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    Oleuropein and Verbascoside - Their Inhibition Effects on Carbonic Anhydrase and Molecular Docking Studies
    (Japan Oil Chemists Soc, 2021) Aggul, Ahmet Gokhan; Taslimi, Parham; Kuzu, Muslum; Uzun, Naim; Bilginer, Sinan; Gulcin, Ilhami
    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.
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    Some phenolic natural compounds as carbonic anhydrase inhibitors: An in vitro and in silico study
    (Wiley-V C H Verlag Gmbh, 2022) Aggul, Ahmet Gokhan; Uzun, Naim; Kuzu, Muslum; Taslimi, Parham; Gulcin, Ilhami
    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. IC50 values for hCA I and II were calculated as 2.02-11.38 mu M and 2.23-9.05 mu M, respectively. The compounds were identified as CA inhibitors, with K-i values in the ranges of 1.66-9.17 mu M for the hCA I isozyme and 1.49-14.21 mu M 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.