某些药物对人红细胞葡萄糖-6-磷酸脱氢酶的影响：体外研究。

Effects of some drugs on human erythrocyte glucose 6-phosphate dehydrogenase: an in vitro study.

机构信息

Ataturk University, Science Faculty, Department of Chemistry, Erzurum, Turkey.

出版信息

J Enzyme Inhib Med Chem. 2010 Dec;25(6):871-5. doi: 10.3109/14756360903489581.

Abstract

Inhibitory effects of some drugs on glucose 6-phosphate dehydrogenase from the erythrocytes of human have been investigated. For this purpose, at the beginning, erythrocyte glucose 6-phosphate dehydrogenase was purified 2256 times in a yield of 44.22% by using ammonium sulphate precipitation and 2', 5'-ADP Sepharose 4B affinity gel. Temperature of +4°C was maintained during the purification process. Enzyme activity was determined with the Beutler method by using a spectrophotometer at 340 nm. This method was utilized for all kinetic studies. Ketotifen, dacarbazine, thiocolchicoside, meloxicam, methotrexate, furosemide, olanzapine, methylprednizolone acetate, paricalcitol, ritodrine hydrochloride, and gadobenate-dimeglumine were used as drugs. All the drugs indicated the inhibitory effects on the enzyme. Ki constants for glucose 6-phosphate dehydrogenase were found by means of Lineweaver-Burk graphs. While methylprednizolone acetate showed competitive inhibition, the others displayed non-competitive inhibition. In addition, IC(50) values of the drugs were determined by plotting Activity% vs [I].

摘要

研究了一些药物对人红细胞葡萄糖-6-磷酸脱氢酶的抑制作用。为此，首先通过硫酸铵沉淀和 2'，5'-ADP Sepharose 4B 亲和凝胶，在+4°C 的温度下，将红细胞葡萄糖-6-磷酸脱氢酶纯化 2256 倍，产率为 44.22%。酶活性通过分光光度计在 340nm 处使用 Beutler 法测定。该方法用于所有动力学研究。酮替芬、达卡巴嗪、硫代秋水仙碱、美洛昔康、甲氨蝶呤、呋塞米、奥氮平、醋酸甲基泼尼松龙、帕立骨化醇、盐酸利托君和钆贝葡胺被用作药物。所有药物均显示对该酶的抑制作用。通过 Lineweaver-Burk 图确定葡萄糖-6-磷酸脱氢酶的 Ki 常数。醋酸甲基泼尼松龙显示竞争性抑制，而其他药物则显示非竞争性抑制。此外，通过绘制 Activity% vs [I]图确定了药物的 IC50 值。