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。     

大环内酯类新化合物天维菌素杀螨活性及田间防治效果

为明确新化合物天维菌素的杀螨活性,采用叶碟喷雾法测定了在室内天维菌素对朱砂叶螨Tetranychus cinnabarinus、柑橘红蜘蛛Panonychus citri及二斑叶螨Tetranychus urticae的毒力,并研究了其制剂对螨类害虫的田间防治效果。结果表明,天维菌素对朱砂叶螨若螨和雌成螨均具有较高的毒力,其LC50分别为0.011、0.11 mg(a.i.)/L,杀螨活性优于弥拜霉素、阿维菌素,但杀卵活性较差。田间试验中2%天维菌素微乳剂具有良好的速效性且具有一定的持效期,在有效成分8~40 mg/kg剂量下,对朱砂叶螨和二斑叶螨药剂处理14 d的防治效果分别为83.22%~92.77%和85.49%~92.64%,有效控制期在14 d以上;在有效成分75 mg/kg剂量下,对柑橘红蜘蛛防治效果最好,处理1、3、7、14 d的防治效果分别达96.53%、97.72%、98.05%和91.42%。表明天维菌素具有作为杀螨剂的潜力。     

秦岭链霉菌发酵液中杀虫活性成分分离及结构鉴定

采用大孔树脂层析、硅胶柱层析以及制备高效液相色谱等技术对具有抑菌和杀虫活性的秦岭链霉菌发酵液中的杀虫活性成分进行了分离纯化,得到3个杀虫活性化合物,经高分辨质谱和核磁共振波谱技术分别鉴定为阿维菌素B1a、B2a和A1a。研究发现,同一菌株发酵液中可以同时产生杀虫和杀菌两类成分,与阿维链霉菌Streptomyces avermectinius亲缘关系差异很大的链霉菌也可以产生阿维菌素成分。     

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。     

Insecticidal toxins from the bacterium Photorhabdus luminescens: gene cloning and toxin histopathology

Four toxin complexes, Tca, Tcb, Tcc and Tcd from the culture broth of Photorhabdus luminescens have been purified and the four toxin complex encoding loci, tca, tcb, tcc and tcd, cloned. Genetic knockout of either tca or tcd reduced oral toxicity to Manduca sexta, and knockout of both loci eliminated activity. Purified Tca specifically affected the insect midgut, despite its putative normal delivery directly into the insect haemocel. These Photorhabdus toxins may form useful alternatives to other orally active bacterial protein toxins such as those from Bacillus thuringiensis.     

苦楝内生真菌及其代谢产物的杀虫活性

在对290株苦楝内生真菌分离纯化鉴定的基础上,研究了30株具有代表性的内生真菌及其代谢产物的杀虫活性。结果表明其中5个菌株对马尾松毛虫5d校正死亡率大于60%,杀虫活性最强的KL042菌株经鉴定为球孢白僵菌。球孢白僵菌作为内生真菌,在国内尚未见报道。进一步选取杀虫活性较强的9株内生真菌,研究其代谢产物的胃毒和触杀活性,结果表明拟青霉KL017菌株发酵液10倍浓缩液对柳蓝叶甲胃毒活性最强,48h校正死亡率达90.09%。球孢白僵菌KL042、拟青霉KL017和交链孢KL062发酵液10倍浓缩液点滴马尾松毛虫前胸背板后,48h校正死亡率分别为76.67%、56.67%和53.33%。     

0.05%氟虫腈杀蚁饵剂对红火蚁的传毒活性测定

应用联杯法等室内测定了0.05%氟虫腈杀蚁饵剂对红火蚁的引诱力、毒杀速度及其传导毒杀活性.结果表明,供试饵剂对红火蚁的引诱性、毒杀速度显著优于正舒(对照药剂).红火蚁觅食到供试饵剂的初始时间为2.00 min,与正舒的2.33 min达显著差异;供试饵剂处理后24 h的工蚁死亡率为80.65%,显著高于对照饵剂的50.15%;72 h的工蚁死亡率即达到100%.联杯法测定结果表明,0.05%氟虫腈杀蚁饵剂能通过工蚁的取食和交哺行为进行传导.供试饵剂受药杯中工蚁、幼蚁和蚁后3 d后死亡率均达到100%,显著高于对照饵剂.0.05%氟虫腈杀蚁饵剂引诱性强、对红火蚁具有高胃毒、高传导毒杀活性,可适用于防控入侵红火蚁.     

