highly potent against both enzymes, and far better than Rivastigmine. Inhibitor activities evaluated by in vitro studies confirm that the drug inhibits AChE and BChE by non-competitive and mixed inhibition, respectively, with IC50 values 33 µM (AChE) and 2.5 µM (BChE). Based on the findings, we propose that Ondansetron may have therapeutic applications in inhibiting cholinesterase, especially for BChE.

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Binding of Cimetidine to Balb/C Mouse Liver Catalase; Kinetics and Conformational Studies

Cited by 5 publications

References 9 publications

Effect of cimetidine on cyclophosphamide-induced liver toxicity in albino rats

Effect of cimetidine on cyclophosphamide-induced liver toxicity in albino rats

In silico and in vitro studies confirm Ondansetron as a novel acetylcholinesterase and butyrylcholinesterase inhibitor

In silico and in vitro Studies Confirm Ondansetron as a Novel Acetylcholinesterase and Butyrylcholinesterase Inhibitor

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