昆虫神经肽类激素的研究及应用前景

由昆虫脑神经内分泌细胞分泌的神经肽类激素 ,咽侧体活化激素 (allatotropin ,AT)和咽侧体抑制激素 (al latostatin ,AS) ,分别刺激或抑制咽侧体的保幼激素的生物合成 ,从而控制昆虫的生长、发育和变态。利用昆虫神经内分泌的失调 ,使其体内激素水平失调 ,来达到控制害虫的目的。     

保幼激素类似物对白蚁的作用研究进展

本文介绍了保幼激素类似物对白蚁的影响,包括诱导前兵蚁、兵蚁和一些中间品级(形态畸形)的产生、抑制白蚁的取食、减少或消除白蚁的共生原生动物群、对白蚁产生不同水平的急性和慢性毒性、抑制工蚁蜕皮以及繁殖蚁建立新群体等方面的影响,其中最主要影响是诱导前兵、兵蚁和一些中间品级的产生破坏了白蚁群体品级比例的平衡性或完整性。因此,保幼激素类似物可用于白蚁的防治,并在田间防治散白蚁和乳白蚁均取得了较好的防治效果,并探讨了应用保幼激素类似物防治白蚁的潜力与前景。     

昆虫蜕皮激素类似物的定量构效关系及其受体三维结构研究进展

蜕皮激素及其类似物具有调节昆虫蜕皮、变态和繁殖的功能。蜕皮激素类似物在农业生产,尤其是鳞翅目害虫的防治中发挥着重要作用。总结近期的文献,同时结合课题组的工作,综述了蜕皮激素类似物的定量构效关系、蜕皮激素受体三维结构的研究进展。     

植物源农药研究进展(综述)

与传统化学杀虫剂相比,植物源天然产物杀虫剂具有靶标特异性强、易降解无残留、对环境无污染等优点,符合绿色农业的发展要求,是杀虫剂研发的重要领域之一。本文围绕不同类型植物源天然产物杀虫剂的结构特征和作用机制,综述了2015年之后以植物源杀虫剂活性成分为先导化合物进行结构改造的研究现状,最后对植物源农药的发展方向、当前面临的挑战以及产品研发策略进行了分析和展望。     

复方苦参注射液对肺癌和肝癌细胞抑瘤作用研究

苦参碱及其类似物是一类来源于苦参和苦豆子的生物碱,具有抗癌、消炎、抗病毒、杀虫、杀螨和抑菌等广泛的医用及农用生物活性。本文概述了近10年来苦参碱及其类似物的农用生物活性研究进展,重点总结了近4年来苦参碱及其类似物在结构改造方面的研究情况,对其构效关系进行了分析,以期为今后更好地开发利用苦参碱及其类似物提供参考。     

昆虫性信息素及其类似物干扰昆虫行为的机理和应用研究进展

昆虫性信息素及其类似物在有害生物综合治理中起到了越来越重要的作用,如可以对目标昆虫进行监测、诱捕和迷向等。干扰昆虫行为是一种环境友好型的植物保护策略,近年来已在害虫防治领域广泛使用。干扰昆虫行为的机理一直是科学家研究的主要方向,明确其机理能使之得到更有效合理的应用。本文主要对昆虫性信息素及其类似物干扰昆虫行为的机理,以及缓释材料、施用剂量及密度、与其他挥发性物质在田间混合应用等方面的研究进展进行简要综述。     

茼蒿素类似物的生物活性与作用机理

进行了21种茼蒿素类似物对小菜蛾2龄幼虫的拒食活性筛选,对8号、12号和20号化合物进行了拒食活性测定,研究了20号化合物对菜粉蝶幼虫体壁及血细胞的影响,并进行了20号化合物对菜粉蝶幼虫的田间小区试验.21种茼蒿素类似物中,20号、16号、12号和8号等化合物的拒食活性较好.8号、12号和20号化合物对小菜蛾4龄幼虫处理后24h的非选择性AFC50分别为549.03、405.97和205.06μg/mL;选择性AFC50分别为432.57、114.34和72.32μg/mL.处理后24h,12号与20号化合物对菜粉蝶4龄幼虫的选择性AFC50分别为398.88和280.54μg/mL,20号化合物对菜粉蝶2龄幼虫非选择性AFC50为112.76μg/mL.20号化合物对菜粉蝶4龄幼虫血细胞数量、体壁及体壁中几丁质有明显的抑制作用.药后第3、5和7天,400μg/mL的20号化合物对菜粉蝶幼虫的防治效果分别为28.60%、54.93%和58.21%.     

抑霉菌素防治白粉病的田间药效试验

白粉病(Sphaerotheca cucurbitae)是农作物上重要病害之一,主要危害葫芦科、茄科、豆科、禾本科等作物。抑霉菌素是我们发现的一种新农用抗真菌抗生素,具有高效、安全的特点。本文报道抑霉菌素对长瓜和黄瓜白粉病的田间防治效果。     

二芳酰肼类昆虫生长调节剂的构效关系研究进展

二芳酰肼类化合物是近年来开发的具有蜕皮激素活性的非甾醇类昆虫生长调节剂,能引起昆虫,特别是鳞翅目幼虫早熟、不完全、致死性蜕皮。文章总结近期文献,结合课题组的研究工作,对该类化合物中各个结构片断对其杀虫活性的影响进行了探讨,对结构与活性的关系进行了综述。     

