Novel and selective acetylcholinesterase inhibitors for Tetranychus cinnabarinus (Acari: Tetranychidae)

The carmine spider mite, Tetranychus cinnabarinus (Acari: Tetranychidae), is an economically important and extremely polyphagous herbivorous pest, with the title of “resistance champion” among arthropods. Anticholinesterase insecticides such as organophosphate and carbamate account for more than one-third of global insecticide sales. The non-target toxicity and resistance problem of organophosphate and carbamate have become of growing concern, which may be due to the fact that they target the ubiquitous catalytic serine residue of acetylcholinesterase (AChE) in mammals, birds, and beneficial insects. In this study, the structural differences between T. cinnabarinus AChE and human AChE, at or near the catalytic pocket, were illustrated. From the SPECS chemical lead-compound database, 55 AChE inhibitor candidates were screened for high affinity for T. cinnabarinus AChE, but low affinity for human AChE, using the DOCK 6 and AutoDock Vina software. Three of the fifty-five candidates had inhibitory activity greater than that of the reversible AChE inhibitor eserine, with no observed inhibitory activities against human AChE. Two of the three had toxicity to T. cinnabarinus comparable to that of natural insecticidal pyrethrins. However, their potency is low compared with that of etoxazole, and further work is needed to optimize their potency. The selectivity of the three compounds over human and mite AChE may be due to their interaction with the mite-specific residues, as analyzed by Cyscore. The three compounds are potential lead compounds for development of novel acaricides against T. cinnabarinus with reduced toxicity to non-target species and a low propensity for resistance.     

Insecticide susceptibility status of Aedes aegypti (Diptera: Culicidae) from Townsville

Insecticide susceptibility of a 1995 Townsville Aedes aegypti (L.) population was investigated in the laboratory according to World Health Organization guidelines. Using baseline data from two Townsville populations (1955 and 1989), larval bioassays detected significant increases in susceptibility to synthetic pyrethroids and malathion, and significant reductions in susceptibility to most organophosphates and propoxur. Adult bioassays detected significant resistance to bendiocarb and DDT. Comparison of larval data with the international reference ROCK strain showed substantial resistance to have developed to malathion and fenthion. Further analysis revealed the presence of distinct substrains in the baseline 1989 population, which displayed varying levels of temephos susceptibility. We concluded that susceptibility investigations should assess mosquito populations collected from many sites within an area rather than taking a single population from one site, and that the 1989 Ae. aegypti colony would be unsuitable for use as a susceptible reference population.     

A nano-delivery system expands the insecticidal target of thiamethoxam to include a devastating pest,the fall armyworm

Nano-delivery systems have been applied to deliver various synthetic/botanical pesticides to increase the efficiency of pesticide use and reduce the volumes of pesticides applied. Previous studies have supported the hypothesis that the nanocarriers can help expand the insecticidal target of pesticides to include non-target pests. However, the potential mechanism underlying this interesting phenomenon remains unclear. Herein, a widely applied star polycation (SPc) nanocarrier was synthesized to construct a thiamethoxam (TMX) nano-delivery system. The SPc-based delivery system could promote the translocation of exogenous substances across the membrane of Sf9 cells, increase the cytotoxicity of TMX against Sf9 cells by nearly 20%, and expand the insecticidal target of TMX to include Spodoptera frugiperda (the fall armyworm), with a 27.5% mortality increase at a concentration of 0.25 mg/mL. Moreover, the RNA-seq analysis demonstrated that the SPc could upregulate various transport-related genes, such as Rab, SORT1, CYTH, and PIKfyve, for the enhanced cellular uptake of TMX. Furthermore, enhanced cell death in larvae treated with the TMX–SPc complex was observed through changes in the expression levels of death-related genes, such as Casp7, BIRC5, MSK1, and PGAM5. The SPc-based nano-delivery system improved the cellular uptake of TMX and expanded its insecticidal target by adjusting the expression levels of death-related genes. The current study mainly identified the transport and cell death genes related to nanocarrier-based insecticidal target expansion, which is beneficial for understanding the bioactivity enhancement of the nano-delivery system.     

