Tamura M, Inagami T, Kinoshita T, Kuwano H
J Hypertens. 1987 Apr;5(2):219-25. doi: 10.1097/00004872-198704000-00014.
An Na+,K+-ATPase inhibitor possessing inhibitory activity against the specific binding of ouabain to Na+,K+-ATPase has been purified from the plasma of acutely saline-infused hogs. The purification was performed by a combination of Amberlite XAD-2 adsorption chromatography and five steps of high-pressure liquid chromatography (HPLC). Fast atom bombardment mass and proton nuclear magnetic resonance (NMR) spectrometric studies identified the purified substance as lysophosphatidylcholine gamma-stearoyl (LPCS). The ouabain-displacing activity in plasma, due to this compound, increased with time during saline infusion. The maximal level reached was approximately 12 times higher than that in the pre-infusion plasma sample. Lysophosphatidylcholines (LPCs) containing myristoyl, palmitoyl and oleoyl groups were also inhibitory to Na+,K+-ATPase and ouabain-binding to the enzyme. These LPCs were effective at 100 mumol/l concentrations in attaining 50% inhibition of the enzyme activity and ouabain-binding activity of Na+,K+-ATPase. These results suggest that LPCs containing long chain fatty acids could play an important role as a Na+,K+-ATPase inhibitors under volume-expanded conditions.
一种对哇巴因与钠钾ATP酶特异性结合具有抑制活性的钠钾ATP酶抑制剂已从急性输注生理盐水的猪血浆中纯化出来。纯化过程通过Amberlite XAD - 2吸附色谱法与五步高压液相色谱法（HPLC）相结合进行。快原子轰击质谱和质子核磁共振（NMR）光谱研究确定纯化后的物质为溶血磷脂酰胆碱γ - 硬脂酰（LPCS）。由于这种化合物，血浆中的哇巴因置换活性在输注生理盐水期间随时间增加。达到的最高水平比输注前血浆样本中的水平高约12倍。含有肉豆蔻酰、棕榈酰和油酰基团的溶血磷脂酰胆碱（LPCs）对钠钾ATP酶以及哇巴因与该酶的结合也有抑制作用。这些LPCs在浓度为100μmol / l时能有效抑制钠钾ATP酶活性和哇巴因结合活性达50%。这些结果表明，含有长链脂肪酸的LPCs在容量扩张条件下可能作为钠钾ATP酶抑制剂发挥重要作用。
