Effect of different droplet size on the knockdown efficacy of directly sprayed insecticides

BACKGROUND: Although insecticidal aerosols have been widely accepted for household use, the discharged amount should be maintained at minimum levels because they contain volatile organic compounds. Hence, it would be valuable to develop a technique whereby insecticide droplets adhere efficiently to an insect's body. The present study was undertaken in order to clarify how differences in the mode of adhesion to the insect body influence the knockdown effect. RESULTS: When the discharged volume of droplets with different diameters was the same, the adhesion volume of larger droplets was twice that of smaller droplets, resulting in a higher insect knockdown. In contrast, when the adhesion volume of the two droplet types was the same, a greater number of smaller droplets than larger droplets adhered, and the smaller droplets caused higher insect knockdown. The knockdown effect of both droplet types was lowered when the mesothoracic spiracles of cockroaches were blocked; however, the effect of larger droplets was lowered to a lesser degree. CONCLUSION: The results suggest that, the probability of adhesion to the more susceptible regions of an insect's body, i.e., areas surrounding the mesothoracic spiracles, was improved when a greater number of smaller droplets were adhered, resulting in higher knockdown. Copyright © 2011 Society of Chemical Industry     

Development of resistance to pyrethroids in field populations of danish houseflies

Houseflies (Musca domestica) on Danish farms have developed high multiresistance to organophosphorus compounds, after successive use of several OPs, mainly dimethoate, in recent years. Topical application tests 1971–73 with flies from many farms showed that the high OP-resistance did not involve resistance to pyrethroids (± the synergist piperonyl butoxide (pb)) above a level of 3–7 x, unless field pressure with synergised pyrethrum (py/pb) or other pyrethroids was applied. In 1971–72 moderate to high, often heterogeneous, pyrethroid resistance was found on a few trial farms treated frequently with pyrethroid aerosols (mainly py/pb) and in 1973 on most of 23 trial farms treated intensively with aerosols (or space spray) containing py/pb, bioresmethrin ± pb, tetramethrin/pb or tetramethrin/resmethrin. The effect of field pressure with these different pyrethroids on development of pyrethroid resistance is summarised and discussed. Maximum resistance ratios, R/S at LD₅₀-LD₉₅, were: py/pb (1:5), 40->100; bioresmethrin, 191–770; bioresmethrin/pb (1:5), 55–133; tetramethrin/pb (1:5), 171->200; tetramethrin/resmethrin (1:5), 78->370. The intensity of selection pressure with pyrethroids is believed to be an important factor. Although py/pb has been widely used as a supplementary fly control on Danish non-trial farms, pyrethroid resistance has only been found on a few of them.     

The activity of some pyrethroids against Periplaneta americana and Blattella germanica

The knockdown and contact killing actions of various pyrethroids were compared using Blattella germanica and Periplaneta americana. A wide range of knockdown activity was found; 5-benzyl-3-furylmethyl (1R)-cis-3-(dihydro-2-oxo-3-thienylidenemethyl)-2,2-dimethylcyclopropanecarboxylate (RU 15525) acted fastest, more rapidly than pyrethrins, against B. germanica as well as having a low LD₅₀ value. Topical application and direct spray tests showed that (S)-α-cyano-3-phenoxybenzyl (1R)-cir-3-(2,2-dibromovinyl)-2,2-dimethylcyclopropanecarboxylate (NRDC 161) was more active as a killing agent, by an order of magnitude, than cismethrin, the next most active compound, and also had considerable knockdown activity. Piperonyl butoxide generally had little synergist effect. Female P. americana were over three times more tolerant than males to a range of insecticides applied topically. Residual knockdown action in the WHO resistance test was observed to provide baseline data. There was little overlap in speed of action between pyrethroids and other insecticides among the compounds tested.     

Thermal behaviour and biological activity against Aedes aegypti (Diptera: Culicidae) of permethrin and pyriproxyfen in a smoke‐generating formulation

