西咪替丁对肾碱性磷酸酶的抑制作用。

Inhibition of renal alkaline phosphatase by cimetidine.

作者信息

Minai-Tehrani Dariush, Khodai Somayeh, Aminnaseri Somayeh, Minoui Saeed, Sobhani-Damavadifar Zahra, Alavi Sana, Osmani Raheleh, Ahmadi Shiva

机构信息

BioResearch Lab, Faculty of Biological Sciences, Shahid Beheshti University G.C, Iran.

出版信息

Drug Metab Lett. 2011 Aug;5(3):197-201. doi: 10.2174/187231211796904982.

DOI:10.2174/187231211796904982

PMID:21679151

Abstract

Alkaline phosphatase (ALP) belongs to hydrolase group of enzymes. It is responsible for removing phosphate groups from many types of molecules, including nucleotides and proteins. Cimetidine (trade name Tagamet) is an antagonist of histamine H2-receptor that inhibits the production of gastric acid. Cimetidine is used for the treatment of gastrointestinal diseases. In this study the inhibitory effect of cimetidine on mouse renal ALP activity was investigated. Our results showed that cimetidine can inhibit ALP by uncompetitive inhibition. In the absence of inhibitor the V(max) and K(m) of the enzyme were found to be 13.7 mmol/mg prot.min and 0.25 mM, respectively. Both the Vmax and Km of the enzyme decreased with increasing cimetidine concentrations (0- 1.2 mM). The Ki and IC(50) of cimetidine were determined to be about 0.5 mM and 0.52 mM, respectively.

摘要

碱性磷酸酶（ALP）属于水解酶类。它负责从多种类型的分子中去除磷酸基团，包括核苷酸和蛋白质。西咪替丁（商品名泰胃美）是组胺H2受体拮抗剂，可抑制胃酸分泌。西咪替丁用于治疗胃肠道疾病。在本研究中，研究了西咪替丁对小鼠肾碱性磷酸酶活性的抑制作用。我们的结果表明，西咪替丁可通过非竞争性抑制作用抑制碱性磷酸酶。在无抑制剂的情况下，该酶的V(max)和K(m)分别为13.7 mmol/mg蛋白·分钟和0.25 mM。随着西咪替丁浓度（0 - 1.2 mM）的增加，该酶的Vmax和Km均降低。西咪替丁的Ki和IC(50)分别测定为约0.5 mM和0.52 mM。