BASF Global Insecticide Research, Research Triangle Park, NC, USA.
Pest Manag Sci. 2021 Aug;77(8):3631-3636. doi: 10.1002/ps.6369. Epub 2021 Mar 29.
Pro-insecticides have been a significant part of the insecticide market for decades. Bioactivation of such compounds is generally an enzyme-controlled process, in which the target insect metabolizes the pro-form into an active compound. This approach has several potential advantages, including improved bio-kinetic properties and safety profiles of the pro-insecticide relative to the active form. A less common advantage of pro-insecticides is increased activity on metabolically resistant strains. Specific cases in which a pro-insecticide demonstrates negative cross-resistance (NCR) on a metabolically resistant strain due to increased bioactivation of the pro-insecticide have been noted sporadically over the past 50+ years but have not been reviewed before. The purpose of this mini-review is to catalog the cases in which a pro-insecticide demonstrated improved activity on an insect strain resistant to a second insecticide via a metabolic mechanism. Cases are relatively rare, but where it does occur the mechanism of NCR is generally recognized as being due to the increased metabolic activity of the resistant strain. These observations can provide learnings with potential application for resistance management if the correct pro-insecticide is selected for a resistant strain which is better able to bioactivate it. A better understanding of the bioactivation of pro-insecticides by resistant insects could also aid in insecticide discovery, potentially leading to improved pro-insecticide design. © 2021 Society of Chemical Industry.
几十年来，前体杀虫剂一直是杀虫剂市场的重要组成部分。此类化合物的生物激活通常是一个酶控过程，其中目标昆虫将原药代谢为活性化合物。这种方法有几个潜在的优点，包括与活性形式相比，原药具有改善的生物动力学特性和安全性特征。原药的一个不太常见的优点是对代谢抗性菌株的活性增加。在过去的 50 多年中，已经偶然注意到特定情况下，由于原药的生物激活增加，前体杀虫剂在代谢抗性菌株上表现出负交叉抗性（NCR），但以前没有对此进行过综述。本综述的目的是列出在通过代谢机制对第二种杀虫剂具有抗性的昆虫品系中，前体杀虫剂表现出增强活性的情况。这种情况相对较少见，但确实发生时，NCR 的机制通常被认为是由于抗性品系的代谢活性增加。如果为能够更好地生物激活它的抗性菌株选择了正确的前体杀虫剂，这些观察结果可为抗性管理提供潜在的应用经验。如果抗性昆虫对前体杀虫剂的生物激活有更好的了解，也可能有助于杀虫剂的发现，从而可能导致更好的前体杀虫剂设计。© 2021 英国化学学会。
