| Title: |
Some Anti-Inflammatory Agents Inhibit Esterase Activities of Human Carbonic Anhydrase Isoforms I and II: An In Vitro Study. |
| Authors: |
Alım, Zuhal, Kılınç, Namık, İşgör, Mehmet M., Şengül, Bülent, Beydemir, Şükrü |
| Source: |
Chemical Biology & Drug Design; Oct2015, Vol. 86 Issue 4, p857-863, 7p |
| Subject Terms: |
ANTI-inflammatory agents, CARBONIC anhydrase, PROTEIN-drug interactions, DEXAMETHASONE, ERYTHROCYTES |
| 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 μ m 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 μ m (noncompetitive) for hCA-I and 9.98 and 8.66 μ m (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. [ABSTRACT FROM AUTHOR] |
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| Database: |
Complementary Index |
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