4-β-O-酰基鬼臼毒素和4-β-O-烷基鬼臼毒素 的合成及其拒食活性

4-β-O-酰基鬼臼毒素和4-β-O-烷基鬼臼毒素的合成及其拒食活性

摘要: 为研究鬼臼毒素类化合物结构与杀虫活性的关系,合成了4个4-β-O-酰基鬼臼毒素和3个 4-β-O-烷基鬼臼毒素类化合物,其中5个化合物未见文献报道,其结构经MS、1H NMR和元素分析确证。采用小叶碟添加法测试了所合成化合物对3龄粘虫Mythimna separate幼虫24 h和 48 h的拒食活性,结果表明:4-β-O-烷基鬼臼毒素类化合物的活性相对高于酰基化产物和对照鬼臼毒素(PPT)和脱氧鬼臼毒素(DPPT)。其中,4-β-O-甲基鬼臼毒素48 h的活性最高,其拒食中浓度(AFC50)为144.6 mg/L,是DPPT的4.3倍。酰基化鬼臼毒素类化合物的活性相对较低。

Abstract: Four 4-β-O-acylpodophyllotoxin and three 4-β-O-alkylpodophyllotoxin analogues were synthesized, and their structure were confirmed by MS, 1H NMR and elemental analysis. The 24 h and 48 h antifeedant activity against the 3rd larvae of Mythimna separate were assayed with leaf-disk method. The bioassay results showed that the activity of 4-β-O-alkylpodophyllotoxin analogues were higher than its carboxylate ones and control compounds podophyllotoxin(PPT) and deoxypodophyllotoxin(DPPT). The 4-β-4-O-methylpodophyllotoxin was the highest one during 48 h bioassay, and its AFC50 was 144.6 mg/L, 4.3 times of DPPT. The 4-β-O-acylpodophyllotoxin had relative lower activity.