Initial verification of the resistance management strategy for Frankliniella occidentalis (Pergande) (Thysanoptera: Thripidae) in Australia

Shortly after the initial detection of western flower thrips (WFT), Frankiniella occidentalis (Pergande), in Australia during 1993 a resistance management strategy based on the alternation of chemical groups was implemented. This study aimed to verify this strategy by field testing α-cypermethrin against WFT with and without chemical alternation. Up to 114 times α-cypermethrin resistance (at LC50) was detected and resistance increased with and without chemical alternation; however, chemical alternation did significantly reduce numbers of thrips compared with a nonalternation strategy. Resistance has the potential to undermine the sustainable use of those chemicals to which there is no current detectable resistance. Consequently, chemicals with a high frequency and level of resistance against WFT need to be identified through monitoring and quickly eliminated from WFT chemical control recommendations.     

Integration of entomopathogenic fungi and eco-friendly insecticides for management of red palm weevil,Rhynchophorus ferrugineus (Olivier)

Red palm weevil (Rhynchophorus ferrugineus) is a voracious pest of date palm worldwide. Pakistan ranks sixth in date palm production globally. Losses to date palm plantations in Pakistan sometimes surpass 10%-20%. Most of the traditional management strategies used by farmers have been found insignificant to combat this voracious pest. The entomopathogenic fungi, Beauveria bassiana [QA-3(L) and QA-3(H)] and insecticides, Nitenpyram (Active 10% SL) [NIT (L) and NIT (H)] were applied to larval (2nd, 4th, and 6th), pupal and adult stages of R. ferrugienus. Integration or alone application of fungi with insecticides at different concentration under laboratory conditions. Combined application was depicted additive and synergistic interactions. Contrarily, highest cumulative mortality (100%) was recorded in 2nd instar larvae as compared to later instar larvae at combined application. The maximum pupal and adult mortality remained 89% and 66% respectively after treatment with [QA-3 (H) + NIT (L)]. The combination of B. bassiana at higher concentration whereas Nitenpyram at lower dose was found more lethal to larvae, pupae and adults of R. ferrugineus. This signifies the need of combining B. bassiana and bio-rational insecticides that can reduce the cost of management with least harm to environment and natural enemies.     

Chemical constituents from the bark of Juglans mandshurica Maxim. and their phenol oxidase inhibitory effects

Botanical insecticides investigation led to 21 compounds from the bark of Juglans mandshurica Maxim., in which, compounds 4, 10, 11, 13, 14 and 15 were isolated from Juglans genus for the first time. The inhibitory effect of dihydrokaempferol (6), naringenin (7) and rhoiptelol C (18) on phenol oxidase (PO) are 5–10 times more than arbutin, a well-known tyrosinase inhibitor. Thus, the selective and effective these inhibitors can be expected for using in the development of environment-friendly pesticide.     

几类杀虫剂对灰飞虱的相对毒力及田间种群的抗药性现状

采用浸苗法测定了6类11种杀虫剂对灰飞虱Laodelphax striatellus (Fallén)3龄若虫的毒力,并分析比较了江苏句容、通州、楚州、大丰、南京和苏州以及安徽庐江等7地灰飞虱种群对10种杀虫剂的抗药性水平。对云南种群而言,在所测杀虫剂中,以乙酰甲胺磷为标准药剂,氟虫腈的相对毒力最高;噻嗪酮、阿维菌素和噻虫嗪次之;高效氯氰菊酯、IPP（硝基亚甲基类化合物）、毒死蜱、敌敌畏和三唑磷间毒力处于同一数量级,低于阿维菌素等杀虫剂;吡虫啉的相对毒力最低。与云南种群相比,2007年采自苏、皖7个不同地区的灰飞虱种群对噻嗪酮产生了极高水平的抗性,其抗性倍数均超过200倍;对高效氯氰菊酯产生了中高水平的抗性,其抗性倍数为7.8～108.8;安徽庐江灰飞虱种群对三唑磷产生了7.7倍的抗性,对毒死蜱产生了12.0倍的抗性,江苏楚州、南京、大丰和句容灰飞虱种群对毒死蜱产生了5.7～12.6倍的抗性; 所有灰飞虱种群对敌敌畏仍然敏感,对氟虫腈、阿维菌素和新烟碱类杀虫剂吡虫啉、噻虫嗪和IPP等也比较敏感。     

