Premium
Some Anti‐Inflammatory Agents Inhibit Esterase Activities of Human Carbonic Anhydrase Isoforms I and II : An In Vitro Study
Author(s) -
Alım Zuhal,
Kılınç Namık,
İşgör Mehmet M.,
Şengül Bülent,
Beydemir Şükrü
Publication year - 2015
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.12561
Subject(s) - tenoxicam , chemistry , carbonic anhydrase , esterase , carbonic anhydrase i , enzyme , in vitro , biochemistry , pharmacology , carbonic anhydrase ii , isozyme , medicine , piroxicam , alternative medicine , pathology
Carbonic anhydrases ( CA s) 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. IC 50 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, K i 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.