三氟羧草醚类似物的合成及除草活性

以2,5-二羟基苯甲酸甲酯和三氟羧草醚为起始原料,设计合成了3个系列20个新的三氟羧草醚类似物,通过核磁共振氢谱、碳谱对其结构进行了表征。分别采用小杯法和室内盆栽法测定了目标化合物的除草活性。结果表明,化合物 III-02 [5-(2-氯-4-三氟甲基苯氧基)-2-硝基苯甲酸-(6-甲基苯并噻唑-2-基)酯]对单子叶杂草的除草活性明显高于对照药剂三氟羧草醚,其对稗草Echinochloa crusgalli和马唐Digitaria sanguinalis根茎生长的EC₅₀值分别为2.03、0.93 μg/mL和1.49、0.52 μg/mL;在有效成分100 g/hm2的施药剂量下,化合物 III-02 对单子叶杂草稗草、马唐及狗尾草Setaria viridis的防治效果均在85%以上,明显高于三氟羧草醚,对阔叶杂草马齿苋Portulaca oleracea、反枝苋Amaranthus retroflexus及苘麻Abutilon theophrasti的防治效果可达100%。初步构效关系表明,2-硝基苯甲酰衍生物的除草活性明显优于其2-甲氧基衍生物,三氟羧草醚苯甲酸酯衍生物对单子叶杂草的除草活性明显高于其苯甲酰胺衍生物。     

保幼激素类似物对红火蚁的作用研究进展

我国发现红火蚁已有4年,但防治技术、产品依然匮乏。为了改善、提高我国红火蚁的防治技术水平,本文就保幼激素类似物(JHA)对红火蚁的作用表现和防治效果进行了总结分析。JHA可以造成蚁后卵巢萎缩、产卵量减少,导致发育畸形和蚁群等级比例失调,如工蚁数量减少、生殖型幼虫比例以及处女蚁后数量增加等,并最终导致整个蚁群死亡。JHA杀虫剂活性高、低残毒、对环境污染小,在田间防治红火蚁效果彻底,并可有效地防止防治区红火蚁种群的再入侵（re invasion）,但JHA毒饵也存在着防治效果缓慢等问题。本文就克服此类问题作了初步的探讨。     

Comparative testing of several juvenile hormone analogues in two species of locusts,Locusta migratoria migratorioides and Schistocerca gregaria

Effective treatment with juvenile hormone analogues (JHAs) of early penultimate or early last-instar locust hoppers induces a supernumerary ‘extra’ nymphal instar. These ‘extra’ nymphs, also termed ‘adultoids’, die in the course of, or shortly after, an ‘extra’ moult. Less effective treatment results in imperfect adults with crumpled twisted wings which presumably limit their flight and migratory abilities. Extremely effective treatment leads to death in the next moult. Comparing dose-response relations of (7S)-methoprene, fenoxycarb, pyriproxyfen and a new JHA, R70-1 (ethyl cis-N-{2-[4-(2-hydroxycyclohept-1-ylmethyl)phenoxy]ethyl}carbamate), we revealed that route of administration, instar of the recipient hopper, and species may alter over 1000-fold the ED₅₀ for the same JHA. Locusta migratoria migratorioides is much more susceptible to JHAs than Schistocerca gregaria. The lowest ED₅₀ found to induce adultoids and subsequent death in the ‘extra’ moult was 0·12 μg pyriproxyfen injected in olive oil to early penultimate instar hoppers of L. m. migratorioides (about 0·5 μg g^-1 fresh weight). R70-1 was more active than pyriproxyfen following the more practical topical application to early last-instar hoppers of L. m. migratorioides, 5·9 μg and 46 μg per hopper, respectively (about 10 μg g^-1 and 78 μg g^-1 fresh weight). The high susceptibility of last-instar L. m. migratorioides nymphs to topically applied R70-1 is promising from the practical standpoint. ©1997 SCI     

Insect peptide hormones: a selective review of their physiology and potential application for pest control

Our knowledge on primary structure, synthesis, release, receptor binding, structure-activity relationships, mode of action and degradation of, mainly, neuropeptides from insects has increased dramatically during the last 10 years or so. Here, five case studies are presented, which deal selectively with effects on: reproduction (trypsin modulating oostatic factor in mosquito); energy metabolism, locomotion and the immune system (adipokinetic hormones); water and ion balance, and feeding behaviour (diuretic hormones, kinins, sulfakinins); sex attraction (pheromone biosynthesis activating neuropeptide); and growth and development, and muscle activity (allatostatins). The literature is reviewed in the context of how the knowledge on neuropeptides has been and can be used for the design of novel, safe and selective compounds to control pest insects in the foreseeable future.     

Quantitative structure—activity studies of insect growth regulators. XI. Stimulation and inhibition of N-acetylglucosamine incorporation in a cultured integument system by substituted N-tert-butyl-N,N′-dibenzoylhydrazines

The ability to stimulate N-acetylglucosamine (GluNAc) incorporation in-vitro of a number of N-tert-butyl-N,N′-dibenzoylhydrazines having various substituents on both phenyl rings was measured in cultured integument excised from the rice stem borer (Chilo suppressalis Walker). The relationship between in-vitro and larvicidal potency was approximately linear. The substituent effects on variations in the potency were similar between in-vitro and larvicidal activities. An inhibitor of oxidative detoxication, piperonyl butoxide, had no synergistic effects on the in-vitro potency. The ability of some dibenzoylhydrazines to inhibit GluNAc incorporation at exposure periods longer than the optimum for stimulation was also measured in a similar cultured integument system. The relationship between the inhibitory and stimulatory potency indices was linear, indicating that the larvicidal activity of dibenzoylhydrazines is closely related to its ability to stimulate as well as to inhibit GluNAc incorporation into the larval cuticle.