蒌蒿精油的杀虫活性与化学成分研究

生物测定结果表明，蒌蒿（Artemisia selengensis）精油对菜青虫具有较强的拒食和胃毒作用，而触杀作用较弱，无熏蒸作用。应用GC／MS／DS鉴定了精油化学成分主要为桉叶油素（37．76％）、龙脑（15．87％）、樟脑（12．34％）、金合欢烯（10．50％）和香草醛（7．12％）。     

Acaricidal activity of triketone analogues derived from Leptospermum scoparium oil against house‐dust and stored‐food mites

BACKGROUND: Various attempts to control the populations of house‐dust and stored‐food mites have been implemented using synthetic chemicals. Although effective, the repeated use of these chemicals has led to resistance owing to the mite's high reproductive potential and short life cycle. Therefore, this study aimed to develop natural acaricides using oils derived from Leptospermum scoparium JR & G Forst., which may affect the overall biological activity of a mite without adverse effects. Results were compared with those from using benzyl benzoate and N,N‐diethyl‐3‐methylbenzamide (DEET). RESULTS: The LD₅₀ values of L. scoparium oil were 0.54, 0.67 and 1.12 µg cm^?2 against Dermatophagoides farinae (Hughes), D. pteronyssinus (Troussart) and Tyrophagus putrescentiae (Schrank) respectively. The active constituent isolated from L. scoparium was identified as leptospermone (6‐isovaleryl‐2,2,4,4‐tetramethyl‐1,3,5‐cyclohexanetrione) by spectroscopic analysis. Based on the LD₅₀ values of leptospermone and its derivatives, the most toxic compound against D. farinae was leptospermone (0.07 µg cm^?2), followed by 2,2,4,4,6,6‐hexamethyl‐1,3,5‐cyclohexanetrione (1.21 µg cm^?2), benzyl benzoate (10.03 µg cm^?2) and DEET (37.12 µg cm^?2). Furthermore, similar results were observed when the leptospermone and its derivatives were tested against D. pteronyssinus and T. putrescentiae. CONCLUSIONS: These results indicate that L. scoparium oil‐derived materials, particularly leptospermone and 2,2,4,4,6,6‐hexamethyl‐1,3,5‐cyclohexanetrione, have potential for development as new agents for the control of three species of mite. Copyright © 2008 Society of Chemical Industry     

Insecticidal activity of daphnane diterpenes from Lasiosiphon kraussianus (Meisn) (Thymelaeaceae) roots

A methanol extract of roots of Lasiosiphon kraussianus (Meisn) (Thymelaeaceae) showed potent insecticidal activity against Aphis gossypii (Glov) and Drosophila melanogaster (Meig). Bioassay-driven fractionation of this extract led to the isolation and characterisation of two known daphnane diterpenoids: Excoecaria toxin (1) and wikstrotoxin D (2) . The two natural products were inferior to methomyl in activity against A gossypii and Myzus persicae (Sulz) in contact assays but were superior in ingestion assays against D melanogaster. This is the first report on insecticidal activities of compounds 1 and 2 . AChE was insensitive to the two natural products. © 1999 Society of Chemical Industry     

含香豆素基团的二氯丙烯类衍生物的合成及杀虫活性

以丙二酸二乙酯、间苯二酚和1,1,3-三氯丙烯等为原料,经取代、环合、缩合等反应合成了9个含有香豆素基团的二氯丙烯类衍生物,化合物结构经IR、 1H NMR、 MS及元素分析确证。初步的生物活性测定结果表明,该类化合物在400 mg/L质量浓度下对小菜蛾Plutella xylostella有较好的杀虫活性,其中化合物 5e 对小菜蛾的致死率达到93%。     

