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    Some Anti-Inflammatory Agents Inhibit Esterase Activities of Human Carbonic Anhydrase Isoforms I and II: An In Vitro Study
    (Wiley, 2015) Alim, Zuhal; Kilinc, Namik; Isgor, Mehmet M.; Sengul, Bulent; Beydemir, Sukru
    Carbonic anhydrases (CAs) are known as a drug-target enzymes. The inhibitors of the enzyme are important compounds for discovering new therapeutic agents and understanding in detail protein-drug interactions at the molecular level. For this purpose, the invitro effects of some anti-inflammatory agents such as tenoxicam, fluorometholone acetate, and dexamethasone were investigated on esterase activity of human erythrocyte CA-I and CA-II in this study. hCA-I and hCA-II were purified by affinity chromatography with a yield of 47.25% and 87%, and a specific activity of 642.8EU/mg proteins and 5576.9EU/mg proteins, respectively. SDS-PAGE was performed to determine the purity of the enzymes. Inhibitory effects of the drugs on hCA-I and hCA-II were determined by spectrophotometric method. IC50 values for hCA-I and hCA-II were 0.198, 2.18, 11.7, 0.11, 17.5 and 14m using tenoxicam, fluorometholone acetate, and dexamethasone, respectively. For fluorometholone acetate and dexamethasone, K-i values from Lineweaver-Burk plots were obtained as 1.044 and 21.2m (noncompetitive) for hCA-I and 9.98 and 8.66m (non-competitive) for hCA-II. In conclusion, tenoxicam, fluorometholone acetate, and dexamethasone showed potent inhibitory effects on esterase activity of hCA-I and hCA-II isozymes under invitro conditions.
  • Küçük Resim
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    The synthesis of novel pyrazole-3,4-dicarboxamidesbearing 5-amino-1,3,4-thiadiazole-2-sulfonamide moiety with effective inhibitory activity against the isoforms of human cytosolic carbonic anhydrase I and II
    (Academic Press Inc Elsevier Science, 2016) Mert, Samet; Alim, Zuhal; Isgor, Mehmet Mustafa; Beydemir, Sukru; Kasimogullari, Rahmi
    A series of 1-(3-substituted-phenyl)-5-phenyl-N-3,N-4-bis(5-sulfamoyl-1,3,4-thiadiazol-2-yl)-1H-pyrazole-3,4- dicarboxamides (4-15) were synthesized. The structures of these pyrazole-sulfonamides were confirmed by FT-IR, H-1 NMR, C-13 NMR and elemental analysis methods. Human cytosolic carbonic anhydrase (CA, EC 4.2.1.1) isozymes (hCA I and II) were purified from erythrocyte cells by affinity chromatography. The inhibitory effects of newly synthesized derivatives (4-15) were investigated in vitro on esterase activities of these isozymes. The K-i values were determined as 0.119-3.999 mu M for hCA I and 0.084-0.878 mu Mfor hCA II. The results showed that the compound 6 for hCA I and the compound 11 for hCA II had the highest inhibitory effect. Beside that, the compound 8 had the lowest inhibition effect on both isozymes. (C) 2016 Elsevier Inc. All rights reserved.