College of Plant Protection, Northwest A&F University, Yangling 712100, Shaanxi, China.
School of Marine Sciences, Ningbo University, Ningbo 315211, Zhejiang, China.
J Agric Food Chem. 2024 Mar 20;72(11):5574-5584. doi: 10.1021/acs.jafc.3c06681. Epub 2024 Mar 11.
To explore the use of nonfood plant-derived secondary metabolites for plant protection, a series of ester derivatives for controlling the major migratory agricultural pests were obtained by structural modification of andrographolide, a labdane diterpenoid isolated from . Compound showed good insecticidal activity against the fall armyworm Smith. Compounds (LC: 0.382 mg/mL) and (LC: 0.563 mg/mL), the acaricidal activities of which were, respectively, 13.1 and 8.9 times that of andrographolide (LC: 4.996 mg/mL), exhibited strong acaricidal and control effects against Boisduval. Against Van der Goot, compounds and displayed 3.9- and 3.7-fold pronounced aphicidal activity of andrographolide. Effects of compound on three protective enzymes (superoxide dismutase, peroxidase, and catalase) of were also observed. The obvious differences of epidermal cuticle structures of mites treated with compound were determined by scanning electron microscopy. Structure-activity relationships indicated that 14-ester derivatives of andrographolide showed potential insecticidal/acaricidal activities and can be further utilized as lead compounds.
为了探索非食用植物源性次生代谢产物在植物保护中的应用，通过对从穿心莲中分离得到的贝壳杉烷二萜内酯——穿心莲内酯进行结构修饰，得到了一系列用于防治主要迁飞性农业害虫的酯类衍生物。化合物 对鳞翅目夜蛾科害虫——草地贪夜蛾 Smith 表现出良好的杀虫活性。化合物 （LC: 0.382 mg/mL）和 （LC: 0.563 mg/mL）对朱砂叶螨的杀螨活性分别是穿心莲内酯（LC: 4.996 mg/mL）的 13.1 倍和 8.9 倍，对二斑叶螨表现出较强的杀螨和防治效果。对桃蚜，化合物 和 表现出比穿心莲内酯强 3.9 倍和 3.7 倍的杀虫活性。还观察了化合物 对 3 种保护酶（超氧化物歧化酶、过氧化物酶和过氧化氢酶）的影响。通过扫描电子显微镜观察到了处理后的螨虫表皮角质层结构的明显差异。构效关系表明，穿心莲内酯的 14-酯衍生物具有潜在的杀虫/杀螨活性，可以进一步作为先导化合物加以利用。
