Show simple item record
dc.contributor.author |
Kos, Jiri
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dc.contributor.author |
Strharsky, Tomas
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dc.contributor.author |
Štěpánková, Šárka
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dc.contributor.author |
Svrčková, Katarína
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dc.contributor.author |
Oravec, Michal
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dc.contributor.author |
Hosek, Jan
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dc.contributor.author |
Imramovský, Aleš
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dc.contributor.author |
Jampilek, Josef
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dc.date.accessioned |
2022-06-03T12:29:29Z |
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dc.date.available |
2022-06-03T12:29:29Z |
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dc.date.issued |
2021 |
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dc.identifier.issn |
2076-3417 |
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dc.identifier.uri |
https://hdl.handle.net/10195/79306 |
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dc.description.abstract |
A series of twelve nature-inspired 3,4,5-trimethoxycinnamates were prepared and characterized. All compounds, including the starting 3,4,5-trimethoxycinnamic acid, were tested for their ability to inhibit acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) in vitro; the selectivity index (SI) was also determined. 2-Fluororophenyl (2E)-3-(3,4,5-trimethoxyphenyl)-prop-2-enoate demonstrated the highest SI (1.71) in favor of BChE inhibition. 2-Chlorophenyl (2E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoate showed the highest AChE-inhibiting (IC50 = 46.18 mu M) as well as BChE-inhibiting (IC50 = 32.46 mu M) activity with an SI of 1.42. The mechanism of action of the most potent compound was determined by the Lineweaver-Burk plot as a mixed type of inhibition. An in vitro cell viability assay confirmed the insignificant cytotoxicity of the discussed compounds on the two cell lines. Trends between structure, physicochemical properties and activity were discussed. |
eng |
dc.format |
p. 4691 |
eng |
dc.language.iso |
eng |
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dc.publisher |
MDPI |
eng |
dc.relation.ispartof |
Applied Science - Basel, volume 11, issue: 10 |
eng |
dc.rights |
open access |
eng |
dc.rights.uri |
https://creativecommons.org/licenses/by/4.0/ |
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dc.subject |
trimethoxycinnamates |
eng |
dc.subject |
cholinesterase-inhibiting activity |
eng |
dc.subject |
cytotoxicity |
eng |
dc.subject |
trimethoxycinamáty |
cze |
dc.subject |
inhibiční aktivita cholinesterázy |
cze |
dc.subject |
cytotoxicita |
cze |
dc.title |
Trimethoxycinnamates and Their Cholinesterase Inhibitory Activity |
eng |
dc.title.alternative |
Trimethoxycinnamáty a jejich cholinesterázová inhibitorní aktivita |
cze |
dc.type |
article |
eng |
dc.description.abstract-translated |
Byla připravena a charakterizována série dvanácti přírodou inspirovaných 3,4,5-trimethoxycinnamátů. Všechny sloučeniny, včetně výchozí 3,4,5-trimethoxyskořicové kyseliny, byly testovány na jejich schopnost inhibovat acetylcholinesterázu (AChE) a butyrylcholinesterázu (BChE) in vitro; byl také stanoven index selektivity (SI). 2-Fluorofenyl (2E)-3-(3,4,5-trimethoxyfenyl)-prop-2-enoát vykazoval nejvyšší SI (1,71) ve prospěch inhibice BChE. 2-Chlorfenyl (2E)-3-(3,4,5-trimethoxyfenyl)prop-2-enoát vykazoval nejvyšší aktivitu AChE-inhibice (IC50 = 46,18 uM) i BChE-inhibice (IC50 = 32,46 uM) s SI = 1,42. Mechanismus účinku nejúčinnější sloučeniny byl stanoven pomocí Lineweaver-Burk grafu jako smíšeného typu inhibice. Test životaschopnosti buněk in vitro potvrdil nevýznamnou cytotoxicitu diskutovaných sloučenin na dvou buněčných liniích. Byly diskutovány trendy mezi strukturou, fyzikálně-chemickými vlastnostmi a aktivitou. |
cze |
dc.peerreviewed |
yes |
eng |
dc.publicationstatus |
published version |
eng |
dc.identifier.doi |
10.3390/app11104691 |
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dc.relation.publisherversion |
https://www.mdpi.com/2076-3417/11/10/4691 |
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dc.rights.licence |
CC BY 4.0 |
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dc.identifier.wos |
000662573000001 |
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dc.identifier.scopus |
2-s2.0-85107275734 |
|
dc.identifier.obd |
39886242 |
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