FRINK Linked Data Fragments server

Matches in SemOpenAlex for { <https://semopenalex.org/work/W3017363733> ?p ?o ?g. }

• W3017363733 endingPage "181" @default.
• W3017363733 startingPage "175" @default.
• W3017363733 abstract "All cholinesterase (ChE) inhibitory drugs in clinical use are nitrogenous compounds and among them, galanthamine as the latest anticholinesterase drug, contains a tetrahydroisoquinoline structure. For this reason, isoquinoline alkaloids seem to be attractive in search for novel drug candidates towards Alzheimer's disease (AD). Therefore, in the current work, we investigated inhibitory capacity of several alkaloids representing expanding group of biogenetically-related isoquinoline alkaloids from the Amaryllidaceae including lycorine, (+)-9-O-demethylhomolycorine, 6-hydroxybuphanisine, 9-O-demethoxymontanine, 3-epi-hydroxy-bulbispermine, tazettine, haemanthamine, (+)-haemanthidine, (-)-crinine, 8-hydroxy-9-methoxycrinine, and N-norgalanthamine against ChEs by microtiter enzyme inhibition assays. Our findings indicated that N-norgalanthamine is the most active one inhibiting both acetylcholinesterase (AChE, IC50 = 2.42 ± 0.16 µg/mL) and butyrylcholinesterase (BChE, IC50 = 20.87 ± 1.01 µg/mL) at 100 μg/mL, whereas IC50 values of galanthamine used as the reference were 1.33 ± 0.11 µg/mL and 37.69 ± 2.93 µg/mL for AChE and BChE, respectively. Beside this, 8-hydroxy-9-methoxycrinine was a strong inhibitor of AChE (IC50 = 6.92 ± 0.51 µg/mL), while (+)-9-O-demethylhomolycorine displayed a moderate BChE inhibition (IC50 = 83.57 ± 1.36 µg/mL). Relevantly, 8-hydroxy-9-methoxycrinine and N-norgalanthamine were docked into active gorges of hAChE (PDB: 4EY6) and hBChE (PDB: 4TPK), which pointed out the detail that N-norgalanthamine displayed a very similar binding mode of to that of galanthamine. Moreover, both AChE-inhibiting alkaloids were found to stably bind to hAChE active site occupying the middle of the gorge between the catalytic site and the peripheral anionic site. 8-Hydroxy-9-methoxycrinine was also docked into the active site of BChE. We can conclude that among the tested alkaloids, N-norgalanthamine with dual ChE inhibitory effect seems to be the most promising anti-Alzheimer candidate molecule for future experiments." @default.
• W3017363733 created "2020-04-24" @default.
• W3017363733 creator A5004481451 @default.
• W3017363733 creator A5052108258 @default.
• W3017363733 creator A5077276290 @default.
• W3017363733 creator A5082663764 @default.
• W3017363733 date "2021-01-01" @default.
• W3017363733 modified "2023-10-03" @default.
• W3017363733 title "Molecular approach to promising cholinesterase inhibitory effect of several amaryllidaceae alkaloids: Further re-investigation" @default.
• W3017363733 cites W1578593546 @default.
• W3017363733 cites W1602284078 @default.
• W3017363733 cites W1971048984 @default.
• W3017363733 cites W1973885230 @default.
• W3017363733 cites W1975463072 @default.
• W3017363733 cites W2012421490 @default.
• W3017363733 cites W2016509150 @default.
• W3017363733 cites W2027627734 @default.
• W3017363733 cites W2034863319 @default.
• W3017363733 cites W2039132949 @default.
• W3017363733 cites W2051068796 @default.
• W3017363733 cites W2075304800 @default.
• W3017363733 cites W2092853296 @default.
• W3017363733 cites W2102377211 @default.
• W3017363733 cites W2112006614 @default.
• W3017363733 cites W2116642619 @default.
• W3017363733 cites W2165960918 @default.
• W3017363733 cites W2229763888 @default.
• W3017363733 cites W2235587340 @default.
