Graduate School of Agricultural and Life Sciences, The University of Tokyo, Tokyo 113-8657, Japan.
Int J Mol Sci. 2023 Aug 4;24(15):12420. doi: 10.3390/ijms241512420.
Ethylene is the only gaseous plant hormone that regulates several aspects of plant growth, from seedling morphogenesis to fruit ripening and organ senescence. Ethylene also stimulates the germination of , a root parasitic weed that severely damages crops in sub-Saharan Africa. Thus, ethylene response stimulants can be used as weed and crop control agents. Ethylene and ethephon, an ethylene-releasing compound, are currently used as ethylene response inducers. However, since ethylene is a gas, which limits its practical application, we targeted the development of a solid ethylene response inducer that could overcome this disadvantage. We performed chemical screening using "triple response" as an indicator of ethylene response. After screening, we selected a compound with a thiourea skeleton and named it ZKT1. We then synthesized various derivatives of ZKT1 and evaluated their ethylene-like activities in . Some derivatives showed considerably higher activity than ZKT1, and their activity was comparable to that of 1-aminocyclopropane-1-carboxylate. Mode of action analysis using chemical inhibitors and ethylene signaling mutants revealed that ZKT1 derivatives activate the ethylene signaling pathway through interactions with its upstream components. These thiourea derivatives can potentially be potent crop-controlling chemicals.
乙烯是唯一一种调节植物生长多个方面的气态植物激素，从幼苗形态发生到果实成熟和器官衰老。乙烯还刺激寄生在根部的杂草种子的萌发，这种杂草在撒哈拉以南非洲严重损害农作物。因此，乙烯反应刺激剂可用作杂草和作物控制剂。乙烯和乙烯膦，一种释放乙烯的化合物，目前被用作乙烯反应诱导剂。然而，由于乙烯是一种气体，这限制了它的实际应用，我们的目标是开发一种可以克服这一缺点的固体乙烯反应诱导剂。我们使用“三重反应”作为乙烯反应的指示剂进行了化学筛选。筛选后，我们选择了一种具有硫脲骨架的化合物，并将其命名为 ZKT1。然后，我们合成了 ZKT1 的各种衍生物，并在 中评估了它们的类似乙烯活性。一些衍生物表现出比 ZKT1 更高的活性，其活性与 1-氨基环丙烷-1-羧酸相当。使用化学抑制剂和乙烯信号突变体的作用模式分析表明，ZKT1 衍生物通过与上游成分相互作用激活乙烯信号通路。这些硫脲衍生物有可能成为有效的作物控制化学品。
