Comparison of Inhibition Effects of Some Benzoic acid Derivatives on Sheep Heart Carbonic Anhydrase


KILIÇ D., YILDIZ M., Senturk M., ERDOĞAN O., KÜFREVİOĞLU Ö. İ.

International Conference on Advances in Natural and Applied Sciences (ICANAS), Antalya, Türkiye, 21 - 23 Nisan 2016, cilt.1726 identifier identifier

  • Yayın Türü: Bildiri / Tam Metin Bildiri
  • Cilt numarası: 1726
  • Doi Numarası: 10.1063/1.4945922
  • Basıldığı Şehir: Antalya
  • Basıldığı Ülke: Türkiye
  • Atatürk Üniversitesi Adresli: Evet

Özet

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.