设计了两个系列的新型槐定碱衍生物,合成,并评估了他们的灭蚊活性。SOP-2g,SOP-2q,SOP-2r对白纹伊蚊幼虫表现出潜在的杀幼虫活性,LC50值为330.98、430.53和411.09ppm,分别。构效关系分析表明,肟酯基团有利于提高杀虫生物活性,而引入了长链脂肪族基团和稠环基团。此外,还根据乙酰胆碱酯酶(AChE)的抑制测定和用衍生物处理的死幼虫的形态学观察研究了杀幼虫的机制。结果表明,优选的三种衍生物的AChE抑制活性为63.16%,46.67%,和35.11%,分别,在250ppm浓度。此外,形态学证据表明,SOP-2q和SOP-2r诱导幼虫肠腔的变化,尾骨,和尾巴,从而显示出对Ae的杀幼虫作用。白纹与AChE一起抑制。因此,这项研究表明,槐定碱及其新型衍生物可用于控制蚊子幼虫的数量,这也可能是降低蚊子种群密度的有效生物碱。
Two series of novel sophoridine derivatives were designed, synthesized, and evaluated for their anti-mosquito activity. SOP-2g, SOP-2q, and SOP-2r exhibited potential larvicidal activity against Aedes albopictus larva with LC50 values of 330.98, 430.53, and 411.09 ppm, respectively. Analysis of structure-activity relationships indicated that the oxime ester group was beneficial for improving the larvicidal biological activity, whereas the long-chain aliphatic group and fused-ring group were introduced. Furthermore, the larvicidal mechanism was also investigated based on the inhibition assay of acetylcholinesterase (AChE) and the morphological observation of dead larva treated with derivatives. Results indicated that the AChE inhibitory activity of the preferred three derivatives were 63.16%, 46.67%, and 35.11%, respectively, at 250 ppm concentration. Additionally, morphological evidence demonstrated that SOP-2q and SOP-2r induced changes in the larva\'s intestinal cavity, caudal gill, and tail, thereby displaying larvicidal action against Ae. albopictus together with AChE inhibition. Therefore, this study implied that sophoridine and its novel derivatives could be used to control the population of mosquito larva, which may also be effective alkaloids to reduce the mosquito population density.