THE MEMBRANES OF CULTURED RAT-BRAIN ASTROCYTES CONTAIN ENDOTHELIN-CONVERTING ENZYME-ACTIVITY

被引：21

作者：

DESCHEPPER, CF ^{[1
]}

HOUWELING, AD ^{[1
]}

PICARD, S ^{[1
]}

机构：

[1] UNIV MONTREAL,MONTREAL,PQ H2W 1R7,CANADA

来源：

EUROPEAN JOURNAL OF PHARMACOLOGY | 1995年 / 275卷 / 01期

基金：

英国医学研究理事会;

关键词：

ENDOTHELIN; BIG-ENDOTHELIN; ENDOTHELIN-CONVERTING ENZYME; BRAIN; ASTROCYTE; PHOSPHOLIPASE A(2);

D O I：

10.1016/0014-2999(94)00746-T

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Both endothelins and their big-endothelin precursors were found capable of inducing the release of arachidonic acid from purified cultures of rat astrocytes. Their order of potency was as follows: big-endothelin-3 < big-endothelin-1 < endothelin-1 = endothelin-3. Mature endothelins induced the release of arachidonic acid in a rapid fashion. In contrast, much longer incubation times were required for big-endothelins to exert an effect, suggesting that their activity was dependent on their conversion. When big-endothelin-1 was added to the incubation medium of intact live astrocytes, it was converted into mature endothelin-1 in a time-dependent manner and the conversion was inhibited by phosphoramidon. This suggests that astrocytic endothelin-converting enzyme is (at least in part) an external membrane-bound metalloprotease. Some conversion of big-endothelin-3 into endothelin-3 also occurred. However, it was less efficient than the conversion of big-endothelin-1, which is compatible with the lower bioactivity of big-endothelin-3 vs, that of big-endothelin-1 in astrocytes.

引用

页码：61 / 66

页数：6

共 34 条

[1] THE ENDOTHELIN-CONVERTING ENZYME FROM HUMAN UMBILICAL VEIN IS A MEMBRANE-BOUND METALLOPROTEASE SIMILAR TO THAT FROM BOVINE AORTIC ENDOTHELIAL-CELLS [J].