Glucose 6-phosphate dehydrogenase: in vitro and in vivo effects of dantrolene sodium.
In our study, effects of dantrolene sodium on glucose 6-phosphate dehydrogenase (G6PD) were examined in the human erythrocytes in vitro and in rat erythrocytes in vivo. Human erythrocyte G6PD was purified using ammonium sulfate fractionation and 2',5'-ADP Sepharose 4B affinity chromatography. The enzyme activity was determined by Beutler's method. The overall purification procedures gave the human G6PD having the specific activity of 97.6 EU/mg of protein, which was purified 9760-fold with a yield of 39%. Dantrolene sodium inhibited the enzyme activity under in vitro conditions and the I(50) value (drug concentration which produces 50% inhibition) of this drug was 0.91 mM. In vivo studies were performed in rats (Sprague-Dawley). Dantrolene sodium at 10 mg/kg inhibited the enzyme activity significantly (p < 0.05) 3 h after dosing. We conclude that dantrolene sodium showed inhibitory effect on G6PD activity both in vitro and in vivo.
Beydemir
Sükrü
S
Atatürk University, Arts and Science Faculty, Department of Chemistry, 25240-Erzurum, Turkey. beydemir@atauni.edu.tr
Gülçin
Ilhami
I
Küfrevioğlu
O Irfan
OI
Ciftçi
Mehmet
M
D000818:Animals; D003620:Dantrolene / Q000008:administration & dosage / Q000009:adverse effects* / Q000493:pharmacokinetics; D004591:Electrophoresis, Polyacrylamide Gel; D004912:Erythrocytes / Q000737:chemistry / Q000187:drug effects / Q000201:enzymology; D005954:Glucosephosphate Dehydrogenase / Q000037:antagonists & inhibitors* / Q000097:blood* / Q000302:isolation & purification; D006801:Humans; D066298:In Vitro Techniques; D051381:Rats; D017207:Rats, Sprague-Dawley
D005954:Glucosephosphate Dehydrogenase; D003620:Dantrolene