İnsan karbonik anhidraz I,II izoenzim aktiviteleri üzerine bazı tiyocrown eterlerin etkisi

Akkemik, Ebru; Çalışır, Ümit; Çiçek, Baki

doi:10.25092/baunfbed.340617

Cited by 8 publications

(8 citation statements)

References 31 publications

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“…Today, CA enzyme is seen to be the focus of interest for many researchers due to wide distribution range in tissues and vital functions . Both the inhibitors and the activators of the enzyme have therapeutic effect for various diseases so the enzyme has pulled attention of the researchers . Our previous studies have led us to consider that crown ethers could have activation effect.…”

Section: Discussionmentioning

confidence: 99%

“…Both the inhibitors and the activators of the enzyme have therapeutic effect for various diseases so the enzyme has pulled attention of the researchers . Our previous studies have led us to consider that crown ethers could have activation effect. Considering that CA II activators could be used for treatment of AD, novel activators of I and II isoenzymes of CA enzyme could be tried to be detected in the present study.…”

Section: Discussionmentioning

confidence: 99%

“…In Figure B, crown ethers are suggested to pull the metal atom outward the enzyme due to the internal cavity and thereby enhance the contact of the enzyme to the substrate. So the enzyme that interact with the substrate faster and easier accelerates the reaction . In inhibition mechanism shown in Figure C, crown ethers are suggested to interact with the active part of the enzyme and hinder or block the interaction between the enzyme and the substrate …”

Section: Discussionmentioning

confidence: 99%

“…280 nm of absorbance was tested in the obtained elutions and high enzyme content was detected. Active fractions were dialyzed one night against 0.05 M Tris–SO 4 (pH 7.4) buffer . Protein detection was done with Bradford method in all fractions .…”

Section: Methodsmentioning

confidence: 99%

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The determination of the carbonic anhydrases activators in vitro effect of mixed donor crown ethers

Akkemik

Çiçek

Camadan

et al. 2018

J Biochem & Molecular Tox

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Carbonic anhydrases (CAs) play an important function in various physiological and pathological processes. Therefore, many researchers work in this field in order to design and synthesize new drugs. Both inhibitors and activators of CAs, which are associated with the diagnosis and treatment of many diseases, are very important. The emergence of the use of CA activators in the treatment of Alzheimer has led many scholars to work on this issue. In this study, CA activators and inhibitors are determined. The crown ethers compounds (1, 2, 3, 6, 7, 8, and 9) were found to cause activation on enzyme activities of hCA I and II. The AC values on hCA I and II of the compounds are in the range of 4.6565-374.979 μM. The 4 (IC ; 1.301 and 3.215 μM for hCA I and II) and 5 (IC ; 73.96 and 378.5 μM for hCA I and II) compounds were found to cause inhibition on enzyme activities of hCA I and II.

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Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

See 2 more Smart Citations

The determination of the carbonic anhydrases activators in vitro effect of mixed donor crown ethers

Akkemik

Çiçek

Camadan

et al. 2018

J Biochem & Molecular Tox

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“…Bazı tiyo taç eterlerin karbonik anhidraz ve polifenol oksidaz enzimlerini inhibe ettiği literatürde belirtilmiştir [40][41][42][43]. Tiyo taç eterlerin metal iyonlarına olan ilgisinden dolayı söz konusu çalışmada inhibitör olarak kullandığımız bileşik, biyomolekül olan PON1 enziminin aktif bölgesindeki Ca 2+ iyonu ile etkileşime girerek inhibe ettiği söylenebilir.…”

Section: Sonuçlar Ve Tartışmaunclassified

PON1 enzimi üzerine DT-15-Crown-5 taç eterinin etkisinin araştırılması

Ergün

Çiçek

2020

Balıkesir Üniversitesi Fen Bilimleri Enstitüsü Dergisi

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Human serum paraoxonase 1 (PON1, EC3.1.8.1) is an important liver enzyme which is bound to HDL, contains calcium in its active site, hydrolyses organophosphate agents and nerve gases, has protective effect against the formation of lipid peroxides by oxidation of LDL and bacterial endotoxins. In our study, in order to purify the enzyme PON1, it was purified by hydrophobic interaction chromatography using sepharose-4B

