Nishiura A, Murakami T, Higashi Y, Yata N
Department of Parmaceutics and Therapeutics, Hiroshima University School of Medicine, Japan.
Pharm Res. 1988 Apr;5(4):209-13. doi: 10.1023/a:1015985511653.
The role of phosphatidylserine in the cellular and subcellular lung distribution of quinidine was investigated in rats, since quinidine was found to bind preferentially to phosphatidylserine. The concentration of phosphatidylserine in the cellular and subcellular fractions was determined after separation by two-dimensional thin-layer chromatography. Selective accumulation of quinidine in vivo was observed in the alveolar macrophage at the cellular level and in the plasma membrane at the subcellular level. Both alveolar macrophages and plasma membranes were rich in phosphatidylserine compared to other fractions. When plasma levels were kept at steady state by i.v. infusion, the distribution of quinidine in the lung cellular and subcellular fractions was linearly correlated with the concentration of phosphatidylserine (r = 0.906). These results suggest that the concentration of phosphatidylserine is a dominant determinant of the cellular and subcellular lung distribution of quinidine.
由于发现奎尼丁优先与磷脂酰丝氨酸结合，因此在大鼠中研究了磷脂酰丝氨酸在奎尼丁细胞和亚细胞肺分布中的作用。通过二维薄层色谱分离后，测定细胞和亚细胞组分中磷脂酰丝氨酸的浓度。在细胞水平上，观察到肺泡巨噬细胞中奎尼丁在体内的选择性积累；在亚细胞水平上，观察到质膜中奎尼丁的选择性积累。与其他组分相比，肺泡巨噬细胞和质膜都富含磷脂酰丝氨酸。通过静脉输注使血浆水平保持稳定状态时，奎尼丁在肺细胞和亚细胞组分中的分布与磷脂酰丝氨酸浓度呈线性相关（r = 0.906）。这些结果表明，磷脂酰丝氨酸浓度是奎尼丁在细胞和亚细胞肺分布中的主要决定因素。