洱源丛枝瑚杀虫活性成分研究

洱源丛枝瑚(Ramaria eryuanensis)石油醚萃取物经过柱层析得到单体化合物B8,该化合物对小菜蛾3龄幼虫72 h的LC50为3.375 7 mg/mL。经FAB-MS、1HNMR、13CNMR及DEPT等波谱鉴定,并与文献值对照,确定其为麦角甾-7,22-二烯-3β,5α,6β-三醇。     

椰子织蛾幼虫致病Bt菌的鉴定与杀虫活性测定

从海南省五指山采集的椰子织蛾僵虫上分离得到一株对椰子织蛾幼虫具有毒杀作用的菌株WZS171并对其生物防治潜力进行评测。通过形态学、cry基因的鉴定明确了该菌株为苏云金芽胞杆菌(Bt)。基因鉴定结果表明该菌株含有cry1Aa13、cry1Gb1、cry1D、cry1Ia、cry2Af共5种新型cry基因,NCBI Blast与GenBank中已知基因序列最大相似性分别为98%、99%、90%、92%、99%;生测结果表明72 h后该菌株菌悬液对椰子织蛾幼虫的LC₅₀为9.08 μg/mL,95%置信区间6.72~12.26 μg/mL。该菌株含有5种新型的杀虫编码基因,并且对椰子织蛾幼虫具有较高毒力,生物防治潜力大。     

藜不同溶剂提取物的杀蚜活性

以萝卜蚜为试虫,对4种不同溶剂藜提取物的杀蚜活性进行了研究。结果表明,石油醚和乙醇提取物的杀虫活性最为显著,对萝卜蚜有很强的触杀和拒食作用,石油醚提取物72 h的平均拒食率为73.33%,拒食中浓度AFC_(50)为61.731 mg/mL,触杀校正死亡率为97.69%,LC_(50)为22.431 mg/mL;乙醇提取物72 h的触杀校正死亡率为93.82%,LC_(50)为34.698 mg/mL,与对照组具有显著差异。此外,藜其他溶剂提取物也表现出一定的杀蚜活性。     

海南瓜实蝇致病细菌的分离鉴定及杀虫活性测定

从海南自然感病死亡的瓜实蝇上分离到1株对瓜实蝇高毒力的致病性菌株BC-hn,对其生防潜能进行评估.通过形态学观察、生理生化测定和16S rDNA序列测定分析,确定菌株BC-hn为黏质沙雷氏菌Serratia marcescens;用1×108 cfu/mL的菌悬液接种瓜实蝇进行室内杀虫活性测定,研究结果表明接种7d后成虫的平均死亡率为81.2％;卵孵化抑制率为37.5％,幼虫平均死亡率为53.0％,对蛹羽化的抑制作用最小,平均死亡率24.0％.用浓度为1×104～1×108菌悬液处理瓜实蝇成虫,7d后的LC50为1.16×106 cfu/mL.对其他昆虫致病性测定发现,菌株BC-hn对菜蚜也有较高的致死作用,接种7d后的死亡率为60.0％,但对供试的斜纹夜蛾、菜青虫、玉米螟和黄粉虫的死亡率均低于10.0％.菌株BC-hn对瓜实蝇成虫的毒力高,并对昆虫具有一定的专化性,具有较高的防治潜力.     

新的吡啶杂环硫代磷酸酯类化合物的合成及杀虫活性

为了寻找高活性的新化合物,通过相转移催化反应,在二氯甲烷/水体系中合成了一系列新的吡啶杂环硫代磷酸酯类化合物,其结构均经1H NMR、13C NMR、31P NMR、IR和MS的表征,并通过元素分析确证。室内生物活性测试结果表明,部分化合物表现出较好的杀虫活性,其中化合物 3a 对苜蓿蚜Aphis medicaginis Koch和化合物 3c 对东方粘虫Mythimna separate的 LC50值分别为 1.64和 0.73 mg/L,与对照药剂毒死蜱的活性相当。     

