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Journals / Hacettepe Journal of Biology and Chemistry / 2011 / Cilt: 39 - Sayı: 2

Levrek (Dicentrarchus labrax) alfa-karbonik anhidraz üzerine bazı sülfonamidlerin inhibisyon etkisi

Inhibition effects of some sulfonamides on α-carbonic anhydrase from european seabass (Dicentrarchus labrax)

Ömer İrfan KÜFREVİOĞLU
Orhan ERDOĞAN
Saltuk Buğrahan CEYHUN
Ramazan DEMİRDAĞ
Deryanur ERDEM
Murat ŞENTÜRK
Emrah YERLİKAYA
Pages
139–144
Publication Date
2022-10-17
DOI
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AI Summary & Key Takeaways

AI Insight
⚡ TL;DR(Too Long; Didn't Read)

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.

📌 3 Key Takeaways

🎯
Objective & Hypothesis:Alpha-carbonic anhydrase (EC: 4.2.1.1; CA) was purified from European seabass gill and liver.
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Key Findings & Data:The purification procedure was composed of preparation of homogenate (or hemolysate) and affinity chromatography on Sepharose 4B-tyrosine-sulfanilamide.
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Conclusion & Impact: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.
🔬Design:Research Article
📍Scope:Comprehensive Sample
⚙️Variables:Domain Parameters

Abstract

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.

Özet

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 IC50 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.

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Cite This Article

KÜFREVİOĞLU, Ö. İ., ERDOĞAN, O., CEYHUN, S. B., DEMİRDAĞ, R., ERDEM, D., ŞENTÜRK, M., YERLİKAYA, E. (2022). Levrek (Dicentrarchus labrax) alfa-karbonik anhidraz üzerine bazı sülfonamidlerin inhibisyon etkisi. Hacettepe Journal of Biology and Chemistry, Cilt: 39 - Sayı: 2, 139–144. https://ajindex.com/articles/529231

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