Evaluation of chalcones as inhibitors of glutathione S‐transferase |
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| Authors: | Muhammet Serhat Özaslan Yeliz Demir Hatice Esra Aslan ?ükrü Beydemir Ömer ?rfan Küfrevio?lu |
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| Affiliation: | 1. Faculty of Sciences, Department of Chemistry, Atatürk University, Erzurum, Turkey;2. Faculty of Pharmacy, Department of Biochemistry, Anadolu University, Eski?ehir, Turkey |
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| 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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| Keywords: | chalcone glutathione S‐transferase inhibition purification |
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