两种寄生蜂对几种农药的敏感性测定

就平腹小蜂、荔枝蒂蛀蛾白茧蜂对几种常用农药的敏感性进行了测定.结果表明：生物性农药的印楝素、定虫隆、灭幼脲对2种寄生蜂均较安全;Bt对平腹小蜂的毒性较小;杀虫双对平腹小蜂的影响较小,但对蒂蛀蛾白茧蜂有较高毒性（2 h内死亡率70%）;拟除虫菊酯类农药对平腹小蜂有一定的毒性,而对蒂蛀蛾白茧蜂有很高的毒性（2 h内死亡率均为100%）;2种寄生蜂均对有机磷杀虫剂如敌百虫、辛硫磷、敌敌畏及氧乐果等极度敏感.表明蒂蛀蛾白茧蜂比平腹小蜂对化学杀虫剂更敏感.因此在综合防治中,尤其是当田间释放平腹小蜂时应合理选择使用杀虫剂,应以生物源性农药为首选,避免使用菊酯类农药,尤其要禁止使用有机磷类农药,以减少对平腹小蜂等寄生性天敌的杀伤.     

毛鱼藤酮与鱼藤酮杀虫活性的比较

毛鱼藤酮是从杀虫植物毛鱼藤根中分离的杀虫活性物质。以菜粉蝶、甘蓝蚜、柑桔全爪螨、小菜蛾和黄曲条跳甲为试虫比较测定了毛鱼藤酮与鱼藤酮的毒杀、拒食、生长发育干扰和忌避产卵活性。结果表明：毛鱼藤酮的杀虫活性依昆虫种类而异,对柑桔全爪螨、小菜蛾、黄曲条跳甲的活性与鱼藤酮相当,其LC₅₀没有显著差异,而对甘蓝蚜和菜粉蝶的活性显著低于鱼藤酮。毛鱼藤酮和鱼藤酮对昆虫均具拒食活性,但前者比后者弱。毛鱼藤酮还与鱼藤酮一样对昆虫有一定的生长发育干扰和忌避产卵作用。NADH 泛醌氧化还原酶抑制活性测定结果显示,毛鱼藤酮的抑制活性低于鱼藤酮,二者抑制中浓度（IC₅₀）分别为5.27 nmol·mL^-１和2.58 nmol·mL^-１。根据拒食、受药途径和酶抑制的试验结果分析认为,毛鱼藤酮在浸叶处理时对某些昆虫有较高杀虫活性是由于其比鱼藤酮有较低的拒食活性,导致虫体摄入药剂量增加所致。     

Effects of insecticides on life history parameters of the aphid parasitoidAphidius rhopalosiphi [Hym.: Aphidiidae]

The effects of four insecticides (two organophosphates, a pyrethroid and a carbamate), applied at different dosages, on different life history parameters of the aphid parasitoidAphidius rhopalosiphi (De Stefani-Perez) were tested. The methods used simulated field conditions in the laboratory. After application on the mummies, only two treatments (parathion and the high dosage of pirimicarb) caused a significant reduction of adult hatching. Fertility and longevity of the wasps were not affected by any of the tested insecticides. Dried residues of parathion, but not of the other insecticides, killed a considerable number ofA. rhopalosiphi females. The searching behaviour of the wasps was affected by demeton-S-methyl and fenvalerate. A direct application of demeton-S-methyl, parathion, and the high dosage of pirimicarb onA. rhopalosiphi females caused high mortality.     

Frontier studies on highly selective bio-regulators useful for environmentally benign agricultural production

Fungal metabolites active for insects were obtained from fermentation products using okara media. The mechanisms of action of these compounds against insects were clarified using voltage clamp electrophysiology. The branching factor inducing hyphal branching in arbuscular mycorrhizal (AM) fungi was isolated from the root exudates of Lotus japonicus and identified as 5-deoxystrigol. Strigolactones were originally identified as seed germination stimulants of parasitic weeds; therefore, synthetic strigolactones were developed to exhibit the inducing activity of hyphal branching in AM fungi and diminish the stimulating activity of seed germination of parasitic weeds. Signaling molecules, acylhomoserine lactones (AHLs), in quorum sensing were identified in the fungal strain Mortierella alpina A-178, and the true producer of AHLs was clarified as symbiotic bacteria in the fungus. Since acyl-(S)-adenosylmethionine analogs may be good candidates for competitive inhibitors of AHL synthases, intermediate mimics in the biosynthesis of AHLs have been synthesized.     

