Regioselective O-demethylation of scoparone: differentiation between rat liver cytochrome P-450 isozymes.

D Müller-Enoch, E Büttgen, A Nonnenmacher
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引用次数: 9

Abstract

The ratios of the scoparone O-demethylation products scopoletin to isoscopoletin were determined for reconstituted complexes of NADPH-P-450 reductase and each of four P-450 isozymes in a 2:1 molar ratio with a 1:1 mixture of [7-O-methyl-14C]- and [6-O-methyl-14C]-scoparone as substrate. The two phenobarbital inducible forms P-450PB-B and P-450PB-D have a 1:0.8 +/- 0.05 scopoletin to isoscopoletin ratio, and the two beta-naphthoflavone inducible forms P-450 beta NF-B and P-450 beta NF/ISF-G have ratios of 1:4.4 +/- 0.1 and 1:3.8 +/- 0.1, respectively. The scoparone-O-demethylation activities of the reconstituted preformed complexes of the four P-450 isozymes are given.

天scopone的区域选择性o -去甲基化:大鼠肝细胞色素P-450同工酶的分化。
以[7- o -甲基- 14c]-和[6- o -甲基- 14c]-天冬酮为底物,以2:1的摩尔比重组NADPH-P-450还原酶和四种P-450同工酶的配合物,测定了天冬酮o -去甲基化产物东莨菪素与异东莨菪素的比例。两种苯巴比妥诱导形式P-450PB-B和P-450PB-D的东莨菪素与异东莨菪素的比值为1:0.8 +/- 0.05,两种β -萘黄酮诱导形式P-450 β NF- b和P-450 β NF/ISF-G的比值分别为1:4.4 +/- 0.1和1:8 .8 +/- 0.1。给出了四种P-450同工酶的重组预形成配合物的天冬酮- o去甲基化活性。
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