<i>In vitro</i> and <i>in vivo</i> effects of dantrolene on carbonic anhydrase enzyme activities

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GÜLÇİN İ., Beydemir Ş., Büyükokuroglu M.

BIOLOGICAL & PHARMACEUTICAL BULLETIN, cilt.27, sa.5, ss.613-616, 2004 (SCI-Expanded) identifier identifier identifier

  • Yayın Türü: Makale / Tam Makale
  • Cilt numarası: 27 Sayı: 5
  • Basım Tarihi: 2004
  • Doi Numarası: 10.1248/bpb.27.613
  • Dergi Adı: BIOLOGICAL & PHARMACEUTICAL BULLETIN
  • Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Sayfa Sayıları: ss.613-616
  • Anadolu Üniversitesi Adresli: Hayır

Özet

The effects of dantrolene were investigated on carbonic anhydrase (CA) enzyme activities in in vitro human and in in vivo Sprague-Dawley rat erythrocytes. For in vitro study, human carbonic anhydrase-I (HCA-I) and -II (HCA-II) were purified by Sepharose 4B-(L)-tyrosine-sulfanylamide affinity chromatography, rats were used for in vivo study. In vivo and in vitro CA enzyme activity was determined colorimetrically using the CO2-hydration method of Wilbur and Anderson. Dantrolene (1.64x10(-5)-6.56x10(-5) M) showed in vitro inhibitory effects on HCA-I and HCA-II hydratase activity, when determined using the CO2-hydratase method. 50% inhibitory concentration (IC50) was 4.09x10(-5) M for HCA(-1) and 3.24x10(-5) M for HCA-II. Rat erythrocyte CA activity was significantly inhibited by 10 mg/kg dantrolene for up to 3 h (p<0.001) following intraperitoneal administration. In conclusion, Dantrolene inhibited the carbonic anhydrase enzyme activity under in vitro and in vivo conditions.