Effect of Sparkill and Tafaban insecticides on the mycoflora of maize plant in Upper Egypt

Sparkill (25% Cypermethrin) and Tafaban (48% Chlorpyrifos) insecticides were used in the treatment of maize plants in the field to investigate the effect of these compounds on fungi associated with roots and shoots of maize as well as on soil fungi. Generally, the two insecticides exhibited an inhibitive effect on the total and individual counts of glucophilic fungi after different periods of treatment except in some cases the counts were not affected or promoted compared with the control samples. Fungal genera and species associated with roots and shoots of maize plants were isolated from untreated plants as control and then compared with those isolated from plants treated with different doses of insecticides. The most common fungal species recovered from soil and different parts of plants were Alternaria alternata, Aspergillus flavus, A. fumigatus, A. niger, A. terreus, Cochliobolus spicifer, Emericella nidulans, E. nidulans var. lata, Fusarium oxysporum, Gibberella fujikuroi, Nectria haematococca, Penicillium chrysogenum, P. funiculosum, P. oxalicum and Rhizopus stolonifer.     

Quantitative analysis of polychlorinated biphenyls, organochlorine insecticides, polycyclic aromatic hydrocarbons, polychlorinated hydrocarbons and polynitrohydrocarbons in spiked samples of soil, water and plasma by selected-ion monitoring gas chromatography–mass spectrometry

A broad range of pollutants such as polycyclic aromatic hydrocarbons (PAHs), polychlorinated hydrocarbons (PCHs), polynitrohydrocarbons (PNHs), polychlorinated biphenyls (PCBs) and organochlorine (OCs) insecticides were simultaneously analyzed in spiked soil, water or plasma samples by using gas chromatography–mass spectrometry (GC–MS). Water and plasma samples containing the pollutants were extracted by a solid-phase extraction (SPE) method using florisil columns. The soil samples, fortified with the toxicants, were extracted with water, methanol or dichloromethane (DCM). The water extract was processed by the SPE method. The methanol and DCM samples were dried, dissolved in acetonitrile and subjected to the SPE extraction. The extracted samples were analyzed by GC–MS programmed to monitor selected ions. The deuterium labelled compounds were used as the internal standards. The chromatographic profile of total ions indicated complete separation of some compounds such as isophorone, naphthalene, all PCBs, most OC insecticides and PNHs; high M_r PAHs and some PCHs were partially or incompletely separated. The chromatographic profile of individual ion indicated good separation of each ion. The minimum detection limit ranged from 1 to 4 pg injected when 1 or 2 ions were monitored or from 20 to 200 pg injected when 20 ions were monitored. The SPE method that provided 60–105% recovery of pollutants from water samples, provided only 2–60% recovery from plasma samples. This may be due to the binding of pollutants to plasma proteins. Water recovered 1–30%, while methanol or DCM recovered 65–100% of the pollutants added to the soil samples. The use of internal standards corrected for the loss of pollutants from plasma or soil.     

双酰胺类杀虫剂对棉铃虫和松毛虫赤眼蜂的选择毒力

为了指导棉铃虫防控中化学杀虫剂和天敌昆虫协调使用,本文采用浸叶法和玻管药膜法测定了4种双酰胺类杀虫剂对棉铃虫3龄幼虫和松毛虫赤眼蜂成蜂的毒力.结果表明,供试双酰胺类杀虫剂中氯虫苯甲酰胺、氟苯虫酰胺和氟氰虫酰胺对棉铃虫幼虫表现出了较高的毒力水平(LC50分别为0.2882、0.3894、0.8609 mg/L),稍低于对照药剂甲氨基阿维菌素苯甲酸盐(简称:甲维盐)(LC50为0.06493 mg/L);而溴氰虫酰胺对棉铃虫的毒力(LC50为3.7638 mg/L)明显低于甲维盐.从对天敌昆虫安全性来看,氯虫苯甲酰胺、氟苯虫酰胺和氟氰虫酰胺对松毛虫赤眼蜂的毒性(LC50分别为1.0060、0.9933、1.1541 mg/L)明显低于甲维盐(其LC50为0.1646 mg/L),表现出了较高的安全性;但是,溴氰虫酰胺对松毛虫赤眼蜂毒性较高(LC50为0.4952 mg/L),安全性较差.本研究将为棉铃虫防控中药剂与天敌协调使用提供依据.     

