Enzyme-Kinetic Studies on the Interaction of Norflurazon with Phytoene Desaturase
Enzyme-Kinetic Studies on the Interaction of Norflurazon with Phytoene Desaturase
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诺氟拉松与八氢番茄红素去饱和酶相互作用的酶动力学研究
DOI：
10.1515/znc-1989-9-1015
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发表时间：
1989
期刊：
影响因子：
--
通讯作者：
P. Böger
中科院分区：
文献类型：
--
作者：
G. Sandmann;H. Linden;P. Böger
漂白除草剂抑制光合生物中胡萝卜素的生物合成。 Norflurazon [4-氯-5-甲氨基-2-(3-三氟甲基苯基)-哒嗪-3(2H)one]与其靶酶八氢番茄红素去饱和酶的相互作用已通过酶动力学研究进行了表征。 Lineweaver-Burk 图显示诺氟草酮抑制呈非竞争性方式。去甲氟草酮与八氢番茄红素去饱和酶的结合是可逆的，如用未标记的去甲氟草酮完全取代结合的14C标记的除草剂所证明的。在线性 Dixon 图中，诺氟拉酮的 ki 值确定为 0.09 μm。利用本研究中使用的 Anacystis 的体外系统，可以对选定的间苯基取代哒嗪酮进行结构活性研究。这些化合物的抑制特性与其亲脂性之间可以建立线性关系。
Bleaching herbicides inhibit carotene biosynthesis in photosynthetic organisms. The interaction of norflurazon [4-chloro-5-methylamino-2-(3-trifluoromethylphenyl)-pyridazin-3(2H)one] with its target enzyme phytoene desaturase, has been characterized by enzyme-kinetic studies. A Lineweaver-Burk plot showed a non-competitive m anner for norflurazon inhibition. Binding of norflurazon to phytoene desaturase was reversible as dem onstrated by complete replacem ent of bound 14C-labeled herbicide by unlabeled norflurazon. In a linear Dixon plot the ki value for norflurazon was determ ined as 0.09 μм . With the in vitro system from Anacystis used in this study it was possible to perform structure-activity studies with selected m -phenyl-substituted pyridazinones. A linear relationship between inhibitory properties of these compounds and their lipophilicity could be established.