一株产几丁质酶、抑真菌的侧孢芽孢杆菌

从524株芽孢杆菌中筛选出一株几丁质酶活力高的侧孢芽孢杆菌1.864菌株。研究表明该菌对小麦赤霉菌等6种病原真菌具有明显的抑制作用。通过几丁质酶抑制剂以及酶活力变化对抑制真菌活性的相关研究,初步认为该菌株的抑菌物质为几丁质酶。生物测定表明1.864的几丁质酶粗酶对蚊幼具有较高的活性,同时对Bt制剂杀虫活性具有明显的增效作用。     

新农抗天山菌素的杀虫抑菌活性

天山菌素（tianshanmysin）是从链霉菌GAAS7310 Streptomyces sp．的发酵菌丝中分离提取出来的一种活性成分。为了确定该抗生素的应用范围和应用方法，在室内测定了它对卫生害虫家蝇和田间常见的12种植物病原真菌的生物活性。结果表明，天山菌素对家蝇Muscadomestica具有很高的毒杀活性，死亡中浓度（Lc50）为0．6μg／mL；对甘薯软腐病病菌Rhizopus nigrtcans Ehrb、炭疽病病菌Colletotrichum nigrum EL．et Halst和玉米弯孢菌叶斑病病菌Curvularia lunata（Wakker）Boed3种病原真菌有较显著的抑制作用，抑制中浓度（IC50）分别为70．66、114．95和47．17μg／mL。因此GAAS7310是一株值得进一步研究的农用抗生素生产菌株，具有潜在的开发价值。     

Design,synthesis and biological activities of new strobilurin derivatives containing substituted pyrazoles

BACKGROUND: Strobilurins are one of the most important classes of agricultural fungicides. To discover new strobilurin analogues with high activity, a series of new strobilurin derivatives containing substituted pyrazoles in the side chain were synthesised and bioassayed. RESULTS: The compounds were identified by ¹H NMR, IR, MS and elemental analysis. Preliminary bioassays indicated that some title compounds exhibited excellent fungicidal activities against Pseudoperonospora cubensis (Burk. & Curt.) Rostovsev and Erysiphe graminis DC f. sp. tritici Marchal, protecting cucumber and wheat at 6.25 and 1.56 mg L^?1 respectively, and showed a moderately high acaricidal activity against Tetranychus cinnabarinus (Boisd.) at 20 mg L^?1. The relationship between structure and biological activity is discussed in terms of effects of the substituent of the pyrazole ring. CONCLUSION: The present work demonstrates that strobilurin analogues with substituted phenylpyrazolylmethoxymethyl side chains can be used as possible lead compounds for further developing novel fungicides and acaricides. Copyright © 2009 Society of Chemical Industry     

南美斑潜蝇成虫活动规律的观察

应用黄板法对南美斑潜蝇活动特性进行观测。结果表明,南美斑潜蝇在作物顶端层飞翔种群数较高,在此层面黄板诱集成虫数量最大。在干热季南美斑潜蝇的日活动高峰在８∶００～１０∶００和１８∶００～２０∶００,成虫量与日气温呈负相关。     

TLC-生物自显影检测26种植物中的抗细菌和抗氧化活性物质

我国华南地区植物资源丰富,为快速筛选和检测具有抗菌和抗氧化活性的植物资源,本研究采用甲醇冷浸提取法制备植物提取物,并采用TLC-生物自显影法快速检测其抗细菌和抗氧化活性。活性测定的结果表明,豺皮樟和桂木的抗细菌活性最强,对所有供试细菌均表现出抑制活性,且抑菌斑的最大直径均大于10 mm。红果仔、锡叶藤和山油柑也对所有供试细菌表现出抑制活性,但其活性弱于豺皮樟和桂木。粪箕笃、海金沙和小蜡未表现出任何抗细菌活性,其他供试植物对部分供试细菌表现出抑制活性。白花酸藤子、海南杜英、黄牛木、山油柑和基及树表现出较好的抗氧化活性,抗氧化斑的R_f值范围为0.0～1.0,说明具有较多的活性化合物。TLC-生物自显影法能够快速、有效地筛选和检测具有抗细菌和抗氧化活性的植物提取物,本研究结果为植物资源的开发和利用提供重要的理论依据。     

