title: Some Anti-Inflammatory Agents Inhibit Esterase Activities of Human Carbonic Anhydrase Isoforms I and II: An In Vitro Study.
abstract: 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 in vitro 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 642.8 EU/mg proteins and 5576.9 EU/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 14 μm using tenoxicam, fluorometholone acetate, and dexamethasone, respectively. For fluorometholone acetate and dexamethasone, Ki values from Lineweaver-Burk plots were obtained as 1.044 and 21.2 μm (noncompetitive) for hCA-I and 9.98 and 8.66 μm (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 in vitro conditions.
authors: Department of Chemistry, Faculty of Sciences, Atatürk University, 25240, Erzurum, Turkey.
authors: Zuhal
authors: Z
authors: Alım
authors: Department of Chemistry, Faculty of Sciences, Atatürk University, 25240, Erzurum, Turkey.
authors: Namık
authors: N
authors: Kılınç
authors: Department of Biochemistry, Faculty of Veterinary Sciences, Mustafa Kemal University, 31000, Hatay, Turkey.
authors: Mehmet M
authors: MM
authors: İşgör
authors: Department of Chemistry, Faculty of Sciences, Atatürk University, 25240, Erzurum, Turkey.
authors: Bülent
authors: B
authors: Şengül
authors: Department of Chemistry, Faculty of Sciences, Atatürk University, 25240, Erzurum, Turkey.
authors: Şükrü
authors: Ş
authors: Beydemir
mesh_terms: D000893:Anti-Inflammatory Agents / Q000494:pharmacology*; D024401:Carbonic Anhydrase I / Q000037:antagonists & inhibitors* / Q000378:metabolism; D024402:Carbonic Anhydrase II / Q000037:antagonists & inhibitors* / Q000378:metabolism; D002257:Carbonic Anhydrase Inhibitors / Q000494:pharmacology*; D002256:Carbonic Anhydrases / Q000378:metabolism; D003907:Dexamethasone / Q000494:pharmacology*; D004950:Esterases / Q000037:antagonists & inhibitors / Q000378:metabolism; D005469:Fluorometholone / Q000494:pharmacology*; D006801:Humans; D010894:Piroxicam / Q000031:analogs & derivatives* / Q000494:pharmacology
chemical_list: D000893:Anti-Inflammatory Agents; D002257:Carbonic Anhydrase Inhibitors; D010894:Piroxicam; D003907:Dexamethasone; D004950:Esterases; D024401:Carbonic Anhydrase I; D024402:Carbonic Anhydrase II; D002256:Carbonic Anhydrases; D005469:Fluorometholone; C032801:tenoxicam
keywords: anti-inflammatory agents; carbonic anhydrase; dexamethasone; inhibition; tenoxicam, fluorometholone acetate