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Imidazole-Derived Alkyl and Aryl Ethers: Synthesis, Characterization, In Vitro Anticancer and Antioxidant Activities, Carbonic Anhydrase I–II Inhibition Properties, and In Silico Studies

Faris,

Bostancı,

Özcan

et al. 2024

ACS Omega

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Imidazole derivatives display extensive applications in pharmaceutical chemistry and have been investigated as bioactive compounds for medicinal chemistry. In this study, besides the starting materials (3a−c and 4a−c), synthesis, characterization, and biological activity studies were conducted on a total of 18 compounds, nine of which are known and the other nine are original. The compounds investigated in the study are a series of alkyl (7−15) and aryl (16−24) ether derivatives bearing substituted phenyl and imidazole rings, which were characterized using various methods including 1 H NMR, 13 C NMR, FT-IR analysis, elemental analysis, and mass spectroscopy. Computeraided drug design studies have been carried out to predict the biological activities of compounds. Besides DFT calculations, the binding affinities of the compounds to EGFR, VEGFR2, FGFR1, HSP90, hCA I, and hCA II were investigated. Additionally, druglikeness and ADME analyses were performed on the compounds. Anticancer, antioxidant, and enzyme inhibition activity tests were performed in biological activity studies on the synthesized compounds. Among the synthesized compounds, compounds 17 and 19− 24 generally exhibited inhibition profiles against the widespread cytosolic hCA I isozyme with IC 50 values ranging from 4.13 to 15.67 nM and cytosolic hCA II isozyme with IC 50 values ranging from 5.65 to 14.84 nM. L929 (mouse fibroblast cell line) was used as the control healthy cell line, and MCF7 (breast cancer), C6 (rat glioblastoma), and HT-29 (colon cancer) cells were used in cell culture studies as cancer cell lines. Before the study on cancer cells, all compounds were examined on healthy cells, and their cytotoxicity was determined. As a result of these data, studies continued with six compounds determined to be nontoxic. On cancerous cells, it was determined that compounds 3a, 3b, 4a, 4b, 4c, and 7 had cytotoxic effects on both colon cancer and brain tumors. It was found that compound 3b had a more toxic effect than cisplatin on the glioma cell line with an IC 50 value of 10.721 ± 0.38 μM, and compound 3a had a more toxic effect on the colon cancer cell line with an IC 50 value of 20.88 ± 1.02 μM. However, it was determined that the same compounds did not have a statistically significant effect on breast cancer. Flow cytometry studies also showed that when the IC 50 dose of compound 3b was applied to the C6 cell line, the cells tended to early and late apoptosis. Additionally, it has been shown by flow cytometry that the cell cycle stops in the G0/G1 phase. A similar effect was observed in the colon cancer cell line with compound 3a. Compound 3b caused early and late apoptosis of the colon cancer cell line with the applied IC 50 dose and stopped the cell cycle in the G0/G1 phase. Finally, the FRAP method studied all synthesized compounds' antioxidant effects. According to the measured antioxidant power results, it was determined that no compound had a more effective reducing power than vitamin E.

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İnsan karbonik anhidraz I,II izoenzim aktiviteleri üzerine bazı tiyocrown eterlerin etkisi

Cited by 8 publications

References 31 publications

The determination of the carbonic anhydrases activators in vitro effect of mixed donor crown ethers

The determination of the carbonic anhydrases activators in vitro effect of mixed donor crown ethers

PON1 enzimi üzerine DT-15-Crown-5 taç eterinin etkisinin araştırılması

Imidazole-Derived Alkyl and Aryl Ethers: Synthesis, Characterization, In Vitro Anticancer and Antioxidant Activities, Carbonic Anhydrase I–II Inhibition Properties, and In Silico Studies

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