Inhibition Effects of Some Sulfonamides on Carbonic Anhydrase from European seabass (Dicentrachus labrax)
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Tarih
2011
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Erişim Hakkı
info:eu-repo/semantics/openAccess
Özet
Alpha-carbonic anhydrase (EC: 4.2.1.1; CA) was purified from European seabass gill and liver. The purification procedure was composed of preparation of homogenate (or hemolysate) and affinity chromatography on Sepharose 4B-tyrosine-sulfanilamide. Some sulfonamides exhibited in vitro inhibitory effects on the enzyme activity. Ki constants and IC50 values for these drugs were determined by Lineweaver-Burk graphs and plotting activity % vs. [I], respectively. IC50 values of sulfanilamide, mafenide, acetazolamide, 2-amino-1,3,5-tiyadiazol-5 sulfonamide were 980 ??M, 142 ??M, 20 ??M and 34 ??M for gill carbonic anhydrase (GCA), 126 ??M, 23 ??M, 14 ??M and 2.58 ??M for liver carbonic anhydrase (LCA), respectively. Some sulfonamides exhibited much stronger inhibitory activity against GCA and LCA at low micromolar concentrations with the Ki values ranging from 0.21 to 76.0 ??M as compared with other CAs.
Açıklama
Anahtar Kelimeler
Carbonic anhydrase (CA), European seabass, liver carbonic anhydrase (LCA), Gill carbonic anhydrase (GCA), inhibition, sulfonamide.
