Some phenolic natural compounds as carbonic anhydrase inhibitors: An in vitro and in silico study        
Yazarlar (5)
Ahmet Gökhan Ağgül
Ağrı İbrahim Çeçen Üniversitesi, Türkiye
Naim Uzun
Ağrı İbrahim Çeçen Üniversitesi, Türkiye
Prof. Dr. Müslüm KUZU Karabük Üniversitesi, Türkiye
Parham Taslımı
Bartın Üniversitesi, Türkiye
İlhami Gülçin
Atatürk Üniversitesi, Türkiye
Makale Türü Özgün Makale
Makale Alt Türü SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale
Dergi Adı Archiv Der Pharmazie
Dergi ISSN 0365-6233 Wos Dergi Scopus Dergi
Dergi Tarandığı Indeksler SCI-Expanded
Dergi Grubu Q2
Makale Dili Türkçe
Basım Tarihi 06-2022
Cilt No 355
Sayı 6
DOI Numarası 10.1002/ardp.202100476
Makale Linki http://dx.doi.org/10.1002/ardp.202100476
Özet
This paper presents experimental and molecular docking studies on the inhibitory effects of tyrosol, hydroxytyrosol, luteolin, diosmetin, caffeic acid, luteolin 7-O-glycoside, and apigenin 7-O-glycoside from olive (Olea europaea L.) leaf against human carbonic anhydrase (hCA, E.C.4.2.1.1) isozymes I and II. After these isozymes were separately purified, their activities were determined using the esterase activity. IC values for hCA I and II were calculated as 2.02-11.38 µM and 2.23-9.05 µM, respectively. The compounds were identified as CA inhibitors, with K values in the ranges of 1.66-9.17 µM for the hCA I isozyme and 1.49-14.21 µM for hCA II. The inhibitory effects of these natural compounds were also compared to acetazolamide, which is a potent inhibitor of both CA isozymes. Our results may contribute to the synthesis of new CA inhibitors and pave the way for new drug design in the treatment of a number of diseases including cancer, obesity, diabetes, and glaucoma.
Anahtar Kelimeler
carbonic anhydrase | enzyme inhibition | molecular docking | olive leaf | phenolic compound