ArticleInternational journal of molecular sciences2013
Caffeine inhibits acetylcholinesterase, but not butyrylcholinesterase.
Article in International journal of molecular sciences, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 44 papers.
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Who cites it
44 citing papers in PubMed, 117 citations in OpenAlex.
- Individual responses to encapsulated caffeine and caffeine chewing gum on strength and power in strength-trained males.Journal of the International Society of Sports Nutrition · 2025Trial
- Caffeine supplementation induces higher IL-6 and IL-10 plasma levels in response to a treadmill exercise test.Journal of the International Society of Sports Nutrition · 2020Trial
- Reduced Pseudocholinesterase Levels Are Associated With Alterations in Lipid Biomarkers and Liver Enzymes Among Ghanaian Male Cocoa Farmers Using Organophosphate Pesticides.TheScientificWorldJournal · 2026Article
- Toxicology of caffeine poisoning: molecular mechanisms, toxicokinetic profiles, and clinical implications.Frontiers in toxicology · 2026Review
- Coffee intake is associated with telomere length in severe mental disorders.BMJ mental health · 2025Article
- Impact of Caffeine on Aquatic Ecosystems: Assessing Trophic-Level Biological Responses.Journal of xenobiotics · 2025Article
- Fluorometric and Colorimetric Biosensors for the Assay of Cholinesterase Inhibitors.Sensors (Basel, Switzerland) · 2025Review
- Tethered cord syndrome (TCS) and constipation in children: a multifaceted approach (literature review).Annals of medicine and surgery (2012) · 2025Review
- Assessment of the Interaction of Acetylcholinesterase Binding with Bioactive Compounds from Coffee and Coffee Fractions DigestedJournal of agricultural and food chemistry · 2024Article
- The Cholinergic Selectivity of FDA-Approved and Metabolite Compounds Examined with Molecular-Docking-Based Virtual Screening.Molecules (Basel, Switzerland) · 2024Article
- Article
- Insights into environmental caffeine contamination in ecotoxicological biomarkers and potential health effects ofHeliyon · 2023Article
- The neuroprotective effect of traditional Chinese medicinal plants-A critical review.Acta pharmaceutica Sinica. B · 2023Review
- Possible Interaction between ZnS Nanoparticles and Phosphonates on Mediterranean ClamsMolecules (Basel, Switzerland) · 2023Article
- Coffee and cardiac arrhythmias: Up-date review of the literature and clinical studies.Cardiology journal · 2023Review
- Natural Product Co-Metabolism and the Microbiota-Gut-Brain Axis in Age-Related Diseases.Life (Basel, Switzerland) · 2022Review
- Design, Synthesis and Assay of Novel Methylxanthine-Alkynylmethylamine Derivatives as Acetylcholinesterase Inhibitors.Molecules (Basel, Switzerland) · 2022Article
- Mental Performance and Sport: Caffeine and Co-consumed Bioactive Ingredients.Sports medicine (Auckland, N.Z.) · 2022Review
- Neuroprotective Effect of Caffeine in Alzheimer's Disease.Molecules (Basel, Switzerland) · 2022Review
- Neurochemical and Behavioral Consequences of Ethanol and/or Caffeine Exposure: Effects in Zebrafish and Rodents.Current neuropharmacology · 2022Review
Corrections and comments
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Authors and funding
2 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Caffeine is an alkaloid with a stimulant effect in the body. It can interfere in transmissions based on acetylcholine, epinephrine, norepinephrine, serotonin, dopamine and glutamate. Clinical studies indicate that it can be involved in the slowing of Alzheimer disease pathology and some other effects. The effects are not well understood. In the present work, we focused on the question whether caffeine can inhibit acetylcholinesterase (AChE) and/or, butyrylcholinesterase (BChE), the two enzymes participating in cholinergic neurotransmission. A standard Ellman test with human AChE and BChE was done for altering concentrations of caffeine. The test was supported by an in silico examination as well. Donepezil and tacrine were used as standards. In compliance with Dixon's plot, caffeine was proved to be a non-competitive inhibitor of AChE and BChE. However, inhibition of BChE was quite weak, as the inhibition constant, Ki, was 13.9 ± 7.4 mol/L. Inhibition of AChE was more relevant, as Ki was found to be 175 ± 9 µmol/L. The predicted free energy of binding was -6.7 kcal/mol. The proposed binding orientation of caffeine can interact with Trp86, and it can be stabilize by Tyr337 in comparison to the smaller Ala328 in the case of human BChE; thus, it can explain the lower binding affinity of caffeine for BChE with reference to AChE. The biological relevance of the findings is discussed.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.