天维菌素酰化衍生物的合成及杀虫杀螨活性

以天维菌素B、天维菌素B单糖苷和天维菌素B苷元为原料,经选择性C-5羟基保护,在C-13、C-4′和C-4″位引入不同酰基基团,合成了3个系列共23个天维菌素B酰化衍生物,并通过1H NMR、13C NMR和高分辨质谱对所有目标化合物的结构进行了表征。生物活性测定结果表明,所有衍生物对小菜蛾Plutella xylostella、朱砂叶螨Tetranychus cinnabarinus以及松材线虫Bursaphelenchus xylophilus均表现出不同程度的毒杀活性,其中天维菌素B C-4″位衍生物的活性优于C-4′位衍生物及13位衍生物。化合物8e对小菜蛾和松材线虫的毒杀活性最优,LC50值分别为9.2 mg/L和0.42 mg/L,化合物8b对朱砂叶螨的毒性最高,LC50值为0.0019 mg/L,均优于对照药天维菌素B。     

Acaricidal activities of Santolina africana and Hertia cheirifolia essential oils against the two-spotted spider mite (Tetranychus urticae)

BACKGROUND: Many plant essential oils show a broad spectrum of activity against pests. This study investigated the effects of two essential oils on Tetranychus urticae, one of the most serious pests in the world. RESULTS: The chemical composition of the two oils was characterised by GC‐MS. The most abundant component in the Santolina africana (Jord. & Fourr) oil was terpinen‐4‐ol (54.96%), while thymol (61%) was prevalent in the Hertia cheirifolia (L.) oil. Mortality and fecundity were measured upon treatment with oil concentrations ranging from 0.07 to 6.75 mg L^?1 with a Potter spray tower. Mite mortality increased with oil concentration, with LC₅₀ values of 2.35 mg L^?1 for S. africana and 3.43 mg L^?1 for H. cheirifolia respectively. For both oils, a reduction in fecundity was observed at concentrations of 0.07, 0.09 and 0.29 mg L^?1. Artificial blends of constituents of oils were also prepared and tested with individual constituents missing from the mixture. The results showed that the presence of all constituents was necessary to equal the toxicity of the two natural oils. CONCLUSION: S. africana and H. cheirifolia oils can provide valuable acaricide activity with significantly lower LC₅₀ values. Thus, these oils cause important mortality and reduce the number of eggs laid by females. Copyright © 2012 Society of Chemical Industry     

Insecticidal activity of chemical constituents from Aristolochia pubescens against Anticarsia gemmatalis larvae

Acetone and ethanol extracts of the tubercula and several compounds isolated from Aristolochia pubescens (Willd) were bioassayed on velvetbean caterpillars, Anticarsia gemmatalis (Hübner), for evaluation of the insecticidal activities. Of the extracts subjected to bioassay, the acetone extract showed the highest activity. (-)-Cubebin did not show activity against soybean caterpillars, whereas aristolochic acid and ent-kaur-15-en-17-ol increased the larval period. These compounds, and (+)-eudesmin and (+)-sesamin, reduced the viability of this period, giving rise to malformed adults. These extracts and compounds are therefore potential botanical insecticide agents for the control of velvetbean caterpillars in soybean crops.     

Insecticidal Activity and HPLC Correlation of Thuringiensin from Fermentation and Two-phase Aqueous Separation Processes

Thuringiensin produced by Bacillus thuringiensis subsp. darmstadiensis was further subjected to a two-phase aqueous separation system. A modified HPLC method and a test for quantitative pathogenicity using the house fly Musca domestica were used for analysis of thuringiensin. Within a realistic range of dosages, more effect was observed in the pupal stage than in the larval stage. The percentage effective control rate (ECR) was calculated by (100-percentage emergence); malformed and non-reproductive adults were considered as emerged. Pupal mortality, pupal weight, and ECR after feeding the three-day-old larvae were the measured response criteria for bioassay. The EC₅₀ of thuringiensin for pupae mortality was 1·64 μg ml^-1 diet, and 0·83 μg ml^-1 for mortality of adults. Insecticidal activity of the broth increased with fermentation time-course from 9th to 21st hour. The bioassay curve constructed with three-hour sampling interval during the fermentation course had good correlation to thuringiensin content as determined by the HPLC method. In the two-phase aqueous separation system, a maximum of 96·7% ECR was achieved with the bottom salt layer, compared to a value of 46·7% with the upper PEG layer. These results suggest that thuringiensin, prepared through a fermentation and recovery process, is suitable for pest control. © 1997 SCI.