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Abstract #20694 Published in IGR 10-1
Purification of carbonic anhydrase from dog erythrocytes and investigation of in vitro inhibition by various compounds
Bayram T; Arslan O; Ugras HI; Cakir U; Ozensoy OJournal of Enzyme Inhibition and Medicinal Chemistry 2007; 22: 739-744
The enzyme carbonic anhydrase (E.C. 4.2.1.1) has a stimulatory effect on glaucoma, an eye disease that has a risk to dogs, which are models for the human eye disease, that is similar to that in humans. In this study, some sulfonamide derivatives, 2-(3-cyclohexene-1-carbamido)-1,3,4-thiadiazole-5-sulfonamide (CCTS), 4-(3-cyclohexene-1-carbamido) methyl-benzenesulfonamide (CCBS), 2-(9-octadecenoylamido)-1,3,4-thiadiazole-5-sulfonamide (ODTS), 2-(4,7,10-trioxa-tetradecanoylamido)-1,3,4-thiadiazole-5-sulfonamide (TDTS), and 2-(8-methoxycoumarine-3-carbamido)-1,3,4-thiadiazole-5- sulfonamide (MCTS), as well as some anionic compounds (perchlorate and chloride) and existing medicines (dorzolamide-HCl, gentamicine sulphate, tropicamide, and procaine-HCl) were assayed for their inhibition of dog carbonic anhydrase (dCA), which was purified from erythrocytes on an affinity gel of L-tyrosine-sulfonamide-Sepharose 4B. ODTS showed the highest potency amongst the synthetic compounds with IC50 value 1.18 x 10-5 M. Amongst the medicines tested, only dorzolamide showed inhibition with IC50 value 5.05 x 0(-4) M. Procaine and tropicamide actually showed an activatory effect, whereas gentamicine sulfate had no significant effect. The inhibitory effects of anionic compounds such as perchlorate and chloride were also investigated; whereas perchlorate showed inhibition, chloride did not.
Dr. O. Ozensoy, Science and Art Faculty, Department of Chemistry, Balikesir University, Balikesir 10100, Turkey
Classification:
3.8 Pharmacology (Part of: 3 Laboratory methods)
11.5 Carbonic anhydrase inhibitors (Part of: 11 Medical treatment)