The spatial distribution of beetles within the canopies of oak trees in Richmond Park, U.K.

1. 5054 adult beetles of 144 species were collected in a total of 696 1‐m² collecting trays by knockdown insecticide fogging of 36 different oak trees in closed canopy woodland at Richmond Park, U.K., with three of the trees sampled on each of 12 dates, at 2‐ to 3‐week intervals, between April and October 1984. 2. In late spring (April/May), more individuals and species of beetles were collected in trays close to the trunks of trees than in trays more distant from the trunk. The reverse was the case in late September/October. Neither pattern prevailed in the intervening months. 3. Individual species exhibited a variety of patterns, with some species more abundant near the trunk, e.g. Leiopus nebulosus (L.), Strophosoma melanogrammum (Forster), Cylindronotus laevioctostriatus (Goeze), and Dromius agilis (Fabricius), and some less abundant near the trunk, e.g. Curculio pyrrhoceras (Marsham) and Rhynchaenus signifer (Creutzer). For Adalia decempunctata (L.), this preference changed with season. The observed species preferences for parts of a tree crown near or distant from the main trunk are discussed with reference to their known biologies. 4. No pronounced pattern of preference for north‐ or south‐facing aspects of trees in closed canopy woodland was observed, however populations of some species exhibited patterns of within‐tree distribution that correlate with compass angle; for one species, the ladybird Adalia decempunctata, this distribution changed with season and between colour morphs.     

苏云金杆菌预处理小菜蛾对有机磷和氨基甲酸酯杀虫剂的增效作用

研究了小菜蛾Plutella xylostella幼虫经苏云金杆菌Bacillus thuringiensis预处理后,对有机磷和氨基甲酸酯杀虫剂敏感性的变化以及预处理对小菜蛾幼虫体内乙酰胆碱酯酶、羧酸酯酶、谷胱甘肽S-转移酶和谷胱甘肽的含量的影响。结果表明：苏云金杆菌预处理抗性小菜蛾幼虫后,其对甲胺磷、水胺硫磷和克百威的敏感性分别为未处理组的6.74、8.83和8.50倍;处理敏感小菜蛾幼虫后则分别为未处理组的2.96、1.69和3.88倍。苏云金杆菌预处理抗性小菜蛾,未处理组乙酰胆碱酯酶的K_m和V_max值分别为预处理组的1.86和1.56倍,所使用的6种杀虫剂对乙酰胆碱酯酶的K_I值,处理组为未处理组的1.80～2.66倍,苏云金杆菌预处理抗性小菜蛾对羧酸酯酶的K_m、K_I影响不大,但能显著地抑制羧酸酯酶和谷胱甘肽S-转移酶的活性并导致谷胱甘肽含量下降(对照分别为处理的2.02、1.76和1.66倍)。苏云金杆菌预处理敏感小菜蛾,对乙酰胆碱酯酶的K_m、V_max、K_I值和羧酸酯酶的K_m、K_I值以及谷胱甘肽含量影响不大,但能显著地抑制羧酸酯酶和谷胱甘肽S-转移酶的活性(对照分别为处理的1.54和1.64倍)。     

Compatibility of Lecanicillium longisporum with acetamipride and imidaclopride under laboratory conditions

Lecanicillium longisporum is one of the facultative insect pathogens with significant host range and host specificity. The conidia survival may be affected by environmental factors or by bio-pesticides and chemical products used to protect crop plants. In this research, the compatibility of the mentioned fungi with acetamipride and imidaclopride and the effect of these insecticides on conidial germination and vegetative growth were studied. The formulations of insecticides were tested in three concentrations (mean concentration (MC), half MC and twice the MC). The study was conducted in completely randomised design (CRD) with four replications. The results indicated that acetamipride and imidaclopride in half MC were compatible with L. longisporum (isolate LRC195). However, based on the results, imidacloprid compared to acetamipride is adaptable with L. longisporum. These insecticides could be used simultaneously in low concentration with this entomopathogenic fungus in integrated pest management.     

