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Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase
Joint Authors
Pohanka, Miroslav
Kostelnik, Adam
Cegan, Alexander
Source
Issue
Vol. 2017, Issue 2017 (31 Dec. 2017), pp.1-5, 5 p.
Publisher
Hindawi Publishing Corporation
Publication Date
2017-07-13
Country of Publication
Egypt
No. of Pages
5
Main Subjects
Abstract EN
Biperiden is a drug used in Parkinson disease treatment and it serves also as an antiseizures compound in organophosphates poisoning.
It acts as antagonist of muscarinic receptor activated by acetylcholine while the enzyme acetylcholinesterase (AChE) cleaves acetylcholine in synaptic junction into choline and acetic acid.
This enzyme is inhibited by various compounds; however there has not been proposed evidence about interaction with biperiden molecule.
We investigated this interaction using standard Ellman’s assay and experimental findings were critically completed with an in silico prediction by SwissDock docking software.
Uncompetitive mechanism of action was revealed from Dixon plot and inhibition constant (Ki) was calculated to be 1.11 mmol/l.
The lowest predicted binding energy was −7.84 kcal/mol corresponding to H-bond between biperiden molecule and Tyr 341 residuum in protein structure of AChE.
This interaction seems to be further stabilized by π-π interaction with Tyr 72, Trp 286, and Tyr 341.
In conclusion, biperiden appears as a very weak inhibitor but it can serve as a lead structure in a pharmacological research.
American Psychological Association (APA)
Kostelnik, Adam& Cegan, Alexander& Pohanka, Miroslav. 2017. Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase. BioMed Research International،Vol. 2017, no. 2017, pp.1-5.
https://search.emarefa.net/detail/BIM-1134877
Modern Language Association (MLA)
Kostelnik, Adam…[et al.]. Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase. BioMed Research International No. 2017 (2017), pp.1-5.
https://search.emarefa.net/detail/BIM-1134877
American Medical Association (AMA)
Kostelnik, Adam& Cegan, Alexander& Pohanka, Miroslav. Anti-Parkinson Drug Biperiden Inhibits Enzyme Acetylcholinesterase. BioMed Research International. 2017. Vol. 2017, no. 2017, pp.1-5.
https://search.emarefa.net/detail/BIM-1134877
Data Type
Journal Articles
Language
English
Notes
Includes bibliographical references
Record ID
BIM-1134877