D-葡糖二酸衍生物对大鼠肝脏溶酶体和红细胞稳定性的影响。

Effect of D-glucaric acid derivatives on stability of rat liver lysosomes and erythrocytes.

作者信息

Furuno K, Matsushita H, Nagashima R, Nakano H, Suzuki S

出版信息

Jpn J Pharmacol. 1974 Dec;24(6):843-52. doi: 10.1254/jjp.24.843.

DOI:10.1254/jjp.24.843

Abstract

For studies on the lysosome-stabilizing effect of D-glucaric acid derivatives which have been found to have anti-inflammatory effect, the available and soluble enzyme activities of acid phosphatase of rat liver lysosomes were determined. Saliployed as standards. Lysosomes were incubated with drugs under specific conditions which allowed the data on the stabilizing activity of the drugs to be reproducible. The inhibitory effect of D-glucaro-1, 4-lactone, salicylic acid and phenylbutazone onover a wide range of concentrations. D-glucaro-1, 4-lactone as well as salicylic acid exhibited concentration-dependent lysosome-stabilizing effect whereas phenlybutazone had an optimum concentration for its lysosome-stabilizing effect. In addition, D-glucaro-1, 4-lactone,saliclicacid and phenylubtazone were also examined for their effects on heat-induced and saponin-induced hemolysis of rat erythrocyres. Both salicylic acid and phenylbutazone exhibited potent stabilziing and labilizing effects on heat-induced and saponin-induced hemolysis of eryhthrocytes, respectively. D-glucaro-1, 4-lactone, however, was incabale of affecting the hemolysis of erythrocytes. There appears to be a difference in the mechanism of the lysosome-stabilizing effects between D-glucaric acid derivatives and other anti-inflammatory drugs.

摘要

对于已发现具有抗炎作用的D - 葡糖二酸衍生物的溶酶体稳定作用的研究，测定了大鼠肝脏溶酶体酸性磷酸酶的可利用和可溶性酶活性。以水杨酸作为标准。溶酶体在特定条件下与药物孵育，以使药物稳定活性的数据具有可重复性。D - 葡糖-1,4-内酯、水杨酸和保泰松在很宽的浓度范围内都有抑制作用。D - 葡糖-1,4-内酯以及水杨酸表现出浓度依赖性的溶酶体稳定作用，而保泰松的溶酶体稳定作用有一个最佳浓度。此外，还研究了D - 葡糖-1,4-内酯、水杨酸和保泰松对大鼠红细胞热诱导溶血和皂苷诱导溶血的影响。水杨酸和保泰松分别对红细胞热诱导溶血和皂苷诱导溶血表现出有效的稳定和不稳定作用。然而，D - 葡糖-1,4-内酯不能影响红细胞的溶血。D - 葡糖二酸衍生物与其他抗炎药物在溶酶体稳定作用的机制上似乎存在差异。