一些胺类作为豌豆二胺氧化酶的抑制剂。

Some amines as inhibitors of pea diamine oxidase.

作者信息

Pec P, Frébort I

机构信息

Department of Analytical and Organic Chemistry, Faculty of Science, Palacký University, Olomouc, Czechoslovakia.

出版信息

J Enzyme Inhib. 1992;5(4):323-9. doi: 10.3109/14756369109069074.

DOI:10.3109/14756369109069074

PMID:1285253

Abstract

The inhibition of pea diamine oxidase (DAO; EC 1.4.3.6) by some amines and chelating agents has been studied. Ethylenediamine (competitive, Ki = 5.2 mmol.l-1), cis-1,2-diaminocyclohexane (noncompetitive, Ki = 2.9 mmol.l-1) and trans-1,2-diaminocyclohexane (competitive, Ki = 3.6 mmol.l-1) are weak inhibitors whereas diethylenetriamine (noncompetitive, Ki = 7.2 mumol.l-1), triethylenetetraamine (partial noncompetitive, Ki = 0.57 mumol.l-1) are potent inhibitors. The chelating agents 1,10-phenanthroline (Ki = 0.031 mmol.l-1), and 2,2'-bipyridyl (Ki = 0.058 mmol.l-1) are noncompetitive inhibitors. The pH-inhibition profile for the inhibitors indicates that the protonated forms are the active species.

摘要

研究了一些胺类和螯合剂对豌豆二胺氧化酶（DAO；EC 1.4.3.6）的抑制作用。乙二胺（竞争性抑制，Ki = 5.2 mmol·l⁻¹）、顺式-1,2-二氨基环己烷（非竞争性抑制，Ki = 2.9 mmol·l⁻¹）和反式-1,2-二氨基环己烷（竞争性抑制，Ki = 3.6 mmol·l⁻¹）是弱抑制剂，而二亚乙基三胺（非竞争性抑制，Ki = 7.2 μmol·l⁻¹）、三亚乙基四胺（部分非竞争性抑制，Ki = 0.57 μmol·l⁻¹）是强效抑制剂。螯合剂1,10-菲啰啉（Ki = 0.031 mmol·l⁻¹）和2,2'-联吡啶（Ki = 0.058 mmol·l⁻¹）是非竞争性抑制剂。抑制剂的pH抑制曲线表明，质子化形式是活性物种。