儿茶酚胺对大鼠脑二肽基氨基肽酶活性的影响。

Effect of catecholamines on the activity of rat brain dipeptidyl aminopeptidase.

作者信息

Imai K, Saito S, Kato T

出版信息

Neurosci Res. 1984 Oct;1(5):353-6. doi: 10.1016/0168-0102(84)90039-7.

Abstract

The inhibitory effect of catecholamines, their metabolic intermediates and derivatives on the activity of rat brain dipeptidyl aminopeptidase was studied. The enzyme was extracted from a crude mitochondrial fraction containing lysosomes (and also synaptosomes) and purified by three-step column chromatography. The activity of the purified enzyme was inhibited by a low concentration (IC50 2 approximately 5 mM) of dopamine, norepinephrine and epinephrine. Dihydroxyphenylalanine or dihydroxyphenylacetic acid, each having a carboxyl group, showed only a weak inhibitory effect (IC50 greater than 10 mM). These results suggest the possibility that brain dipeptidyl aminopeptidase activity may be regulated by the changing of the concentration of catecholamines in the central nervous system.

摘要

研究了儿茶酚胺及其代谢中间体和衍生物对大鼠脑二肽基氨基肽酶活性的抑制作用。该酶从含有溶酶体（以及突触体）的粗线粒体组分中提取，并通过三步柱色谱法进行纯化。纯化后的酶活性受到低浓度（IC50约为2至5 mM）的多巴胺、去甲肾上腺素和肾上腺素的抑制。具有羧基的二羟基苯丙氨酸或二羟基苯乙酸仅表现出较弱的抑制作用（IC50大于10 mM）。这些结果表明，脑二肽基氨基肽酶活性可能受中枢神经系统中儿茶酚胺浓度变化的调节。