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BÜTÜN, BURCU

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Author: TOPÇU, GÜLAÇTI × Type: Article ×

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Now showing 1 - 6 of 6
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    Investigation of Anticholinesterase Activity of a Series of Salvia Extractsand the Constituents of Salvia staminea
    (2013-03-01) Topçu, Gülaçtı; Boğa, Mehmet; Kolak, Ufuk; Öztürk, Mehmet; Dirmenci, Tuncay; Bahadori, Fatemeh; Bütün, Burcu; TOPÇU, GÜLAÇTI; BAHADORİ, FATEMEH; BÜTÜN, BURCU
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    Antioxidant and anticholinesterase activities of lupane triterpenoids and other constituents of Salvia trichoclada
    (2015-11-01) Butun, Burcu; Hatipoglu, Seda Damla; Dönmez, Ayşe; Topcu, Gülaçtı; BÜTÜN, BURCU; TOPÇU, GÜLAÇTI
    The methanol extract of the aerial parts of Salvia trichoclada Bentham (Lamiaceae) was studied for bioactive non-volatile secondary metabolites, and nine compounds were isolated. Structures of the isolated compounds were elucidated as lupeol (1), lupenone (2), glochidone (3), monogynol A (4), oleanolic acid (5), ursolic acid (6), beta-sitosterol (7), apigenin-7-O-rhamnoside (8), and rosmarinic acid (9) by using 1D and 2D-NMR spectroscopic techniques. A lupane triterpene glochidone was isolated from a Salvia species and Lamiaceae family for the first time in this study. The antioxidant potential of the extract and the isolated compounds were carried out by using lipid peroxidation inhibitory activity (beta-carotene bleaching method) and DPPH free radical scavenging activity test assays. Their anticholinesterase activity was investigated by the Ellman method against both acetylcholinesterase (AChE) and butyrylcholinesterase enzymes. Compounds 1, 3, 5, 6, 8 and 9 showed fairly high anticholinesterase activity almost at all concentrations. Among them, a flavone glycoside apigenin-7-O-rhamnoside exhibited the highest and selective AChE inhibitory activity. Glochidone (3) was found to be the most active one among the isolated lupanes, which exhibited a close activity to that of standard compound galanthamine. Among all the tested compounds, rosmarinic acid (9) exhibited highest antioxidant and good anticholinesterase activity.
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    Recent advances on 3-hydroxyflavone derivatives: Structures and properties
    (2018-01-01) Butun, Burcu; TOPÇU, GÜLAÇTI; Öztürk, Turan; BÜTÜN, BURCU; TOPÇU, GÜLAÇTI
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    Antioxidant and Anticholinesterase Activities of Some Dialkylamino Substituted 3-Hydroxyflavone Derivatives
    (2017-01-01) Culhaoglu, Burcu; Capan, Asli; Boga, Mehmet; Ozturk, Mehmet; Öztürk, Turan; Topcu, Gülaçtı; BÜTÜN, BURCU; TOPÇU, GÜLAÇTI
    Background: Flavones, are a class of naturally occuring polyphenolic compounds which have 2-phenylchromen-4-one structure. Various studies showed that flavones have several pharmacological activities such as antioxidant, anti-inflammatory, antimicrobial, cytotoxic, antitumour and antiallergic. In the present study, 3-hydroxyflavones also called flavonols, posessing 4--dialkylamino moiety were synthesized, and their antioxidant and anticholinesterase activities were investigated by comparison with unmodified 3-hydroxflavone.
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    SAR Evaluation of Disubstituted Tacrine Analogues as Promising Cholinesterase and Carbonic Anhydrase Inhibitors
    (2019-04-01) ÖKTEN, S; EKIZ, M; TUTAR, A; BÜTÜN, BURCU; Gülçin, İlhami; TOPÇU, GÜLAÇTI; BÜTÜN, BURCU; TOPÇU, GÜLAÇTI
    Background: The inhibition of both hydrolysis products of acetylcholine (ACh), Acetylcholinesterase (AChE) and Butyrylcholinesterase (BChE), is essential for successful treatment of Alzhemier patients. Objectives: This study was investigated inhibition potentials of recently synthesized disubstituted tacrines derivatives on going our research against AChE, BChE and carbonic anhydrase cyctosolic (hCA I and H) enzymes to explore the Structure activity relationship (SAR). Methods: Inhibitory activities of tested compounds against AChE and BChE were measured by spectrophotometric method, developed by Ellman et al. Furthermore, the disubstituted tacrines were determined as inhibitors of two physiologically relevant CA isoforms, the cytosolic hCA I and H by an esterase assay method. Results: The silyl, thiomethyl and cyano substituted seven membered hydrocycle tacrines (9, 11 and 14) significantly inhibited AChE, compared with starting compound 3 (6,8-dibromo-2,3,4,5-teytrahydro-1H-cyclohepta[1,2-b] quinoline) and reference compounds, galantamine and tacrine, while methoxy substituted seven membered hydrocycle tacrine derivative 10 showed selective inhibition against BChE (IC50 = 563 nM). Interestingly, disubstituted tacrines displayed higher or parallel inhibition to galantamine. Additionally, all these tacrine analogues were recorded to be powerful inhibitor compounds of the cytosolic isoenzyme hCA I with K-i in the range of 43.81-471.67 nM, as well as a moderate selectivity toward hCA II isoenzyme with K-i in the range from 87.14 to 614.68 nM compared with AZA, as standard. Conclusion: The disubstituted seven membered hydrocycle tacrine analogues 9-12 and 14 may have promising anti Alzhemier drug candidate and dibromo six membered hydrocycle 2 and dibromo seven membered hydrocycle 3 derivatives may be novel hCA I and II enzyme inhibitors.
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    Synthesis, characterization, and SAR of arylated indenoquinoline-based cholinesterase and carbonic anhydrase inhibitors.
    (2018-09-01) EKIZ, M; TUTAR, A; ÖKTEN, S; Bütün, BURCU; KOÇYIĞIT, ÜM; TASLIMI, P; TOPÇU, GÜLAÇTI; BÜTÜN, BURCU; TOPÇU, GÜLAÇTI