Evaluation of chalcones as inhibitors of glutathione S-transferase

Journal of Biochemical and Molecular Toxicology
M Serhat ÖzaslanO Irfan Küfrevioğlu

Abstract

Glutathione S-transferases (GSTs) are the superfamily of multifunctional detoxification isoenzymes and play an important role in cellular signaling. In the present study, potential inhibition effects of chalcones were tested against human GST. For this purpose, GST was purified from human erythrocytes with 5.381 EU⋅mg-1 specific activity and 51.95% yield using a GSH-agarose affinity chromatographic method. The effects of chalcones on in vitro GST activity were tested at various concentrations. Ki constants of chalcones were found in the range of 7.76-41.93 μM. According to the results, 4-fluorochalcone showed a better inhibitory effect compared with the other compounds. The inhibition mechanisms of 2'-hydroxy-4-methoxychalcone and 4-methoxychalcone were noncompetitive, whereas the inhibition mechanisms of 4'- hydroxychalcone, 4- fluorochalcone, and 4,4'- diflurochalcone were competitive.

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Citations

Jun 5, 2018·Drug and Chemical Toxicology·Hatice Esra AslanÖmer Irfan Küfrevioğlu
Jul 18, 2018·Journal of Biochemical and Molecular Toxicology·Muhammet Serhat ÖzaslanŞükrü Beydemir
Dec 27, 2019·Journal of Food Biochemistry·Zeynep KoksalHasan Ozdemir
Feb 19, 2020·Anti-cancer Agents in Medicinal Chemistry·Yeliz DemirŞükrü Beydemir
Mar 5, 2019·Protein and Peptide Letters·Hamid CeylanŞükrü Beydemir
May 7, 2020·International Journal of Molecular Sciences·Karol BukowskiRenata Kontek
May 22, 2019·Pharmacological Reports : PR·Yeliz Demir, Zeynep Köksal
Aug 14, 2020·Journal of Biomolecular Structure & Dynamics·Cüneyt TürkeşŞükrü Beydemir
Oct 3, 2018·Journal of Biochemical and Molecular Toxicology·Jun-Hui ChoiSeung Kim
Aug 24, 2021·Journal of Biomolecular Structure & Dynamics·Yeliz DemirŞükrü Beydemir
May 31, 2018·Biomedicine & Pharmacotherapy = Biomédecine & Pharmacothérapie·Shelly PathaniaRavindra K Rawal

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