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dc.contributor.authorErdoğan Orhan, İlkay
dc.contributor.authorTosun, Fatma
dc.contributor.authorŞenol Deniz, Fatma Sezer
dc.contributor.authorEren, Gökçen
dc.contributor.authorMıhoğlugil, Feyyaz
dc.contributor.authorAkalgan, Demet
dc.contributor.authorMiski, Mahmut
dc.date.accessioned2021-06-04T06:02:09Z
dc.date.available2021-06-04T06:02:09Z
dc.date.issued2021en_US
dc.identifier.citationErdoğan Orhan, İ., Tosun, F., Şenol Deniz, F. S., Eren, G., Mıhoğlugil, F., Akalgan, D. ... Miski, M. (2021). Butyrylcholinesterase-inhibiting natural coumarin molecules as potential leads. Phytochemistry Letters, 44, 48-54. https://dx.doi.org/10.1016/j.phytol.2021.05.001en_US
dc.identifier.issn1874-3900
dc.identifier.issn1876-7486
dc.identifier.urihttps://dx.doi.org/10.1016/j.phytol.2021.05.001
dc.identifier.urihttps://hdl.handle.net/20.500.12511/7029
dc.description.abstractSeventeen natural coumarin derivatives; badrakemin (1), 14′-acetoxybadrakemin (2), badrakemone (3), 14′-acetoxybadrakemone (4), colladonin (5), colladonin acetate (6), 14′-acetoxycolladonin (7), karatavicinol (8), deltoin (9), smyrnioridin (10), marmesin (11), osthol (12), oxypeucedanin (13), oxypeucedanin hydrate (14), isoimperatorin (15), scopoletin (16), and umbelliprenin (17), were tested against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE), the sister enzymes that play a critical role in the pathology of Alzheimer's disease as well as tyrosinase (TYR) as the target for Parkinson's disease. The tested coumarins were more selective against BChE, where the coumarins 2, 5, 8, and 15 (IC50 = 30.3 μM, 29.2 μM, 37.2 μM, and 50.1 μM, respectively) displayed higher BChE inhibition than the reference (galanthamine, IC50 = 60.2 μM) at 100 μg/mL. Only four coumarins (2, 5, 9, and 15) showed inhibition against AChE. Binding conformations of the coumarins (2, 5, 8, 9, and 15) within the active sites of AChE and BChE were explored via molecular docking experiments. The docked compounds were oriented by the interactions with the oxyanion hole and the peripheral anionic site residues of AChE/BChE. The coumarin derivatives 1–17 was found to have no or low inhibition (2.03 ± 0.92 %–12.91 ± 0.40 %) against TYR at 100 μg/mL. Our findings revealed that coumarins could be promising lead compounds for designing novel anti-Alzheimer drug candidates.en_US
dc.language.isoengen_US
dc.publisherElsevier Ltden_US
dc.rightsinfo:eu-repo/semantics/embargoedAccessen_US
dc.subjectAlzheimer's Diseaseen_US
dc.subjectCholinesteraseen_US
dc.subjectCoumarinen_US
dc.subjectMolecular Dockingen_US
dc.subjectTyrosinaseen_US
dc.titleButyrylcholinesterase-inhibiting natural coumarin molecules as potential leadsen_US
dc.typearticleen_US
dc.relation.ispartofPhytochemistry Lettersen_US
dc.departmentİstanbul Medipol Üniversitesi, Eczacılık Fakültesi, Eczacılık Meslek Bilimleri Bölümü, Farmakognozi Ana Bilim Dalıen_US
dc.authorid0000-0003-2533-5141en_US
dc.identifier.volume44en_US
dc.identifier.startpage48en_US
dc.identifier.endpage54en_US
dc.relation.publicationcategoryMakale - Uluslararası Hakemli Dergi - Kurum Öğretim Elemanıen_US
dc.identifier.doi10.1016/j.phytol.2021.05.001en_US
dc.identifier.wosqualityQ3en_US
dc.identifier.scopusqualityQ2en_US


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