WoS İndeksli Yayınlar Koleksiyonu

Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6

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Subject: search.filters.subject.Enzyme Inhibition

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  • Article
    Synthesis, Molecular Modeling, Anti-Cancer and COX-1/2 Inhibitory Activities of Novel Thiazolidinones Containing Benzothiazole Core
    (Bangladesh Pharmacological Society, 2024) Kulabas, Necla; Guven, Cansu Tamniku; Duracık, Merve; Bingol Ozakpinar, Ozlem; Küçükgüzel, İlkay; Ozakpinar, Ozlem Bingol
    In this study, new 1,3-thiazolidin-4-one derivatives containing arylmethylene groups in the 5-position were obtained from 6-(trifluoromethoxy)-1,3-benzo-thiazol-2-amine (riluzole). Synthesized compounds were characterized by spectral data and elemental analysis. In vitro, cytotoxic activities of the synthesized molecules were evaluated against the human lung cancer (A549) and human prostate cancer (PC-3) cell lines. Compounds were also tested on mouse embryonic fibroblast cells (NIH/3T3) to determine selectivity. Ten target compounds 3-12 were also screened for their COX-1 and COX-2 inhibitory activities. Of these compounds, 4 showed the highest COX-2 inhibition at 10 μM. Molecular docking calculations were performed to understand the binding interactions of compounds with COX-1 and COX-2 proteins. In silico studies of the tested compounds represented important binding modes that may be responsible for their anti-cancer activity via selective inhibition of the COX-2 enzyme. ADMET predictions were conducted to assess the drug-like properties of the novel compounds. © 2024 Elsevier B.V., All rights reserved.
  • Article
    Citation - WoS: 4
    Citation - Scopus: 4
    Determination of Chemical Composition and Antioxidant, Cytotoxic, Antimicrobial, and Enzyme Inhibition Activities of <i>rumex Acetosella</I> L. Plant Extract
    (Springer int Publ Ag, 2024) Kandemir, Sevgi Irtegun; Aktepe, Necmettin; Baran, Ayse; Baran, Mehmet Firat; Atalar, Mehmet Nuri; Keskin, Cumali; Khalilov, Rovshan; Irtegün Kandemir, Sevgi
    Purpose The phenolic composition, antioxidant, antimicrobial activity, enzyme inhibition activity, and cytotoxic activity potentials of the plant Rumex acetosella L. (R. acetosella) were examined in this study. Materials and Methods: The chemical composition of R. acetosella methanol extract was identified by the LC-MS/MS method. The antioxidant activity was tested using beta-carotene/linoleic acid, DPPH free radical scavenging, ABTS cation radical scavenging, CUPRAC reducing power, and metal chelating activity methods. The cytotoxic activity was determined by the MTT assay using human ovarian adenocarcinoma (Skov-3), glioblastoma (U87), human dermal fibroblasts (HDF), and human colorectal adenocarcinoma (CaCo-2) cell lines. The antimicrobial activity of methanolic extracts was tested on gram-negative (Escherichia coli and Pseudomonas aeuriginosa) and gram-positive bacteria (Staphylococcus aureus and Bacillus subtilis) using the in vitro minimum inhibition concentration method (MIC). Enzyme inhibition activity of R. acetosella methanol extract was measured spectrophotometrically against acetylcholinesterase (AChE) and glutathione S-transferase (GST) enzymes. Results: The findings showed that the major components of the methanol extract content were luteolin-7-O-glucoside (1.599 m/L), polydatin (91,024 m/L), and shikimic acid (0.773 m/L). It was determined that the extract and standard antioxidant (a-tocopherol) results in DPPH center dot, and ABTS center dot + tests performed to determine the antioxidant activity were close to each other, and this value was more effective than the standard antioxidant (alpha-tocopherol) in the CUPRAC test. These results suggested that the plant's antioxidant potential was higher when compared with reference antioxidant compounds. It was determined that the methanol extract of R. acetosella had a weaker effect on the growth of the tested microorganisms than the antibiotics used as standard. The activity of the GST and AChE enzymes was found to be severely inhibited by the methanol extract of R. acetosella. Conclusion: Based on these findings, R. acetosella L. is a medicinal and commercially beneficial plant that warrants further investigation.