Identification of the ryanodine receptor mutation I4743M and its contribution to diamide insecticide resistance in Spodoptera exigua (Lepidoptera: Noctuidae)

Insect ryanodine receptors (RyRs) are the targets of diamide insecticides. Two point mutations G4946E and I4790M (numbering according to Plutella xylostella, PxRyR) in the transmembrane domain of the insect RyRs associated with diamide resistance have so far been identified in three lepidopteran pests, P. xylostella, Tuta absoluta and Chilo suppressalis. In this study, we identified one of the known RyR target site resistance mutations (I4790M) in a field‐collected population of Spodoptera exigua. The field‐collected WF population of S. exigua exhibited 154 fold resistance to chlorantraniliprole when compared with the susceptible WH‐S strain. Sequencing the transmembrane domains of S. exigua RyR (SeRyR) revealed that the resistant WF strain was homozygous for the I4743M mutation (corresponding to I4790M in PxRyR), whereas the G4900E allele (corresponding to G4946E of PxRyR) was not detected. The 4743M allele was introgressed into the susceptible WH‐S strain by crossing WF with WH‐S, followed by three rounds of backcrossing with WH‐S. The introgressed strain 4743M was homozygous for the mutant 4743M allele and shared about 94% of its genetic background with that of the recipient WH‐S strain. Compared with WH‐S, the near‐isogenic 4743M strain showed moderate levels of resistance to chlorantraniliprole (21 fold), cyantraniliprole (25 fold) and flubendiamide (22 fold), suggesting that the I4743M mutation confers medium levels of resistance to all three diamides. Genetic analysis showed diamide resistance in the 4743M strain was inherited as an autosomal and recessive trait. Results from this study have direct implications for the design of appropriate resistance monitoring and management practices to sustainably control S. exigua.     

化学杀虫剂对不同类型棉田害虫、天敌种群的影响

研究了化学杀虫剂对6种不同类型棉田的害虫、天敌种群数量及其相互作用的影响。结果表明,化学防治使棉花苗期棉蚜数量下降,但不能抑制中后期棉蚜数量;除豆间棉田外,其他类型棉田化防区棉红蜘蛛和棉铃虫数量低于未防区。化学防治使各类型棉田天敌数量减少,以单作棉田天敌数量减少最明显,间套作棉田天敌数量下降幅度较小;此外,棉田不同天敌种群所受的影响存在一定差异,化学防治对瓢虫、捕食蝽类的影响显著,数量下降剧烈,但蜘蛛类群下降幅度比前两者小。化学防治对棉田害虫与天敌的相互关系的影响随棉田类型或害虫、天敌种类的不同而有所差异。     

Insecticidal and sublethal reproductive effects of Metarhizium anisopliae culture supernatant protein extract on the Mediterranean fruit fly

Because natural product‐based pesticides are thought to be more rapidly degradable than synthetic chemicals while having a lower ecotoxicological effect, the interest in these products for pest control has grown substantially. Recently, a new insecticide compound, which is the crude soluble protein extract (CSPE) from the fermentation product of the entomopathogenic fungus (EF) Metarhizium anisopliae (strain EAMa 01/58‐Su), has appeared in the literature as a promising insecticide for the control of the Mediterranean fruit fly, Ceratitis capitata. This CSPE has a moderate acute insecticide effect against adults of C. capitata when administered per os at 1 mg of protein/ml, as an exposure time of 8.3 h is necessary to get 50% of mortality. Even though the ingestion of this compound produces serious injuries in the midgut epithelium, it has a very low antifeedant effect on the flies. The effect of sublethal challenges on reproduction of adult flies was studied, and a reduction was found on the female fecundity levels during the first days after the treatment. On the other hand, the sublethal exposure to the CSPE affected neither the egg fertility nor the mortality of the larvae. However, the CSPE did affect the mortality of the pupae from the F1 generation, which suggests that there is a hormetic response from CSPE challenged females. The described sublethal reproductive effects are as important as direct lethal effects in contributing to the total value of the CSPE of the EF M. anisopliae 01/58‐Su strain.