海洋真菌次级代谢产物在植物保护中的研究与应用

病虫害严重影响我国农业生产，每年造成巨额经济损失，传统化学农药虽然在一定程度上能够减轻这些危害，但其不合理的使用也造成严重的负面影响，亟需开发新型生物农药。海洋真菌生存于独特的海洋环境中，形成了有别于陆生真菌的生存繁殖方式和遗传代谢机制，能够产生许多结构新颖、生物活性显著的次级代谢产物，其中许多化合物具有抗植物病原菌、杀虫和抗病毒等农用生物活性，具有开发成为新型生物农药的巨大潜力。本文综述了2010年以来前人在海洋真菌次级代谢产物农用生物活性方面的研究成果，涵盖了90个化合物，结构类型主要包括聚酮类、萜类、生物碱类和甾体类化合物等，以期为生物农药的开发提供依据。     

新化合物天维菌素的杀虫杀螨活性

为明确天维菌素(tenvermectin)的杀虫杀螨活性,分别测定了其对小菜蛾Plutellaxylostella (药膜法)、粘虫Mythimna separate Walker (小叶碟添加法)、棉铃虫Helicoverpaarmigera Hübner (饲料混药法)、松材线虫Bursaphelenchus xylophilus (浸渍法)和朱砂叶螨Tetranychus cinnabarinus (叶片浸渍法和玻片浸渍法)的室内毒力,并采用叶碟喷雾法测定了其对朱砂叶螨的盆栽药效。结果表明:天维菌素对鳞翅目害虫小菜蛾、粘虫和棉铃虫的LC50值分别为22.21、19.66和22.09 mg/L,对松材线虫的LC50值为1.94 mg/L,毒力显著高于米尔贝霉素(P50值分别为0.0051和0.0089 mg/L。盆栽试验结果表明:0.2 mg/L的天维菌素药后5 d对朱砂叶螨的防效最高,达97.42%;药后7 d,尽管天维菌素与阿维菌素的防治效果均有所下降,但天维菌素不同浓度(0.0125~0.2 mg/L)处理防效仍保持在80.23%~91.96%之间。研究表明,天维菌素对供试的有害生物均具有较高活性,具有研究开发潜力。     

抑菌霉素A17对12种病原真菌及3种害虫的生物活性

从稀有放线菌7310菌株的发酵菌丝中经溶媒萃取和硅胶柱层析初步分离出来一种活性成分，经结构鉴定为新结构化合物——抑茵霉素A17。抑茵霉素A17杀虫活性结果表明，对家蝇具有很强的杀虫活性，其LC50值仅为1．56μg／ml，并能在较短的时间内击倒供试虫体；对菜粉蝶和小菜蛾幼虫也具有较强的杀虫活性，LC50值分别为106．27和172．9μg／ml。以常见的12种病原真菌作为供试菌，在室内进行了抑菌霉素A17抑菌活性的定性及定量分析，结果表明抑菌霉素A17硅胶层析粗提物对12种供试真菌中的甘薯软腐病病菌、柑桔酸腐病病菌、桃黑星病病菌、番茄早疫病病菌、番茄芽枝病病菌、莴苣菌核病病菌、荔枝霜霉病病菌、炭疽菌、弯孢霉、拟茎点霉和果腐葡萄孢的菌丝生长有明显的抑制作用，其中对拟茎点霉的活性最强，抑制中浓度仅为0．1μg／ml。     

