Characterization and inhibition studies of an alpha-carbonic anhydrase from the endangered sturgeon species Acipenser gueldenstaedti

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KOLAYLI S., Karahalil F., Şahin H., DINCER B., Supuran C. T.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.26, sa.6, ss.895-900, 2011 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 26 Sayı: 6
  • Basım Tarihi: 2011
  • Doi Numarası: 10.3109/14756366.2011.554415
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.895-900
  • Anahtar Kelimeler: Carbonic anhydrase, sturgeon, enzyme inhibition, pesticides, dithiocarbamate, TROUT ONCORHYNCHUS-MYKISS, IN-VITRO INHIBITION, THERAPEUTIC APPLICATIONS, ENZYME-ACTIVITIES, ISOFORMS-I, ERYTHROCYTES, PURIFICATION, DERIVATIVES, PHENOLS, XIV
  • Karadeniz Teknik Üniversitesi Adresli: Evet

Özet

An alpha-carbonic anhydrase (CA, EC 4.2.1.1) was purified and characterized kinetically from erythrocytes of the sturgeon Acipenser gueldenstaedti, an endangered species. The sturgeon enzyme (AgCA) showed kinetic parameters for the CO(2) hydration reaction comparable with those of the human erythrocytes enzyme hCA II, being a highly active enzyme, whereas its esterase activity with 4-nitrophenyl acetate as substrate was lower. Sulphonamide inhibitors (acetazolamide, sulphanilamide) strongly inhibited AgCA, whereas metal ions (Ag(+), Zn(2+), Cu(2+) and Co(2+)) were weak, millimolar inhibitors. Several widely used pesticides (2,4-dichlorophenol, dithiocarbamates, parathion and carbaryl) were also assayed as inhibitors of this enzyme. The dithiocarbamates were low micromolar AgCA inhibitors (IC(50) of 16-18 mu M), whereas the other pesticides inhibited the enzyme with IC(50)s in the range of 102-398 mu M. The wide use of dithiocarbamate pesticides may be one of the factors enhancing the vulnerability of this sturgeon species to pollutants.