The in vitro and in vivo inhibitory effects of some sulfonamide derivatives on rainbow trout (Oncorhynchus mykiss) erythrocyte carbonic anhydrase activity

BULBUL M., HISAR O., BEYDEMIR S., CIFTCI M., Kufrevioglu I.

JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY, cilt.18, sa.4, ss.371-375, 2003 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 18 Sayı: 4
  • Basım Tarihi: 2003
  • Doi Numarası: 10.1080/1475636031000138769
  • Dergi Adı: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.371-375
  • Anahtar Kelimeler: sulfonamides, carbonic anhydrase, rainbow trout, erythrocyte, PRESSURE LOWERING PROPERTIES, ENZYME-ACTIVITIES, PHARMACOKINETICS, SULFADIMETHOXINE
  • Atatürk Üniversitesi Adresli: Evet

Özet

The in vitro and in vivo inhibitory effects of 5-(3alpha, 12alpha-dihydroxy-5-beta-cholanamido)-1,3,4-thiadiazole-2-sulfonamide ( 1 ), 5-(3alpha, 7alpha, 12alpha-trihydroxy-5-beta-cholanamido)-1,3,4-thiadiazole-2-sulfonamide ( 2 ), 5-(3alpha, 7alpha, 12alpha-triacetoxy-5-beta-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 CO 2 -Hydratase method in vitro and in vivo studies. From in vitro studies, it was found that all the compounds inhibited CA. The obtained I 50 value for the sulfonamides ( 1 ), ( 2 ) and ( 3 ) and acetazolamide were 0.83, 0.049, 0.82 and 0.052 muM, respectively. From in vivo studies, it was observed that CA was inhibited by the sulfonamides ( 1 ), ( 2 ) and ( 3 ) and acetazolamide.