WoS İndeksli Yayınlar Koleksiyonu
Permanent URI for this collectionhttps://hdl.handle.net/20.500.14627/6
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Article Citation - WoS: 7Citation - Scopus: 5Synthesis and Evaluation of Novel Metacetamol Derivatives With Hydrazone Moiety as Anticancer and Antimicrobial Agents(Wiley-v C H verlag Gmbh, 2023) Senkardes, Sevil; Atlihan, Irem; Cayir, Elif; Tiber, Pinar Mega; Orun, Oya; Nigiz, Seyma; Kucukguzel, S. Guniz; Mega Tiber, PınarBy exploiting the wide biological potential of the hydrazone scaffold, a series of hydrazone derivatives were synthesized, starting from N-(3-hydroxyphenyl)acetamide (metacetamol). The structures of the compounds were determined using IR, H-1 and C-13-NMR, and mass spectroscopic methods. The obtained molecules (3 a-j) were evaluated for their anticancer potential against MDA-MB-231 and MCF-7 breast cancer cell lines. According to the CCK-8 assay, all tested compounds showed moderate to potent anticancer activity. Among them, N-(3-(2-(2-(4-nitrobenzylidene)hydrazinyl)-2-oxoethoxy)phenyl)acetamide (3 e) was found to be the most effective derivative with an IC50 value of 9.89 & mu;M against MDA-MB-231 cell lines. This compound was further tested for its potential effects on the apoptotic pathway. Molecular docking studies was also carried out for 3 e in the colchicine binding pocket of tubulin. Additionally, compound 3 e also demonstrated effective antifungal activity, particularly against Candida krusei (MIC=8 & mu;g/ml), indicating that nitro group at the 4(th) position of the phenyl ring was the most preferable substituent for both cytotoxic and antimicrobial activity. Our preliminary findings suggest that compound 3 e could be exploited as a leading structure for further anticancer and antifungal drug development.Article Citation - WoS: 4Citation - Scopus: 4Determination 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, SevgiPurpose 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.