Besides structural modification of natural bioactive products to afford promising agrochemical candidates, investigation of their mechanisms of action against pests is also an important strategy to obtain novel potentially botanical pesticides. N-(p-Ethyl)phenylsulfonylmatrinic acid (2), derived from an natural alkaloid matrine (1), exhibited about 5.9-fold more pronounced acaricidal activity than 1 against the adult females of Tetranychus cinnabarinus Boisduval, and good control efficiency in the greenhouse. By comparison of nAChR, AChE and VGSC of treated and untreated T. cinnabarinus via RT-PCR and qRT-PCR analysis, it was found that compound 2 could activate nAChR and VGSC via up-regulation of nAChR α1, α4 and α5 subunits and VGSC expressions; compound 2 may be the AChE and AChE enzyme inhibitor. Importantly, a scheme of compound 2 interaction with nAChR, AChE and VGSC of T. cinnabarinus was proposed. It will lay the foundation for future optimization and application of matrine derivatives as agrochemicals.

除了对天然生物活性产品进行结构修饰以提供有前途的农药候选物之外，研究其对害虫的作用机理也是获得新型潜在植物性农药的重要策略。源自天然生物碱苦参碱（1）的N-（p-乙基）苯磺酰matrinic酸（2）对Tetranychus cinnabarinus Boisduval的成年雌性的杀螨活性比1增强了约5.9倍，并且在温室中的防治效果良好。通过比较处理过的和未处理过的朱砂丁香线的nAChR，AChE和VGSC通过RT-PCR和qRT-PCR分析，发现化合物2可以通过上调nAChR的α1，α4和α5亚基以及VGSC的表达来激活nAChR和VGSC 。化合物2可以是AChE和AChE酶抑制剂。重要的是，提出了一种化合物2与朱砂丁香的nAChR，AChE和VGSC相互作用的方案。这将为将来优化和应用苦参碱衍生物作为农用化学品奠定基础。