BACKGROUND: The most common ways to control dengue vector Aedes aegypti (L.) are larval source reduction in domestic habitats and ground application of small quantities of aerosol insecticide (ultralow volume). Nevertheless, these actions have been shown repeatedly to be ineffective in controlling Ae. aegypti populations. RESULTS: The efficacy of a new smoke‐generating formulation containing pyriproxyfen and permethrin was evaluated in the laboratory. Smoke‐generating tablets containing each insecticide individually or combined were prepared, and the recovery of the insecticides from the smoke was determined. Recovery values of over 90% were obtained for pyriproxyfen, and around 50% for permethrin. The biological efficacy of pyriproxyfen released in the smoke was evaluated in the laboratory, on late third‐instar or early fourth‐instar Ae. aegypti larvae, using different concentrations of pyriproxyfen and exposure times. Adult emergence inhibition (EI) values of 100% were obtained at 30 min, and a dose‐dependent effect was observed at 5 min. The effect of pyriproxyfen released in the smoke was due to direct contact with the larvicide in the water rather than by inhalation of the fumes. The efficacy of permethrin released in the fumes was also evaluated as knockdown effect (KT₅₀) on adults for a tablet containing permethrin alone or permethrin plus pyriproxyfen. There was no significant difference in KT₅₀ values obtained for permethrin (KT₅₀ = 19.9 min) and permethrin plus pyriproxyfen (KT₅₀ = 19.4 min). CONCLUSION: The excellent laboratory performance of this new formulation on immature stages and adults indicates that a smoke‐generating tablet containing pyriproxyfen and permethrin could be a new tool for controlling mosquitoes. Copyright © 2009 Society of Chemical Industry     

Monooxygenase mediated pyrethroid detoxification in sea lice (Lepeophtheirus salmonis)

The role of monooxygenases in detoxification of the pyrethroids cypermethrin and deltamethrin was examined. Four strains of sea lice (Lepeophtheirus salmonis Krøyer) with normal or moderately reduced sensitivity towards the pyrethroids were tested in bioassays by exposure to the pyrethroid alone and in combination with an oxygenase inhibitor, piperonyl butoxide (PBO). The normal (baseline) sensitivity was considered as the sensitivity range for the two most sensitive strains. Pre‐treatment with PBO elevated the sensitivity (P < 0.01) compared with groups exposed to the pyrethroid only. A positive, but not statistically significant, correlation between the activity of haem peroxidases and the pyrethroid concentration immobilizing 50% of the parasites was demonstrated (ρ = 0.500 for deltamethrin and ρ = 0.310 for cypermethrin). The results indicate that cytochrome P450 monooxygenases are involved in detoxification of pyrethroids in sea lice. ¹⁴C‐Deltamethrin was absorbed in a lesser amount in a group of sea lice exposed to a mixture of the compound and PBO than in a group exposed to ¹⁴C‐deltamethrin alone. A significant difference could be demonstrated both immediately after exposure (P < 0.01) and 24 h after exposure (P < 0.05). No significant differences were found between groups pre‐treated with PBO and groups exposed to ¹⁴C‐deltamethrin only. ¹⁴C‐Deltamethrin was taken up mainly through the cuticle, especially the cuticle on the extremities of the ventral surface, and subsequently distributed throughout the body of the parasite. Copyright © 2005 Society of Chemical Industry     

Pyrethroid insecticide resistance in British populations of the cabbage whitefly, Aleyrodes proletella

BACKGROUND: The cabbage whitefly, Aleyrodes proletella L., is emerging as a significant pest of field brassica crops in certain regions of the United Kingdom. In order to investigate the contribution of pesticide resistance to this phenomenon, A. proletella populations were sampled from five different areas in England in 2008 and 2009. Adult residual leaf‐dip bioassays were carried out using pyrethroid and neonicotinoid insecticides. RESULTS: Significant resistance to pyrethroids was found in multiple samples collected from two areas. No evidence of cross‐resistance to neonicotinoids was found in a subset of the pyrethroid‐resistant populations. While the patterns of resistance to different pyrethroids were broadly correlated, the magnitude of resistance factors differed substantially. Survival of strains at a putative diagnostic concentration of lambda‐cyhalothrin was found to provide a guide to their LC₅₀. Significant differences in LC₅₀ were found when different brassica crops were used in the bioassay, although the resistance patterns between strains were maintained. CONCLUSION: Reduced susceptibility to multiple pyrethroid insecticides exists in populations of A. proletella in the United Kingdom, corresponding to recent major outbreaks. The mechanism(s) of resistance are yet to be determined, but molecular structural differences in pyrethroids probably influence the magnitude of cross‐resistance within this group of insecticides. Copyright © 2011 Society of Chemical Industry     

A Stable Synthetic Pyrethroid,NRDC 147, and the Control of Spodoptera littoralis

Abstract

Pyrethrins, the botanical insecticides and their synthetic analogues are well known for their power of producing very rapid paralysis (knockdown) in treated insects. The use of pyrethrins or synthetic analogues in agriculture to combat insect pests on field crops has been rather limited. The main reason for this is their non-persistence in field conditions. A recently developed synthetic pyrethroid NRDC 147, which is 10–100 times more stable in light than previous pyrethroids was tested in the laboratory and field against the Egyptian cotton leafworm Spodoptera littoralis (Boisd). Results indicate higher efficiency (LC₅₀ 320 ppm), compared with 460, 422, 1250, 180, 2150 and 265 ppm for cyolane, chlorpyrifos, leptophos, methomyl, monocrotophos and methamidophos respectively. The residual effect (LT₅₀) is more than 7 days in the field for NRDC 147, while it was 5.8, 6.8 and 4.2 for cyolane, leptophos and methamidophos.     

