Evaluation of chalcones as inhibitors of glutathione S-transferase
 
Yazarlar (5)
Doç. Dr. Muhammet Serhat Özaslan Ardahan Üniversitesi, Türkiye
Prof. Dr. Yeliz Demir Ardahan Üniversitesi, Türkiye
Prof. Dr. Şükrü Beydemir Anadolu Üniversitesi, Türkiye
Prof. Dr. Ömer İrfan Küfrevioğlu Atatürk Üniversitesi, Türkiye
Makale Türü Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
Dergi Adı JOURNAL OF BIOCHEMICAL AND MOLECULAR TOXICOLOGY (Q2)
Dergi ISSN 1095-6670 Dergi Bilgileri (2018)
Dergi Tarandığı Indeksler SCI-Expanded
Makale Dili İngilizce Basım Tarihi 05-2018
Kabul Tarihi Yayınlanma Tarihi 23-02-2018
Cilt / Sayı / Sayfa 32 / 5 / – DOI 10.1002/jbt.22047
Makale Linki http://doi.wiley.com/10.1002/jbt.22047
UAK Araştırma Alanları
Tıbbi Biyokimya
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−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.
Anahtar Kelimeler
chalcone | glutathione S-transferase | inhibition | purification
BM Sürdürülebilir Kalkınma Amaçları
Atıf Sayıları
Web of Science 62
Google Scholar 76
Evaluation of chalcones as inhibitors of glutathione S-transferase

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