The discovery of a novel site of action for herbicidal bisphosphonates
The discovery of a novel site of action for herbicidal bisphosphonates
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DOI：
10.1006/pest.1999.2397
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发表时间：
1999-02-01
影响因子：
4.7
通讯作者：
Grossman, JN
中科院分区：
文献类型：
--
作者：
Cromartie, TH;Fisher, KJ;Grossman, JN
在对一类含有1，1-双膦酸酯部分的除草剂重新产生兴趣之后，开始了鉴定这些化合物的分子靶标的研究。发现N-（2-（3-甲基吡啶基））氨基亚甲基二膦酸（化合物I），这组的代表性实例，不抑制液泡膜中的可溶性植物焦磷酸酶或H+-易位焦磷酸酶。从乙酸酯或丙酮酸酯的脂肪酸生物合成也不被这种除草剂抑制。植物种子的发芽没有受到抑制的双膦酸盐，但根的生长在黑暗中强烈抑制呼吸没有显着的影响。二膦酸盐对核酸生物合成的影响不大。然而，水仙（Narcissus sp.）发现化合物I在2.5 μ M时强烈抑制质体。进一步的研究表明，异戊烯基焦磷酸：二甲基烯丙基焦磷酸异构酶不被化合物阻断，但法呢基焦磷酸合酶被化合物I非常强烈地抑制，IC 50为23 nM。有人提出，双膦酸盐如化合物I是除草剂，这是由于抑制异戊烯基生物合成途径中的法呢基焦磷酸合酶，并且这种酶代表了开发除草剂的新靶位点。(C)北京：科学出版社.
Following renewed interest in a class of herbicides containing a 1,1-bisphosphonate moiety, studies to identify the molecular target for these compounds were initiated. N-(2-(3-methylpyridyl)) aminomethylene diphosphonic acid (compound I), a representative example of this group, was found not to inhibit soluble plant pyrophosphatases or H+-translocating pyrophosphatases in the vacuolar membrane. Fatty acid biosynthesis from acetate or from pyruvate was also not suppressed by this herbicide. Germination of plant seeds was not inhibited by the bisphosphonate, but root growth in the dark was strongly inhibited without a significant effect on respiration. The bisphosphonate had little effect on nucleic acid biosynthesis. However, the biosynthesis of carotenoids from isopentenyl pyrophosphate in daffodil (Narcissus sp.) chromoplasts was found to be strongly inhibited by compound I at 2.5 mu M. Further study showed that isopentenyl pyrophosphate:dimethylallylpyrophosphate isomerase was not blocked by the compound but that farnesyl pyrophosphate synthase was very strongly inhibited by compound I with an IC50 of 23 nM. It is proposed that bisphosphonates such as compound I are herbicidal as a result of the inhibition of farnesyl pyrophosphate synthase in the prenyl biosynthetic pathway and that this enzyme represents a new target site for the development of herbicides. (C) 1999 Academic Press.