Deryanur ERDEM, Emrah YERLİKAYA, Saltuk Buğrahan CEYHUN, Ramazan DEMİRDAĞ, Murat ŞENTÜRK, Orhan ERDOĞAN, Ömer İrfan KÜFREVİOĞLU

Levrek Dicentrachus labrax Alfa-Karbonik Anhidraz üzerine Bazı Sülfonamidlerin İnhibisyon Etkisi

Alfa-karbonik anhidraz EC: 4.2.1.1; CA levrek solungaç ve karaciğerden saflaştırıldı. Saflaştırma prosedürü homojenat hazırlama ve Sepharose 4B-tirozin-sülfanilamid afinite kramatografisinden oluştu. Bazı sülfonamidlerin enzim aktivitesi üzerine in vitro inhibisyon etkisi incelendi. Bu maddeler için Ki sabitleri ve IC50 değerleri Lineweaver-Burk grafikleri ve % aktivite-[I] grafikleri kullanılarak belirlendi. Sülfanilamid, mafenid, asetazolamid, 2-amino-1,3,5-tiyadiazol-5 sülfonamid için IC değerleri sırası ile solungaç karbonik anhidraz GCA için 980, 142, 20 ve 34 μM, karaciğer karbonik anhidraz LCA için 126, 23, 14 ve 2.58 μM, olarak belirlendi. Bazı sülfonamidlerin diğer CA izoenzimleri ile Ki sabitleri karşılaştırıldığında düşük mikromolar derişimlerde 0.21’den 76.0 μM’a kadar GCA ve LCA’ya karşı çok güçlü inhibitör aktiviteleri olduğu belirlendi

Anahtar Kelimeler:

Karbonik anhidraz CA, European seabass, karaciğer karbonik anhidraz LCA, solungaç karbonik anhidraz GCA, inhibitör, sülfonamid

Inhibition Effects of Some Sulfonamides on α-Carbonic Anhydrase from European seabass Dicentrachus labrax

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 μM, 142 μM, 20 μM and 34 μM for gill carbonic anhydrase GCA , 126 μM, 23 μM, 14 μM and 2.58 μM 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 μM as compared with other CAs.

Keywords:

Carbonic anhydrase CA, European seabass, liver carbonic anhydrase LCA, Gill carbonic anhydrase GCA, Inhibition, sulfonamide,

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