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Evaluation of chalcones as inhibitors of glutathione S-transferase      
Yazarlar
Muhammet Serhat Özaslan
Ardahan Üniversitesi, Türkiye
Yeliz Demir
Ardahan Üniversitesi, Türkiye
Doç. Dr. Hatice Esra DURAN
Türkiye
Şükrü Beydemir
Anadolu Üniversitesi, Türkiye
Ömer İrfan Küfrevioğlu
Atatürk Üniversitesi, Türkiye
Özet
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 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. K 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.
Anahtar Kelimeler
chalcone,glutathione S-transferase,inhibition,purification
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale
Dergi Adı Journal of Biochemical and Molecular Toxicology
Dergi ISSN 1095-6670
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce
Basım Tarihi 05-2018
Cilt No 32
Sayı 5
Doi Numarası 10.1002/jbt.22047
Makale Linki http://doi.wiley.com/10.1002/jbt.22047
BM Sürdürülebilir Kalkınma Amaçları
Atıf Sayıları
WoS 51
Google Scholar 65
Evaluation of chalcones as inhibitors of glutathione S-transferase

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