含酰腙结构的新型吡唑酰胺衍生物对小菜蛾的生物活性

采用浸虫法、夹毒叶片法和叶碟法分别测定了13个含酰腙结构的新型吡唑酰胺衍生物对小菜蛾3龄幼虫的触杀、胃毒和拒食活性。结果表明:该类化合物对小菜蛾3龄幼虫具有较高的胃毒和拒食活性,其中苯环上含有氯原子、且酰腙一端的取代基含有杂原子且体积较小的化合物 H7的胃毒和拒食活性最好,明显高于对照药剂毒死蜱。H7 72 h胃毒作用LC50值为0.6 mg/L(毒死蜱的LC50值为7.4 mg/L);有10个化合物的拒食活性高于毒死蜱,其中 H7 48 h的拒食中浓度(AFC50) 最低,为0.6 mg/L,明显低于毒死蜱(AFC50=6.5 mg/L)。供试化合物对小菜蛾3龄幼虫均无触杀活性。     

In vitro antimicrobial and in vivo antioomycete activities of the novel antibiotic thiobutacin

BACKGROUND: A number of synthetic fungicides are not effective when confronted by oomycete pathogens because many fungicide targets are absent from oomycetes. Moreover, resistance to fungicides has already arisen in oomycete species, and thus development of new, effective and safe compounds for use in oomycete disease control is necessary.RESULTS: Zoospore lysis began at 10 microg mL(-1) of thiobutacin, and most of the zoospores were collapsed at 50 microg mL(-1). Thiobutacin also revealed inhibitory activity against the cyst germination and hyphal growth of Phytophthora capsici at 50 microg mL(-1). Treatment with thiobutacin exhibited protective activity against development of Phytophthora disease on pepper plants.CONCLUSION: The authors verified in vitro antioomycete activity of thiobutacin against P. capsici and its control efficacy against Phytophthora blight in vivo. This is the first report to demonstrate in vivo antioomycete activity of the novel antibiotic thiobutacin against P. capsici infection.     

米尔贝霉素类似物的合成及杀螨杀蚜活性

为寻找高活性的米尔贝霉素衍生物,以伊维菌素为原料,经脱糖、羟基保护、氧化、还原胺化、脱保护等将其转变为13-氨基米尔贝霉素类似物,通过三组分反应设计合成了一系列米尔贝霉素磺酰脒类化合物(7a~7i),并初步测定了其对朱砂叶螨Tetranychus cinnabarinus和豆蚜Aphis craccivora的室内活性。结果表明:各衍生物对朱砂叶螨和豆蚜均有较好的触杀活性,其中7f、7h和7i对朱砂叶螨24 h的LC50值分别为1.04×10–2、9.60×10–4和1.44×10–2 mg/L;7i对豆蚜24 h的LC50值为7.81 mg/L。米尔贝霉素13位氨基上磺酰化的结构修饰有助于提高米尔贝霉素类化合物的杀螨、杀蚜活性。     

Structural effects of dinotefuran and analogues in insecticidal and neural activities

The insecticidal potencies of dinotefuran and analogues against the adult male American cockroach, Periplaneta americana (L) were measured by injection with or without metabolic inhibitors. The potency of dinotefuran was close to those of clothianidin and imidacloprid under the conditions used. The nerve-excitatory and nerve-blocking activities were measured with central nerve cords of P americana. The nerve-excitatory activity of dinotefuran was lower than that of imidacloprid, but was comparable with that of clothianidin. The nerve-blocking activity of dinotefuran was comparable with that of imidacloprid and slightly higher than that of clothianidin. Quantitative analyses showed that variations in the insecticidal activity were better correlated with variations in the nerve-blocking activity than with those in the nerve-excitatory activity when the contribution of the hydrophobic factor was allowed for.     

