Cederbaum A I
Alcohol Clin Exp Res. 1981 Jan;5(1):38-44. doi: 10.1111/j.1530-0277.1981.tb04862.x.
Compared to other substrates, the oxidation of pyruvate by isolated mitochondria is especially sensitive to inhibition by acetaldehyde. It is not known whether this inhibition represents a direct effect of acetaldehyde or requires the metabolism of acetaldehyde. Experiments were therefore carried out in the presence of cyanamide, an inhibitor of aldehyde dehydrogenase. After a brief incubation period, cyanamide inhibited the state 4 and state 3 rate of acetaldehyde (0.1-1.0 mM) oxidation by isolated rat liver mitochondria. Little inhibition was found in the absence of the incubation period. Maximum inhibition was found at cyanamide concentrations of 0.01 to 0.033 mM. Cyanamide also inhibited the activity of aldehyde dehydrogenase assayed in disrupted mitochondrial fractions. The inhibition by cyanamide was specific since cyanamide did not affect mitochondrial oxidation of succinate, glutamate, or pyruvate. Acetaldehyde inhibited the state 3 rate of pyruvate oxidation by liver mitochondria. Despite preventing acetaldehyde oxidation, cyanamide did not prevent the inhibition of pyruvate oxidation by acetaldehyde. These results indicate that (a) cyanamide can be used as an effective in vitro inhibitor of acetaldehyde oxidation and (b) the unique sensitivity of pyruvate oxidation to acetaldehyde represents a direct effect of acetaldehyde on pyruvate dehydrogenase.
与其他底物相比,分离出的线粒体对丙酮酸的氧化作用对乙醛抑制尤为敏感。尚不清楚这种抑制是乙醛的直接作用还是需要乙醛的代谢。因此,在存在氨基氰(一种乙醛脱氢酶抑制剂)的情况下进行了实验。经过短暂的温育期后,氨基氰抑制了分离出的大鼠肝线粒体对乙醛(0.1 - 1.0 mM)氧化的状态4和状态3速率。在没有温育期的情况下几乎没有发现抑制作用。在氨基氰浓度为0.01至0.033 mM时发现最大抑制作用。氨基氰还抑制了在破碎的线粒体组分中测定的乙醛脱氢酶活性。氨基氰的抑制作用具有特异性,因为氨基氰不影响琥珀酸、谷氨酸或丙酮酸的线粒体氧化。乙醛抑制肝线粒体对丙酮酸的状态3氧化速率。尽管阻止了乙醛氧化,但氨基氰并未阻止乙醛对丙酮酸氧化的抑制作用。这些结果表明:(a)氨基氰可作为体外乙醛氧化的有效抑制剂;(b)丙酮酸氧化对乙醛的独特敏感性代表了乙醛对丙酮酸脱氢酶的直接作用。