Postius S, Schneider F
Z Naturforsch C Biosci. 1977 Nov-Dec;32(11-12):944-8. doi: 10.1515/znc-1977-11-1211.
The inhibition of the proliferation of hyperdiploid Ehrlich ascites tumor cells in suspension cultures by amobarbital is coupled to an increased glycolytic activity as shown by lactic acid production and glucose consumption; higher concentrations of amobarbital than 1 mM enhance the ATP/ADP ratio of the total cell. The actual activity of pyruvate dehydrogenase of intact cells is completely inhibited in the presence of 2 mM amobarbital as was shown by the 14CO2 evolution from [114C]pyruvate or the incorporation of 14CO2 into the total lipid fraction of the cells from [U-14C]lactate. The pyruvate dehydrogenase complex from Ehrlich ascites tumor cells is completely inhibited by 1 mM amobarbital in vitro. The activity of alpha-oxoglutarate dehydrogenase is inhibited by amobarbital, too, as well as shown by measuring the 14CO2 evolution from [1-14C]glutamate with intact cells. It is suggested that the inhibition of pyruvate dehydrogenase in the presence of amobarbital is the result of a direct action on the enzyme as well as the consequence of a change in the cellular redox state or its energy charge.
异戊巴比妥对悬浮培养的超二倍体艾氏腹水肿瘤细胞增殖的抑制作用与糖酵解活性增加相关，这可通过乳酸生成和葡萄糖消耗表现出来；异戊巴比妥浓度高于1 mM时会提高细胞总体的ATP/ADP比值。如通过[1-¹⁴C]丙酮酸释放¹⁴CO₂或[U-¹⁴C]乳酸中¹⁴CO₂掺入细胞总脂质部分所显示，在2 mM异戊巴比妥存在的情况下，完整细胞的丙酮酸脱氢酶实际活性被完全抑制。在体外，1 mM异戊巴比妥可完全抑制艾氏腹水肿瘤细胞的丙酮酸脱氢酶复合体。α-酮戊二酸脱氢酶的活性也受到异戊巴比妥的抑制，这同样通过用完整细胞测量[1-¹⁴C]谷氨酸释放¹⁴CO₂得以显示。有人提出，在异戊巴比妥存在的情况下，丙酮酸脱氢酶的抑制是对该酶直接作用的结果，也是细胞氧化还原状态或其能量电荷变化的结果。
