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[疏水性硝酰自由基抑制5-脂氧合酶介导的亚油醇氧化]

[Hydrophobic nitroxyl radicals inhibit linoleyl alcohol oxidation by 5-lipoxygenase].

作者信息

Vovk A I, Kharchenko O V, Kharitonenko A I, Kukhar' V P, Babiĭ L B, Kazachkov M G, Mel'nik A K, Khil'chevskiĭ A N

出版信息

Bioorg Khim. 2004 Jul-Aug;30(4):436-40. doi: 10.1023/b:rubi.0000037267.60712.21.

Abstract

The linoleyl alcohol oxidation catalyzed by potato tuber 5-lipoxygenase was found to be efficiently inhibited by stable nitroxyl radicals: 1-oxyl-2,2,6,6-tetramethylpiperidin-4-yl 1-bicyclo[2,2,2]octane-1-carboxylate, 1-adamantylacetate, dodecanoate, and octadecanoate. The dependence of apparent IC50 values on the rotational correlation times of times of 4-hydroxy-1-oxyl-2,2,6,6-tetramethylpiperidine and its derivatives in model micellar systems was analyzed. The inhibition mechanism was proposed; it involves the interaction of hydrophobic nitroxyl radical with the intermediate radical enzyme-substrate complex.

摘要

马铃薯块茎5-脂氧合酶催化的亚油醇氧化被发现可被稳定的硝酰自由基有效抑制:1-氧基-2,2,6,6-四甲基哌啶-4-基 1-双环[2,2,2]辛烷-1-羧酸酯、1-金刚烷基乙酸酯、十二烷酸酯和十八烷酸酯。分析了模型胶束体系中表观IC50值与4-羟基-1-氧基-2,2,6,6-四甲基哌啶及其衍生物旋转相关时间的关系。提出了抑制机制;它涉及疏水性硝酰自由基与中间自由基酶-底物复合物的相互作用。

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