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

Creative Commons License

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

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, vol.26, no.6, pp.895-900, 2011 (SCI-Expanded) identifier identifier identifier

  • Publication Type: Article / Article
  • Volume: 26 Issue: 6
  • Publication Date: 2011
  • Doi Number: 10.3109/14756366.2011.554415
  • Journal Name: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.895-900
  • Keywords: 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 Technical University Affiliated: Yes

Abstract

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.