10种N-取代氨基香豆素的合成及生物活性

基于结构拼接思想,设计合成了10个N-取代氨基香豆素类化合物,并测定了其抑菌及除草活性。6-硝基香豆素经Fe/NH4Cl还原得6-氨基香豆素,再与不同醛缩合得Schiff碱,最后经硼氢化钠还原制得10个N-取代氨基香豆素类化合物(4a~4J),其中9个未见文献报道,其结构均经红外光谱、核磁共振氢谱和质谱确认。抑菌活性测试结果表明,所有化合物对苹果腐烂病菌Valsa mali、葡萄白腐病菌Coniothyrium diplodiella、棉花枯萎病菌Fusarium oxysporium和柑橘炭疽病菌Citrusanthrax bacteria均有一定抑制作用,其中 4e 的抑菌活性最强,对苹果腐烂病菌和柑橘炭疽病菌的EC50值分别为7.53和12.93 mg/L,对其余2种植物病原菌的EC50值均小于25 mg/L;化合物 4f 次之,对苹果腐烂病菌和葡萄白腐病菌的EC50值均约为11 mg/L。除草活性测试结果表明,除 4f 外,所有目标化合物均有一定除草作用,其中 4c 的活性最强,100 mg/L下对反枝苋Amaranthus retroflexus种子根、茎生长的抑制率均为99%。     

2-酰氨基苯并噻唑-7-甲酸甲酯类化合物的合成及其抗病诱导活性

以3-氨基苯甲酸为原料,经酯化、关环、酰基化等反应合成了22个未见文献报道的2-酰氨基苯并噻唑-7-甲酸甲酯类化合物,其结构经过IR、1H NMR和元素分析确认。初步的生物活性测定结果表明:在1 000mg/L浓度下,部分化合物对黄瓜灰霉病菌Botrytis cinerea具有一定的离体抑制活性,抑制率为60%~73%;化合物Ⅲ-4、Ⅲ-13、Ⅲ-19、Ⅲ-20的活体抑菌活性(抑制率)分别为83.0%、65.0%、88.9%和74.8%,均高于相应的离体活性,表现出一定的抗病诱导活性。     

Design, synthesis and antifungal/insecticidal evaluation of novel nicotinamide derivatives

A series of nicotinamide derivatives based on Boscalid were prepared and tested for their activities against seven plant pathogenic fungi and two insects. The preliminary bioassays indicated that almost all of the synthesized target compounds displayed the antifungal activities and some of them also had certain insecticidal activities. And, compound 12 showed the strongest activity of all against Rhizoctonia solani (EC₅₀ = 0.010 mg L⁻¹) and Sphaceloma ampelimum (EC₅₀ = 0.040 mg L⁻¹), even stronger than Boscalid, a new nicotinamide fungicide. Additionally, both compounds 1 and 2 showed strong activities against Plutella xylostella (90% and 80%, respectively, at 1000 mg L⁻¹).     

具有农业生物活性壳寡糖的研究进展

壳寡糖是一类由N-乙酰氨基葡萄糖或氨基葡萄糖通过β-(1,4)-糖苷键连接起来的低聚合度水溶性的糖类,在食品、医药、化妆品等方面具有广泛用途。主要评述了壳寡糖在植物生长调节(诱导抗性)、杀菌作用以及杀虫活性方面的应用,表明壳寡糖是一种对环境友好的、良好的生物源农药。     

来自大兴安岭凋落物的绿僵菌及其相近菌属真菌的生物活性

为研究绿僵菌Metarhizium及其相近菌属真菌的生物活性,采用形态学和分子生物学的方法对来自大兴安岭凋落物的肉色基思菌Keithomyces carneus（曾用名：肉色绿僵菌M.carneum）与马氏马昆德菌Marquandomyces marquandii（曾用名马昆德绿僵菌M. marquandii）以及金龟子绿僵菌Metarhizium anisopliae进行了鉴定,并分析了它们对3种害虫、4种植物病原菌的活性。杀虫活性测定表明,肉色基思菌与马氏马昆德菌对双斑萤叶甲Monolepta hieroglyphica、玉米蚜Rhopalosiphum maidis、绿豆象Callosobruchus chinensis具有侵染能力,为非寄主专化型真菌。抑菌活性测定表明,肉色基思菌对立枯丝核菌Rhizoctonia solani,水稻白叶枯病菌Xanthomonas oryzae pv. oryzae等病原菌具有抑菌活性。本研究揭示了3种供试真菌具有防治双斑萤叶甲的潜力,也发现了肉色基思菌与马氏马昆德菌的生防潜力,为它们进一步开发利用打下了基础。