About: Cholinesterase inhibitory activities of some flavonoid derivatives and chosen xanthone and their molecular docking studies     Goto   Sponge   NotDistinct   Permalink

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  • Flavonoids are one of the largest classes of plant secondary metabolites and are known to possess a number of significant biological activities for human health. In this study, we examined in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of four flavonoid derivatives quercetin, rutin, kaempferol 3-O-β-d-galactoside and macluraxanthone. The in vitro results showed that quercetin and macluraxanthone displayed a concentration-dependant inhibition of AChE and BChE. Macluraxanthone showed to be the most potent and specific inhibitor of both the enzymes having the IC50 values of 8.47 and 29.8 μM, respectively. The enzyme kinetic studies revealed that quercetin inhibited both the enzymes in competitive manner, whereas the mode of inhibition of macluraxanthone was non-competitive against AChE and competitive against BChE. The inhibitory profiles of the compounds have been compared with standard AChE inhibitor galanthamine. To get insight of the intermolecul
  • Flavonoids are one of the largest classes of plant secondary metabolites and are known to possess a number of significant biological activities for human health. In this study, we examined in vitro acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) inhibitory activities of four flavonoid derivatives quercetin, rutin, kaempferol 3-O-β-d-galactoside and macluraxanthone. The in vitro results showed that quercetin and macluraxanthone displayed a concentration-dependant inhibition of AChE and BChE. Macluraxanthone showed to be the most potent and specific inhibitor of both the enzymes having the IC50 values of 8.47 and 29.8 μM, respectively. The enzyme kinetic studies revealed that quercetin inhibited both the enzymes in competitive manner, whereas the mode of inhibition of macluraxanthone was non-competitive against AChE and competitive against BChE. The inhibitory profiles of the compounds have been compared with standard AChE inhibitor galanthamine. To get insight of the intermolecul (en)
Title
  • Cholinesterase inhibitory activities of some flavonoid derivatives and chosen xanthone and their molecular docking studies
  • Cholinesterase inhibitory activities of some flavonoid derivatives and chosen xanthone and their molecular docking studies (en)
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  • Cholinesterase inhibitory activities of some flavonoid derivatives and chosen xanthone and their molecular docking studies
  • Cholinesterase inhibitory activities of some flavonoid derivatives and chosen xanthone and their molecular docking studies (en)
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  • RIV/62157124:16370/09:00002069!RIV10-MSM-16370___
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  • 306993
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  • RIV/62157124:16370/09:00002069
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  • Alzheimer's disease; Acetylcholinesterase; Butyrylcholinesterase; Flavonoids; Xanthone; Molecular docking Alzheimer's disease; Acetylcholinesterase; Butyrylcholinesterase; Flavonoids; Xanthone; Molecular docking (en)
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  • [A0B0C7D8C203]
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  • Chemico-biological interactions
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  • 181
http://linked.open...iv/tvurceVysledku
  • Šmejkal, Karel
  • Šlapetová, Tereza
  • Dvorská, Margita
  • Kartal, Murat
  • Khan, Mahmud
  • Orhan, Ilkay
  • Sener, Bilge
  • Senol, Sezer
http://linked.open...ain/vavai/riv/wos
  • 000271043800014
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  • 0009-2797
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  • 16370
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