• W3017363733 cites W2274811202 @default.
• W3017363733 cites W2317110841 @default.
• W3017363733 cites W2411084687 @default.
• W3017363733 cites W2487766919 @default.
• W3017363733 cites W2580711452 @default.
• W3017363733 cites W2605149391 @default.
• W3017363733 cites W2748019328 @default.
• W3017363733 cites W2748973442 @default.
• W3017363733 cites W2749988758 @default.
• W3017363733 cites W2796118964 @default.
• W3017363733 cites W2913678295 @default.
• W3017363733 cites W2943954503 @default.
• W3017363733 cites W2801015199 @default.
• W3017363733 doi "https://doi.org/10.1016/j.sajb.2020.03.017" @default.
• W3017363733 hasPublicationYear "2021" @default.
• W3017363733 type Work @default.
• W3017363733 sameAs 3017363733 @default.
• W3017363733 citedByCount "10" @default.
• W3017363733 countsByYear W30173637332021 @default.
• W3017363733 countsByYear W30173637332022 @default.
• W3017363733 countsByYear W30173637332023 @default.
• W3017363733 crossrefType "journal-article" @default.
• W3017363733 hasAuthorship W3017363733A5004481451 @default.
• W3017363733 hasAuthorship W3017363733A5052108258 @default.
• W3017363733 hasAuthorship W3017363733A5077276290 @default.
• W3017363733 hasAuthorship W3017363733A5082663764 @default.
• W3017363733 hasBestOaLocation W30173637331 @default.
• W3017363733 hasConcept C142724271 @default.
• W3017363733 hasConcept C169760540 @default.
• W3017363733 hasConcept C17077164 @default.
• W3017363733 hasConcept C181199279 @default.
• W3017363733 hasConcept C185592680 @default.
• W3017363733 hasConcept C202751555 @default.
• W3017363733 hasConcept C2776923262 @default.
• W3017363733 hasConcept C2777667214 @default.
• W3017363733 hasConcept C2777752497 @default.
• W3017363733 hasConcept C2778105851 @default.
• W3017363733 hasConcept C2778816929 @default.
• W3017363733 hasConcept C2779056891 @default.
• W3017363733 hasConcept C2779059548 @default.
• W3017363733 hasConcept C2779101902 @default.
• W3017363733 hasConcept C2779134260 @default.
• W3017363733 hasConcept C2779483572 @default.
• W3017363733 hasConcept C2780904820 @default.
• W3017363733 hasConcept C2781465977 @default.
• W3017363733 hasConcept C2910425318 @default.
• W3017363733 hasConcept C31896038 @default.
• W3017363733 hasConcept C55493867 @default.
• W3017363733 hasConcept C59822182 @default.
• W3017363733 hasConcept C65556437 @default.
• W3017363733 hasConcept C71240020 @default.
• W3017363733 hasConcept C71924100 @default.
• W3017363733 hasConcept C86803240 @default.
• W3017363733 hasConcept C98274493 @default.
• W3017363733 hasConceptScore W3017363733C142724271 @default.
• W3017363733 hasConceptScore W3017363733C169760540 @default.
• W3017363733 hasConceptScore W3017363733C17077164 @default.
• W3017363733 hasConceptScore W3017363733C181199279 @default.
• W3017363733 hasConceptScore W3017363733C185592680 @default.
• W3017363733 hasConceptScore W3017363733C202751555 @default.
• W3017363733 hasConceptScore W3017363733C2776923262 @default.
• W3017363733 hasConceptScore W3017363733C2777667214 @default.
• W3017363733 hasConceptScore W3017363733C2777752497 @default.
• W3017363733 hasConceptScore W3017363733C2778105851 @default.
• W3017363733 hasConceptScore W3017363733C2778816929 @default.
• W3017363733 hasConceptScore W3017363733C2779056891 @default.
• W3017363733 hasConceptScore W3017363733C2779059548 @default.
• W3017363733 hasConceptScore W3017363733C2779101902 @default.
• W3017363733 hasConceptScore W3017363733C2779134260 @default.
• W3017363733 hasConceptScore W3017363733C2779483572 @default.

• next