作为除草剂解毒剂的喹喔啉衍生物，通过提高玉米的耐受性。
Quinoxaline derivatives as herbicide safeners by improving Zea mays tolerance.
机构信息
Department of Chemistry, College of Arts and Sciences, Northeast Agricultural University, Harbin 150030, China.
Department of Chemistry, College of Arts and Sciences, Northeast Agricultural University, Harbin 150030, China.
出版信息
Pestic Biochem Physiol. 2021 Nov;179:104958. doi: 10.1016/j.pestbp.2021.104958. Epub 2021 Aug 26.
Isoxaflutole (IXF), a 4-hydroxyphenylpyruvate dioxygenase (HPPD) inhibitor, causes injury to crops leading to reductions in grain yield. In order to solve the phytotoxicity caused by IXF, the present work evaluated the protective response of the substituted quinoxaline derivatives as potential safeners on Zea mays. The bioassay results showed that all of the test compounds displayed protection against IXF. In particular, safener I-6 exhibited excellent safener activity against IXF injury via enhancing glutathione (GSH) content, glutathione S transferases (GSTs) and cytochrome P450 monooxygenases (CYP450) activity. The tested compounds induced the activity of CYP450 and GSTs in Z. mays. The physicochemical properties and ADMET properties of safener I-6, benoxacor and diketonitrile (DKN, IXF metabolite) were compared to predict pharmaceutical behavior. The present work demonstrates that the safener I-6 could be considered as a potential candidate for developing novel safeners in the future.
异恶唑草酮（IXF）是一种 4-羟基苯丙酮酸双加氧酶（HPPD）抑制剂，会对作物造成伤害，导致谷物产量下降。为了解决 IXF 引起的植物毒性，本工作评估了取代喹喔啉衍生物作为潜在解毒剂对玉米的保护响应。生物测定结果表明，所有测试化合物均显示出对 IXF 的保护作用。特别是解毒剂 I-6 通过提高谷胱甘肽（GSH）含量、谷胱甘肽 S 转移酶（GSTs）和细胞色素 P450 单加氧酶（CYP450）活性，对 IXF 损伤表现出优异的解毒活性。测试化合物诱导了玉米中 CYP450 和 GSTs 的活性。对解毒剂 I-6、解草𬪩和二酮腈（IXF 代谢物）的理化性质和 ADMET 性质进行了比较，以预测药物行为。本工作表明，解毒剂 I-6 将来可能被认为是开发新型解毒剂的潜在候选物。
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