【作者】 刘国强；

【导师】 吴文君；

【作者基本信息】 西北农林科技大学 ， 农药学， 2003， 博士

【摘要】 通过对植物杀虫活性成分筛选、分离与鉴定，发现新的天然杀虫活性先导化合物，是创制新农药的重要途径。 本项研究在国家自然科学基金重点项目“新型昆虫消化毒剂的先导优化及作用靶标研究（30130130）”支持下，对卫矛科卫矛属和南蛇藤属 13 种植物进行了室内杀虫活性筛选，在此基础上，采用柱层析、反相 HPLC 制备及纯化，应用高分辨质谱和核磁共振等现代波谱技术，在生物活性追踪指导下，分离、鉴定冬青卫矛、大芽南蛇藤、短枝南蛇藤根皮提取物杀虫活性成分。主要结果如下： 1、对 13 种植物杀虫活性测定结果表明，拒食活性以无柄卫矛的活性最高。胃毒杀虫活性最高的植物为大芽南蛇藤、冬青卫矛。触杀杀虫活性绿花卫矛的石油醚提取物活性最高。无柄卫矛的石油醚提取物和曲脉卫矛甲醇提取物抑制玉米象种群繁殖抑制活性最高。 2、 从大芽南蛇藤根皮中分离鉴定了 6 个化合物，其中 NW06 为苯甲酸，NW10 为β—谷甾醇，均为已知化合物；分离得到 3 个对昆虫具有毒杀活性的三取代 β-二氢沉香呋喃骨架的化合物： NW02（NW08）为 1α,9β-二呋喃甲酰氧基-6β-乙酰氧基-β-二氢沉香呋喃；NW04 为 1α-呋喃甲酰氧基-6β-乙酰氧基-9β-苯甲酰氧基-β-二氢沉香呋喃；NW05 为 1α,9β-二苯甲酰氧基-2α-乙酰氧基-β-二氢沉香呋喃。经文献检索，NW02（NW08）、NW04 和 NW05 为首次分离鉴定的新化合物。 3、从短枝南蛇藤的根皮粉中分离得到 2 个对昆虫具有毒杀活性的 β-二氢沉香呋喃骨架类化合物：LY01 为 1α-乙酰氧基-2α-α甲基丁酰氧基-4β，9β-二羟基-6β，8β-二苯甲酰氧基-β-二氢沉香呋喃；LY02 为 1α，9β-二乙酰氧基-2α，8β--二苯甲酰氧基-4β，6β-二羟基-β-二氢沉香呋喃。经文献检索，LY01 和 LY02 为首次分离鉴定的新化合物。 4、从冬青卫矛根皮中分离得到 3 个化合物， LY14：Celangulin V 和 Ly19：1α，2α，4β，6β，8β，9α，13-七羟基-β-二氢沉香呋喃，均为首次从冬青卫矛中分离的化合物； LY11 为β—谷甾醇。 5、采用载毒叶碟饲喂法测定 6 个二氢沉香呋喃骨架化合物对粘虫和小菜蛾的杀虫活性， 除 LY19 没有活性外，均表现毒杀活性，毒杀活性大小依次为 NW04> NW05>NW02>LY02> LY01。NW04 在质量体积比 2.5%和 1.25％浓度下，对 3 龄粘虫幼虫的死亡率分别为 100%和 70%，对 3 龄小菜蛾幼虫的死亡率分别为 50％和 20%。更多还原

【Abstract】 The study was funded by National Natural Science Fund, which was a part of theproject “Study on Lead Optimizing of Novel Insect Digest poison and Action Target” (NO.30130130). Based on the preliminary screening results of insecticidal activities among 13species Celastraceae, 11 chemicals were isolated from 3 species plants (Celastrusgemmatus Loes., C. rosthornianus Loes. and Euonymus japonicus Thunb.), and 6chemicals exhibited insecticidal activity. The process of isolation and purity of insecticidalchemicals were guided by the bioassay and phytochemistry method, such as the columnChromatography, Preparative TLC and Preparative HPLC, have been used. Six compounds (NW02, NW04, NW05, NW06, NW08, NW10) were isolated fromroot bark of Celastrus gemmatus Loes, and the structure were elucidated by spectralmethods. NW06 is benzoic acid and NW10 is β-sterol, they are both known chemicals.NW02 is 6β-diacetoxy-1α,9β-difurancarbonyloxy-β-dihydroagarofuran and NW08 is thesame as it, NW04 is 6β-diacetoxy-9β-benzoyloxy-1α-difurancarbonyloxy-β-dihydroagarofuran, NW05 is2α-acetoxy-1α,9β-dibenzoyloxy-β-dihyfroagarofuran. Based on searching on novelty,above three chemicals are all novel nature products. Two new compounds (LY01 and LY02) were isolated from root bark of C.rosthornianus Loes. LY01 is 1α-acetoxy-6β,8β-dibenzoyloxy-4β,9β-dihydroyl-2α-（ α-methylbutanoyloxy ） -β-dihydroagarofuran and LY02 is1α,9β-diacetoxy-2α,8β-dibenzoyloxy-4β,6β-dihydroyl-β-dihydroagarofuran. Three compounds (LY11, LY14 and LY19) were isolated from root bark of Euonymusjaponicus Thunb.. LY11 isβ-sterol, LY14 is Celangulin V which was first reported fromCelastrus angulatus Max., LY19 is 1 α ,2 α ,4 β ,6 β ,8 β ,9α,13-hepthydroyl-β-dihydroagarofuran. Both LY14 and LY19 were isolated from the plantat the first time. The insectidical activies of six compounds with β-dihydroagarofuran sketon againstthe 3rd instars larvae of Mythimna separata Walker and Plutella xylostella were tested. Theresults showed that 5 compounds exhibited the stomach-toxicity activity, the order ofactivity is NW04> NW05> NW02>LY02> LY01, but LY19 did not exhibit activity. The<WP=9>mortality of NW04 against Mythimna separata Walker and Plutella xylostella were 100%and 50% at the concentration of 2.5% (W/V) respectively, 70% and 20% at theconcentration of 1.25% (W/V) respectively.更多还原