Inhibition of Acetylcholinesterase and Butyrylcholinesterase by a Plant Secondary Metabolite Boldine

BioMed Research International
Adam Kostelnik, Miroslav Pohanka

Abstract

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 of AChE. We reinvestigated this effect on AChE 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.

References

Oct 1, 1994·Agents and Actions·N BackhouseH Speisky
Jan 1, 1994·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·H Speisky, B K Cassels
Mar 16, 2001·Expert Opinion on Pharmacotherapy·D G Wilkinson
Jan 18, 2003·Analytical Biochemistry·Peter EyerElsa Reiner
Jul 19, 2003·The Journal of Biological Chemistry·Yvain NicoletFlorian Nachon
Jul 1, 1961·Biochemical Pharmacology·G L ELLMANR M FEATHER-STONE
Jul 21, 2004·Journal of Computational Chemistry·Eric F PettersenThomas E Ferrin
Oct 14, 2005·Chemico-biological Interactions·Peter O'BrienHernán Speisky
Feb 9, 2010·Chemico-biological Interactions·Hay DvirJoel L Sussman
Jun 30, 2010·Journal of Enzyme Inhibition and Medicinal Chemistry·Stevan PecicWayne W Harding
Jan 31, 2012·Biomedical Papers of the Medical Faculty of the University Palacký, Olomouc, Czechoslovakia·Miroslav Pohanka
Jul 10, 2012·Expert Opinion on Therapeutic Patents·Miroslav Pohanka
Dec 18, 2013·Bratislavské lekárske listy·M Pohanka

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Citations

Aug 30, 2020·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Geum Seok JeongHoon Kim
Feb 13, 2021·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Yew Rong KongKooi Yeong Khaw
Mar 9, 2021·Frontiers in Pharmacology·Chee Kei KongPoh Hui Goh
Jan 28, 2020·Combinatorial Chemistry & High Throughput Screening·Hayrettin O Gulcan, Ilkay E Orhan

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