Häussinger D
Biol Chem Hoppe Seyler. 1986 Aug;367(8):741-50. doi: 10.1515/bchm3.1986.367.2.741.
With physiological portal HCO3- and CO2 concentrations of 25mM and 1.2mM in the perfusate, respectively, acetazolamide inhibited urea synthesis from NH4Cl in isolated perfused rat liver by 50-60%, whereas urea synthesis from glutamine was inhibited by only 10-15%. A decreased sensitivity of urea synthesis from glutamine to acetazolamide inhibition was also observed when the extracellular HCO3- and CO2 concentrations were varied from 0-50mM and 0-2.4mM, respectively. Stimulation of intramitochondrial CO2 formation at pyruvate dehydrogenase with high pyruvate concentrations (7mM) was without effect on the acetazolamide sensitivity of urea synthesis from NH4Cl. Urea synthesis was studied under conditions of a limiting HCO3- supply for carbamoyl-phosphate synthesis. In the absence of externally added HCO3- or CO2, when 14CO2 was provided intracellularly by [U-14C]glutamine or [1-14C]-glutamine oxidation, acetazolamide had almost no effect on label incorporation into urea, whereas label incorporation from an added tracer H14CO3- dose was inhibited by about 70%. 14CO2 production from [U-14C]glutamine was about twice as high as from [1-14C]glutamine, indicating that about 50% of the CO2 produced from glutamine is formed at 2-oxoglutarate dehydrogenase. The fractional incorporation of 14CO2 into urea was about 13% with [1-14C]-as well as with [U-14C]glutamine. Addition of small concentrations of HCO3- (1.2mM) to the perfusate increased urea synthesis from glutamine by about 70%. This stimulation of urea synthesis was fully abolished by acetazolamide. The carbonate-dehydratase inhibitor prevented the incorporation of added HCO3- into urea, whereas incorporation of CO2 derived from glutamine degradation was unaffected. Without HCO3- and CO2 in the perfusion medium, when 14CO2 was provided by [1-14C]-pyruvate oxidation, acetazolamide inhibited urea synthesis from NH4Cl as well as 14C incorporation into urea by about 50%. Therefore carbonate-dehydratase activity is required for the utilization of extracellular CO2 or pyruvate-dehydrogenase-derived CO2 for urea synthesis, but not for CO2 derived from glutamine oxidation. This is further evidence for a special role of glutamine as substrate for urea synthesis.
在灌注液中,生理门静脉HCO₃⁻和CO₂浓度分别为25mM和1.2mM时,乙酰唑胺使离体灌注大鼠肝脏中由氯化铵合成尿素的过程受到50 - 60%的抑制,而由谷氨酰胺合成尿素的过程仅受到10 - 15%的抑制。当细胞外HCO₃⁻和CO₂浓度分别在0 - 50mM和0 - 2.4mM范围内变化时,也观察到由谷氨酰胺合成尿素对乙酰唑胺抑制的敏感性降低。用高浓度丙酮酸(7mM)刺激丙酮酸脱氢酶处的线粒体内CO₂生成,对由氯化铵合成尿素的乙酰唑胺敏感性没有影响。在氨基甲酰磷酸合成的HCO₃⁻供应受限的条件下研究了尿素合成。在没有外源添加HCO₃⁻或CO₂时,当通过[U - ¹⁴C]谷氨酰胺或[1 - ¹⁴C] - 谷氨酰胺氧化在细胞内提供¹⁴CO₂时,乙酰唑胺对¹⁴C掺入尿素几乎没有影响,而从添加的示踪剂H¹⁴CO₃⁻剂量的¹⁴C掺入受到约70%的抑制。由[U - ¹⁴C]谷氨酰胺产生的¹⁴CO₂约为[1 - ¹⁴C]谷氨酰胺产生的¹⁴CO₂的两倍,表明由谷氨酰胺产生的CO₂中约50%是在2 - 氧代戊二酸脱氢酶处形成的。用[1 - ¹⁴C] - 和[U - ¹⁴C]谷氨酰胺时,¹⁴CO₂掺入尿素的分数约为13%。向灌注液中添加低浓度的HCO₃⁻(1.2mM)使由谷氨酰胺合成尿素增加约70%。这种尿素合成的刺激被乙酰唑胺完全消除。碳酸酐酶抑制剂阻止添加的HCO₃⁻掺入尿素,而谷氨酰胺降解产生的CO₂掺入不受影响。在灌注介质中没有HCO₃⁻和CO₂时,当由[1 - ¹⁴C] - 丙酮酸氧化提供¹⁴CO₂时,乙酰唑胺抑制由氯化铵合成尿素以及¹⁴C掺入尿素约50%。因此碳酸酐酶活性是利用细胞外CO₂或丙酮酸脱氢酶衍生的CO₂进行尿素合成所必需的,但不是谷氨酰胺氧化产生的CO₂进行尿素合成所必需的。这进一步证明了谷氨酰胺作为尿素合成底物的特殊作用。