双硫仑对绵羊肝脏醛脱氢酶的影响。
The effect of disulfiram on the aldehyde dehydrogenases of sheep liver.
作者信息
Kitson T M
出版信息
Biochem J. 1975 Nov;151(2):407-12. doi: 10.1042/bj1510407.
Abstract
- The effect of disulfiram on the activity of the cytoplasmic and mitochondrial aldehyde dehydrogenases of sheep liver was studied. 2. Disulfiram causes an immediate inhibition of the enzyme reaction. The effect on the cytoplasmic enzyme is much greater than on the mitochondrial enzyme. 3. In both cases, the initial partial inhibition is followed by a gradual irreversible loss of activity. 4. The pH-rate profile of the inactivation of the mitochondrial enzyme by disulfiram and the pH-dependence of the maximum velocity of the enzyme-catalysed reaction are both consistent with the involvement of a thiol group. 5. Excess of 2-mercaptoethanol or GSH abolishes the effect of disulfiram. However, equimolar amounts of either of these reagents and disulfiram cause an effect greater than does disulfiram alone. It was shown that the mixed disulphide, Et2N-CS-SS-CH2-CH2OH, strongly inhibits aldehyde dehydrogenase. 6. The inhibitory effect of diethyldithiocarbamate in vitro is due mainly to contamination by disulfiram.
摘要
- 研究了双硫仑对绵羊肝脏细胞质和线粒体醛脱氢酶活性的影响。2. 双硫仑可立即抑制酶反应。对细胞质酶的影响远大于对线粒体酶的影响。3. 在两种情况下，最初的部分抑制之后是活性的逐渐不可逆丧失。4. 双硫仑使线粒体酶失活的pH速率曲线以及酶催化反应最大速度的pH依赖性均与巯基的参与一致。5. 过量的2-巯基乙醇或谷胱甘肽可消除双硫仑的作用。然而，这些试剂中的任何一种与双硫仑等摩尔量会产生比单独使用双硫仑更大的作用。结果表明，混合二硫化物Et2N-CS-SS-CH2-CH2OH强烈抑制醛脱氢酶。6. 二乙基二硫代氨基甲酸盐在体外的抑制作用主要归因于双硫仑的污染。
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