Cholinesterase inhibition activity and molecular docking study of eugenol derivatives
The study was conducted to explore the anticholinesterase inhibition property of eugenol derived molecules. Ten eugenol derivatives were synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) by Ellman’s method. Most of the te...
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Main Authors: | , , , , , , , , |
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Format: | Article |
Language: | English |
Published: |
Penerbit Universiti Kebangsaan Malaysia
2021
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Online Access: | http://journalarticle.ukm.my/17176/1/14.pdf http://journalarticle.ukm.my/17176/ https://www.ukm.my/jsm/malay_journals/jilid50bil4_2021/KandunganJilid50Bil4_2021.html |
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Summary: | The study was conducted to explore the anticholinesterase inhibition property of eugenol derived molecules. Ten
eugenol derivatives were synthesized and evaluated for the inhibitory activities against acetylcholinesterase (AChE)
and butyrylcholinesterase (BChE) by Ellman’s method. Most of the tested derivatives showed higher inhibition on BChE
than AChE, however, their overall inhibitory activity was weak. In contrast, three derivatives (compounds 3,6,9) showed
higher and good AChE inhibitory activity of more than 50% inhibition at 10 µg/mL. Among them, compound 9
bearing a ethyl substituent at para position of the benzoyl ring showed the most potent AChE inhibition, with IC50 of 5.64
µg/mL. Ligand-protein docking simulation was also performed for the most active derived molecules (compounds 3,6,9). |
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