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Publication detail

Inhibition of acetylcholinesterase and butyrylcholinesterase by a plant secondary metabolite boldine
Authors: Kostelník Adam | Pohanka Miroslav
Year: 2018
Type of publication: článek v odborném periodiku
Name of source: Biomed Research International
Page from-to: "9634349-1"-"9634349-5"
Titles:
Language Name Abstract Keywords
cze Inhibiční studie boldinu na acetylcholinesterasu a butyrylcholinesterasu Acetylcholinesterasa (AChE) and butyrylcholinesterasa (BChE) jsou enzymy citlivé k rozličným inhibitorům. Boldin je přírodní alkaloid, který byl v literatuře zmíněn jako inhibitor AChE. V naší práci byl přezkoumán jeho efekt na AChE a rovněž BChE za použití standardní Ellmanovy metody. Z výsledků byly vypočteny IC50 pro AChE (372 𝜇mol/l) a pro BChE (321 𝜇mol/l). Rovněž bylo provedeno modelování boldinu do struktury cholinesteras pro zjištění mechanismu molekulární interakce. Acetylcholinesterasa; butyrylcholinesterasa; inhibice; dokování; boldin
eng Inhibition of acetylcholinesterase and butyrylcholinesterase by a plant secondary metabolite boldine Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are two enzymes sensitive to various chemical compounds having ability to bind to crucial parts of these enzymes. Boldine is a natural alkaloid and it was mentioned in some older works that it can inhibit some kinds ofAChE.We reinvestigated this effect onAChE and also on BChE using acetyl (butyryl) thiocholine and Ellman’s reagents as standard substances for spectrophotometric assay.We found out IC50 of AChE equal to 372 𝜇mol/l and a similar level to BChE, 321 𝜇mol/l.We conclude our experiment by a finding that boldine is cholinesterase inhibitor; however we report significantly weaker inhibition than that suggested in literature. Likewise, we tried to investigate the mechanism of inhibition and completed it with in silico study. Potential toxic effect on cholinesterases in real conditions is also discussed. Acetylcholinesterase; butyrylcholinesterase; inhibition; docking; boldine

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