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TOPÇU, GÜLAÇTI

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GÜLAÇTI
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TOPÇU
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Start date: 2020 × End date: 2023 × Author: Topçu G. ×

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Now showing 1 - 7 of 7
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    Importance of Functional Foods in Brain Health
    (2023-03-19) Topçu G.; TOPÇU, GÜLAÇTI
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    Synthesis and Comprehensive in Vivo Activity Profiling of Olean-12-en-28-ol, 3β-Pentacosanoate in Experimental Autoimmune Encephalomyelitis: A Natural Remyelinating and Anti-Inflammatory Agent
    (2023-01-01) Şenol H.; Özgün Acar Ö.; Dağ A.; Eken A.; Güner H.; Aykut Z. G.; Topçu G.; Şen A.; ŞENOL, HALIL; DAĞ, AYDAN; TOPÇU, GÜLAÇTI
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    Functional Food Ingredients for Brain Health and Cancer Chemoprevention
    (2022-10-02) Topçu G.; TOPÇU, GÜLAÇTI
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    PublicationOpen Access
    Isoquinoline alkaloids isolated from Glaucium corniculatum var. corniculatum and Glaucium grandiflorum subsp. refractum var. torquatum with bioactivity studies
    (2023-06-01) Kuşman Sayğı T.; Tan N.; Alim Toraman G. Ö.; Gürer Ç.; Tugay O.; Topçu G.; ALİM TORAMAN, GÜLBAHAR ÖZGE; TOPÇU, GÜLAÇTI
    Context: The genus Glaucium Mill., one of the important Papaveraceae family plants, is rich in isoquinoline alkaloids and distributed worldwide. Objective: Isolation and identification of bioactive alkaloids from Glaucium grandiflorum Boiss. & Huet. subsp. refractum (Nabelek) Mory var. torquatum (Cullen) Mory and G. corniculatum (L.) Rudolph var. corniculatum (Aslan 2012), and investigation of their antioxidant and anticholinesterase activities. Materials and methods: The aerial parts of each plant were dried, powdered, and percolated with methanol, then each extract was fractionated between 50% aqueous acetic acid and petroleum. Their aqueous acidic layer was adjusted to pH 7-8 with NH4OH and extracted with chloroform, the extract was subjected to CC separation and isolation. Structures of the isolated alkaloids were elucidated by 1D and 2D-NMR and mass spectral analyses. The alkaloid extracts and their pure alkaloids were tested for anti-cholinesterase (AChE and BuChE) and antioxidant (ABTS, CUPRAC, β-carotene linoleic acid tests) activities in vitro. Results: Methanol extracts of Glaucium grandiflorum subsp. refractum var. torquatum and G. corniculatum var. corniculatum afforded a novel compound glauciumoline and seven known isoquinoline alkaloids three of which have an aporphine-type and the other five have a protopine-type skeleton. Among them, trans-protopinium (7) and cis-protopinium (8) were isolated from a Glaucium species for the first time. Tertiary amine extracts (TAEs) of both plants showed very strong acetylcholinesterase inhibitory activity. The TAE of the plants also showed strong antioxidant activity while the isolated alkaloids showed no meaningful activity in the anticholinesterase and antioxidant tests. Discussion and conclusions: Glaucium species are considered promising therapeutic agents in the treatment of Alzheimer's disease.
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    PublicationOpen Access
    Synthesis and anticancer activity of novel derivatives of α,β‐unsaturated ketones based on oleanolic acid: in vitro and in silico studies against prostate cancer cells
    (2023-08-01) Şenol H.; Ghaffari-Moghaddam M.; Bulut Ş.; Akbaş F.; Köse A.; Topçu G.; ŞENOL, HALIL; AKBAŞ, FAHRİ; TOPÇU, GÜLAÇTI
    Herein, new derivatives of α,β-unsaturated ketones based on oleanolic acid (4 a-i) were designed, synthesized, characterized, and tested against human prostate cancer (PC3). According to the in vitro cytotoxic study, title compounds (4 a-i) showed significantly lower toxicity toward healthy cells (HUVEC) in comparison with the reference drug doxorubicin. The compounds with the lowest IC50 values on PC3 cell lines were 4 b (7.785 μM), 4 c (8.869 μM), and 4 e (8.765 μM). The results of the ADME calculations showed that the drug-likeness parameters were within the defined ranges according to Lipinski's and Jorgensen's rules. For the most potent compounds 4 b, 4 c, and 4 e, a molecular docking analysis using the induced fit docking (IFD) protocol was performed against three protein targets (PARP, PI3K, and mTOR). Based on the IFD scores, compound 4 b had the highest calculated affinity for PARP1, while compound 4 c had higher affinities for mTOR and PI3K. The MM-GBSA calculations showed that the most potent compounds had high binding affinities and formed stable complexes with the protein targets. Finally, a 50 ns molecular dynamics simulation was performed to study the behavior of protein target complexes under in silico physiological conditions.