The In Vitro and In Vivo Inhibitory Effects of Some Sulfonamide Derivatives on Rainbow Trout (Oncorhynchus Mykiss) Erythrocyte Carbonic Anhydrase Activity

Author： BÜLBÜL Metin HİSAR Olcay BEYDEMİR Şükrü ÇİFTÇİ Mehmet KÜFREVIOĞLU Ö. İrfan

Publisher： Informa Healthcare

ISSN： 1475-6366

Source： Journal of Enzyme Inhibition and Medicinal Chemistry, Vol.18, Iss.4, 2003-01, pp. : 371-375

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

Previous Menu Next

Abstract

The in vitro and in vivo inhibitory effects of 5-(3, 12-dihydroxy-5-&bgr;-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (1), 5-(3, 7, 12-trihydroxy-5-&bgr;-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (2), 5-(3, 7, 12-triacetoxy-5-&bgr;-cholanamido)-1,3,4-thiadiazole-2-sulfonamide (3) and acetazolamide on rainbow trout (Oncorhynchus Mykiss) (RT) erythrocyte carbonic anhydrase (CA) were investigated. The RT erythrocyte CA was obtained by affinity chromatography with a yield of 20.9%, a specific activity of 422.5 EU/mg protein and a purification of 222.4-fold. The purity of the enzyme was confirmed by SDS-PAGE. Inhibitory effects of the sulfonamides and acetazolamide on the RT erythrocyte CA were determined using the CO₂-Hydratase method in vitro and in vivo studies. From in vitro studies, it was found that all the compounds inhibited CA. The obtained I₅₀ value for the sulfonamides (1), (2) and (3) and acetazolamide were 0.83, 0.049, 0.82 and 0.052 μM, respectively. From in vivo studies, it was observed that CA was inhibited by the sulfonamides (1), (2) and (3) and acetazolamide.