Coude F X, Sweetman L, Nyhan W L
J Clin Invest. 1979 Dec;64(6):1544-51. doi: 10.1172/JCI109614.
In the search for the mechanism by which hyperammonemia complicates propionic and methylmalonic acidemia the effects of a series of acyl-coenzyme A (CoA) derivatives were studied on the activity of N-acetylglutamate synthetase in rat liver mitochondria using acetyl-CoA as substrate. Propionyl-CoA was found to be a competitive inhibitor. The inhibition constant of 0.71 mM is in the range of concentrations of propionate found in the serum of patients with propionic and methylmalonic acidemia. Propionyl-CoA was also found to be a substrate for N-acetylglutamate synthetase, forming N-propionylglutamate. This compound was a weak activator of rat liver carbamoylphosphate synthetase; the activation constant was 1.1 mM as compared with 0.12 mM for N-acetylglutamate. A decreased level of N-acetylglutamate in liver mitochondria that would follow inhibition of N-acetylglutamate synthetase by propionyl-CoA would be expected to lead to hyperammonemia. Methylmalonyl-CoA, tiglyl-CoA, and isovaleryl-CoA at a concentration of 3 mM caused 30-70% inhibition of N-acetylglutamate synthetase. 3the latter two compounds are readily detoxified by the formation of N-acylglycine conjugates in liver, which may prevent large accumulations and could explain why hyperammonemia is not characteristic of patients with beta-ketothiolase deficiency or isovaleric acidemia in whom these compounds would be expected to be elevated.
在探寻高氨血症使丙酸血症和甲基丙二酸血症病情复杂化的机制过程中,以乙酰辅酶A为底物,研究了一系列酰基辅酶A(CoA)衍生物对大鼠肝线粒体中N - 乙酰谷氨酸合成酶活性的影响。发现丙酰辅酶A是一种竞争性抑制剂。其抑制常数为0.71 mM,处于丙酸血症和甲基丙二酸血症患者血清中丙酸浓度范围内。还发现丙酰辅酶A是N - 乙酰谷氨酸合成酶的底物,可形成N - 丙酰谷氨酸。该化合物是大鼠肝细胞质中氨甲酰磷酸合成酶的弱激活剂;其激活常数为1.1 mM,而N - 乙酰谷氨酸的激活常数为0.12 mM。丙酰辅酶A抑制N - 乙酰谷氨酸合成酶后,预计肝线粒体中N - 乙酰谷氨酸水平降低会导致高氨血症。浓度为3 mM的甲基丙二酰辅酶A、巴豆酰辅酶A和异戊酰辅酶A对N - 乙酰谷氨酸合成酶有30 - 70%的抑制作用。后两种化合物在肝脏中可通过形成N - 酰基甘氨酸共轭物而易于解毒,这可能会防止大量蓄积,并且可以解释为什么高氨血症不是β - 酮硫解酶缺乏症或异戊酸血症患者的特征,而在这些患者中预计这些化合物会升高。