链脲佐菌素在体外和体内对琥珀酰辅酶A合成酶活性的抑制作用。

Inhibition by streptozotocin of the activity of succinyl-CoA synthetase in vitro and in vivo.

作者信息

Boquist L, Ericsson I

出版信息

FEBS Lett. 1986 Feb 17;196(2):341-3. doi: 10.1016/0014-5793(86)80275-7.

Abstract

The activity of succinyl-CoA synthetase from mouse liver and kidney was inhibited by streptozotocin in vitro. Streptozotocin behaved essentially as a non-competitive inhibitor, and the following kinetic values were obtained (in the presence of 10 nM streptozotocin): apparent Km 1.7 mM, apparent Ki 10 nM, and kcat 440 nkat X kg-1. Compared with non-diabetic control mice, the succinyl-CoA synthetase activity was significantly decreased in the islets and kidneys of mice with early (1 h) and manifest (greater than or equal to 2 days) streptozotocin diabetes, whereas the activity in the liver was not significantly altered. Inhibited succinyl-CoA synthetase activity is believed to play a prominent role in the cellular effects of streptozotocin.

摘要

链脲佐菌素在体外可抑制小鼠肝脏和肾脏中琥珀酰辅酶A合成酶的活性。链脲佐菌素表现为基本的非竞争性抑制剂，并且获得了以下动力学值（在存在10 nM链脲佐菌素的情况下）：表观Km为1.7 mM，表观Ki为10 nM，以及kcat为440 nkat X kg-1。与非糖尿病对照小鼠相比，早期（1小时）和明显（大于或等于2天）链脲佐菌素糖尿病小鼠的胰岛和肾脏中琥珀酰辅酶A合成酶活性显著降低，而肝脏中的活性未发生显著改变。琥珀酰辅酶A合成酶活性受到抑制被认为在链脲佐菌素的细胞效应中起重要作用。