当前位置： SCI文献检索 > BIOORGANIC & MEDICINAL CHEMISTRY期刊下所有文献 > Mechanism of biochemical action of substituted 4-methylbenzopyran-2-ones. Part 4: hyperbolic activation of rat liver microsomal NADPH-cytochrome C reductase by the novel acetylator 7,8-diacetoxy-4-methylcoumarin.

Mechanism of biochemical action of substituted 4-methylbenzopyran-2-ones. Part 4: hyperbolic activation of rat liver microsomal NADPH-cytochrome C reductase by the novel acetylator 7,8-diacetoxy-4-methylcoumarin.

Abstract：

:The effect of 7,8-diacetoxy-4-methylcoumarin (DAMC) has been studied on hepatic NADPH cytochrome C reductase-- an enzyme participating in the microsomal electron transport. The preincubation of liver microsomes with DAMC resulted in a time-dependent activation of NADPH cytochrome C reductase. The catalytic activity of the enzyme enhanced nearly 600% by 25 microM concentration of DAMC after 10 min of preincubation. The action of DAMC on the reductase resulted in enhanced v(max) while Km remained constant. A plot of 1/v(max) as a function of DAMC concentration resulted in a non-linear, but rectangular hyperbola indicative of hyperbolic activation. DAMC was also proved to be effective in significantly enhancing the activity of NADPH cytochrome C reductase in vivo. 7,8-Dihydroxy-4-methylcoumarin (DHMC), the deacetylated product of DAMC failed to irreversibly activate the enzyme. The activation effect of DAMC upon the enzyme was abolished by p-hydroxymercury benzoate. The role of a transacetylase in transferring the acetyl group of DAMC to the amino acid(s) of the active site of NADPH cytochrome C reductase causing irreversible enzyme activation is enunciated.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Raj HG,Parmar VS,Jain SC,Goel S,Singh A,Tyagi YK,Jha HN,Olsen CE,Wengel J

doi

10.1016/s0968-0896(98)00228-4

subject

Has Abstract

pub_date

1999-02-01 00:00:00

pages

369-73

issue

2

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(98)00228-4

journal_volume

7

pub_type

杂志文章

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