ENZYMATIC OXIDATION OF PHENOTHIAZINES BY LIPOXYGENASE H2O2 SYSTEM

被引：26
|
作者：
PEREZGILABERT, M [1 ]
SANCHEZFERRER, A [1 ]
GARCIACARMONA, F [1 ]
机构：
[1] UNIV MURCIA,FAC BIOL,DEPT BIOQUIM & BIOL MOLEC A,E-30071 MURCIA,SPAIN
来源：
BIOCHEMICAL PHARMACOLOGY | 1994年 / 47卷 / 12期
关键词：
LIPOXYGENASE; PHENOTHIAZINE; HYDROPEROXIDASE ACTIVITY; XENOBIOTIC;
D O I：
10.1016/0006-2952(94)90260-7
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
Lipoxygenase (LOX) (EC 1.13.11.12) oxidized a wide range of phenothiazine (Pt) tranquillizers to their corresponding radical cations in the presence of H2O2 by means of an enzymatic chemical second-order mechanism with substrate regeneration similar to that of horseradish peroxidase. The optimum pH of LOX for this hydroperoxidase activity was in the acid range (pH 3.0-4.0), as has been shown for other Pt oxidizing systems, such as peroxidase/H2O2 and haemoglobin. LOX showed Michaelis constants for Pt ranging from 1.4 to 8.5 mM and which, in some cases, e.g. trifluoperazine, displayed substrate inhibition. By contrast, it had a high affinity for H2O2 in the mu M to mM range. A new, previously undescribed plot, which relates the enzymatic affinity and the apparent second-order decay of the cation radical, was developed to study the influence of the 2- and 10-substituents in the Pt ring. The implications of this new plot and the LOX-mediated Pt oxidation are also discussed.
引用
收藏
页码：2227 / 2232
页数：6
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