Ma Tengfei, Li Tiansong, Zhang Yi, Lakhvich Fedor A, Khlebnicova Tatyana S, Fu Ying, Ye Fei
Department of Chemistry, College of Arts and Sciences, Northeast Agricultural University, Harbin 150030, China.
Institute of Bioorganic Chemistry, National Academy of Sciences of Belarus, Minsk 220084, Belarus.
Pestic Biochem Physiol. 2025 Nov;214:106572. doi: 10.1016/j.pestbp.2025.106572. Epub 2025 Jul 11.
Pigment biosynthesis serves as a fundamental physiological process vital for weeds survival. Disruption of this pathway leads to the depletion of critical pigments, ultimately resulting in weeds death. Consequently, pigment biosynthesis has become a valuable target in modern herbicide development. Herbicides that interfere with pigment biosynthesis often cause visible bleaching symptoms in treated plants, which has led to their classification as "bleaching herbicides." These compounds constitute a critical component of contemporary crop protection programs due to their distinct mode of action and observable effects. They offer numerous advantages, including high efficiency, low toxicity, enhanced crop safety, minimal resistance, and good environmental compatibility. Notably, natural product-inspired pesticides demonstrate particular significance due to their safety and environmentally friendly properties, which are usually selective, effective, and safe for non-target organisms. Capitalizing on these complementary strengths, the strategic incorporation of natural products and their derivatives into bleaching herbicide development offers a highly promising route to novel bioactive molecules. This review systematically examines recent advancements in the exploration of natural products and their structural analogues as bleaching herbicides, with particular emphasis on a comprehensive analysis of critical structure-activity relationship (SAR) and summarizing their action mechanisms and molecular representative scaffolds, including descriptions of the mechanisms of action of bleaching herbicides targeting key enzymes such as p-hydroxyphenylpyruvate dioxygenase (HPPD), phytoene dehydrogenase (PDS), and protoporphyrinogen oxidase (PPO).
色素生物合成是杂草生存所必需的基本生理过程。该途径的破坏会导致关键色素的消耗，最终导致杂草死亡。因此，色素生物合成已成为现代除草剂开发中的一个重要靶点。干扰色素生物合成的除草剂通常会在处理过的植物中引起明显的白化症状，这导致它们被归类为“白化除草剂”。由于其独特的作用方式和可观察到的效果，这些化合物构成了当代作物保护计划的关键组成部分。它们具有许多优点，包括高效、低毒、增强作物安全性、最小抗性和良好的环境相容性。值得注意的是，受天然产物启发的农药因其安全性和环境友好性而具有特殊意义，这些特性通常对非靶标生物具有选择性、有效性和安全性。利用这些互补优势，将天然产物及其衍生物战略性地纳入白化除草剂开发中，为新型生物活性分子提供了一条极具前景的途径。本综述系统地研究了作为白化除草剂的天然产物及其结构类似物探索的最新进展，特别强调了对关键构效关系（SAR）的全面分析，并总结了它们的作用机制和分子代表性支架，包括对白化除草剂靶向对羟基苯丙酮酸双加氧酶（HPPD）、八氢番茄红素脱氢酶（PDS）和原卟啉原氧化酶（PPO）等关键酶的作用机制的描述。
