Oleuropein and Verbascoside - Their Inhibition Effects on Carbonic Anhydrase and Molecular Docking Studies
Küçük Resim Yok
Tarih
2021
Dergi Başlığı
Dergi ISSN
Cilt Başlığı
Yayıncı
Japan Oil Chemists Soc
Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Recently, carbonic anhydrase (CA, E.C.4.2.1.1) inhibitors from natural product have paved the way for novel drug design in the treatment and prevention of some global diseases such as glaucoma, diabetes, and cancer. For this purpose, the inhibition effects of oleuropein and verbascoside from olive (Olea europaea L.) oil on human carbonic anhydrase I, and II (hCA I, and II) isoenzymes were evaluated in the current study. The inhibition effects of both natural compounds were determined by the esterase activity (in vitro). IC50 value of oleuropein and verbascoside was calculated as 1.57 and 1.73 mu M for hCA I isoenzyme, respectively. At the same manner, K-i values were determined as 1.25 +/- 0.42 and 2.00 +/- 0.42 mu M, respectively. Then, IC50 value of each compound for hCA II isoenzyme was calculated as 2.23 and 1.90 mu M, respectively. Similarly, K-i values were determined as 2.37 +/- 0.87 mu M and 1.49 +/- 0.33 mu M, respectively. Also, the inhibitory effects and potent binding mechanisms of oleuropein and verbascoside on hCA I, and II isoenzymes were realized by molecular docking studies. Consequently, both natural phenolic compounds demonstrated the potent inhibition profiles against the both isoenzymes. Therefore, we believe that these results may break new ground in the drug development for the treatment of some global disorders.
Açıklama
Anahtar Kelimeler
oleuropein, verbascoside, carbonic anhydrase, enzyme inhibition, molecular docking
Kaynak
Journal of Oleo Science
WoS Q Değeri
Q3
Scopus Q Değeri
Q3
Cilt
70
Sayı
9
