101. Comparison of Inhibition Effects of Some Benzoic acid Derivatives on Sheep Heart Carbonic Anhydrase
- Author
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Melike Yildiz, Orhan Erdoğan, Ömer İrfan Küfrevioğlu, Deryanur Kilic, Murat Şentürk, Aslan, I, Bayrak, Y, Akdemir, AO, Ekinci, A, Polat, K, Dadasoglu, F, Turkoglu, EA, Belirlenecek, and deryanur -- 0000-0002-9115-136X
- Subjects
chemistry.chemical_classification ,biology ,Stereochemistry ,Cofactor ,In vitro ,chemistry.chemical_compound ,Enzyme ,Biochemistry ,chemistry ,Affinity chromatography ,Carbonic anhydrase ,Yield (chemistry) ,biology.protein ,Ic50 values ,Benzoic acid - Abstract
International Conference on Advances in Natural and Applied Sciences (ICANAS) -- APR 21-23, 2016 -- Antalya, TURKEY, Carbonic anhydrase (CA) is a family of metalloenzymes that requires Zn as a cofactor and catalyze the quick conversion of CO2 to HCO3- and H+. Inhibitors of the carbonic anhydrases (CAs) have medical usage of significant diseases such as glaucoma, epilepsy, gastroduodenal ulcers, acid-base disequilibria and neurological disorders. In the present study, inhibition of CA with some benzoic derivatives (1-6) were investigated. Sheep heart CA (shCA) enzyme was isolated by means of designed affinity chromatography gel (cellulose-benzyl-sulfanylamide) 42.45-fold in a yield of 44 % with 564.65 EU/mg. Purified shCA enzyme was used in vitro studies. In the studies, IC50 values were calculated for 3-aminobenzoic acid (1), 4-aminobenzoic acid (2), 2-hydroxybenzoic acid (3), 2-benzoylbenzoic acid (4), 2,3-dimethoxybenzoic acid (5), and 3,4,5-trimethoxybenzoic acid (6), showing the inhibition effects on the purified enzyme. Such molecules can be used as pioneer for discovery of novel effective CA inhibitors for medicinal chemistry applications.
- Published
- 2016