title: In vitro and in vivo effects of dantrolene on carbonic anhydrase enzyme activities.
abstract: 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 CO(2)-hydration method of Wilbur and Anderson. Dantrolene (1.64 x 10(-5)-6.56 x 10(-5) M) showed in vitro inhibitory effects on HCA-I and HCA-II hydratase activity, when determined using the CO(2)-hydratase method. 50% inhibitory concentration (IC(50)) was 4.09 x 10(-5) M for HCA-I and 3.24 x 10(-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.
authors.affiliation: Atatürk University, Science and Arts Faculty, Department of Chemistry, Turkey. igulcin@atauni.edu.tr
authors.forename: Ilhami
authors.initials: I
authors.lastname: Gülçin
authors.forename: Sükrü
authors.initials: S
authors.lastname: Beydemir
authors.forename: Mehmet Emin
authors.initials: ME
authors.lastname: Büyükokuroğlu
mesh_terms: D000818:Animals; D002256:Carbonic Anhydrases / Q000378:metabolism*; D003620:Dantrolene / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D004789:Enzyme Activation / Q000187:drug effects / Q000502:physiology; D004791:Enzyme Inhibitors / Q000494:pharmacology; D004912:Erythrocytes / Q000187:drug effects / Q000201:enzymology; D006801:Humans; D051381:Rats; D017207:Rats, Sprague-Dawley
chemical_list: D004791:Enzyme Inhibitors; D002256:Carbonic Anhydrases; D003620:Dantrolene