The actions of pyrethroids upon the peripheral nervous system and associated organs in the locust

The actions of a number of pyrethroids upon the crural nerve, chordotonal organs and skeletal muscles of the desert locust were investigated. The compounds were principally 3-phenoxybenzyl esters (with or without an α substituent), and particular attention was given to fenvalerate and related compounds. Four different effects were observed, both during the early stages of intoxication of intact locusts and during perfusion of physiological preparations with low concentrations of the pyrethroids. The type of effect produced was determined by the molecular structure of the pyrethroid. Knockdown activity was associated with one particular effect, and it is suggested that it is the type of action caused by a pyrethroid, rather than its rate of penetration into the insect, that determines whether or not it will have knockdown activity.     

Differential efficacy of three commonly used pyrethroids against laboratory and field‐collected larvae and adults of Helicoverpa zea (Lepidoptera: Noctuidae) and significance for pyrethroid resistance management

BACKGROUND: Helicoverpa zea (Boddie) pyrethroid resistance monitoring programs typically utilize cypermethrin in the adult vial test. Here we investigated if differences in insect growth stage and pyrethroid structure affect resistance ratios and discuss implications for pyrethroid resistance management. RESULTS: Vial bioassays with cypermethrin, esfenvalerate and bifenthrin were conducted on H. zea third instars and male moths from a susceptible laboratory colony and the F1 generation of a pyrethroid‐resistant field population. In the susceptible population, both growth stages were most sensitive to bifenthrin and adults were more sensitive to esfenvalerate than cypermethrin. LC₅₀ resistance ratios for the larvae and adults of the resistant population were approximately two times higher for bifenthrin than cypermethrin or esfenvalerate. CONCLUSION: For the resistant population, vial assays using either growth stage gave similar resistance ratios for each of the three pyrethroids, respectively, proving the adult vial test accurately reflects larval resistance. However, as resistance ratios varied considerably depending on the pyrethroid used, resistance ratio values obtained with one pyrethroid may not be predictive of resistance ratios for other pyrethroids. Our results suggest that carefully chosen pyrethroid structures diagnostic for specific mechanisms of resistance could improve regional monitoring programs. Copyright © 2009 Society of Chemical Industry     

Insecticide resistance in the tropical bedbug Cimex hemipterus

Insecticide resistance in the bedbug Cimex hemipterus was investigated using 4211 bedbugs collected from three districts of Sri Lanka. Insecticide bioassays were carried out with discriminating dosages of deltamethrin, permethrin, DDT, malathion, and propoxur. Activity levels of insecticide metabolizing enzymes and the insecticide target site acetylcholinesterase were monitored using biochemical assays. Percentage survivals after DDT, malathion, and propoxur exposure were 41-88%, 18-64%, and 11-41%, respectively. For deltamethrin and permethrin, KT₅₀/KT₉₀ (time to knock-down 50%/90% of the population) values were 0.5-24/1.0-58 and 1.3-10/2.5-47 h, respectively. Both elevated esterase and malathion carboxylesterase mechanisms were present in bedbug populations. Monooxygenase levels were heterogeneous. Organophosphate and carbamate target site acetylcholinesterase, was insensitive in 29-44% of the populations. High DDT resistance was probably due to glutathione S-transferases. Malathion carboxylesterases are mainly responsible for high malathion resistance. High tolerance to both DDT and pyrethroids suggests the presence of ‘kdr’ type resistance mechanism in one population.     

Promotion of norepinephrine release and inhibition of calcium uptake by pyrethroids in rat brain synaptosomes

A series of 25 pyrethroids were assessed for their effects on Na⁺-dependent norepinephrine release and on Ca²⁺ uptake in vitro using a crude rat brain synaptosomal preparation. The most effective pyrethroids required a concentration of 3–10 μM to promote norepinephrine release. Plotting release data versus lipophilicity (as log P) for each compound resulted in a parabolic curve with log P_opt being 5.4 for maximal release. The release promoted by most of the compounds assessed at 30 μM could not be or was only partially reversed by either tetrodotoxin or substituting choline for Na⁺ conditions which readily reversed the release promoting effects of veratridine. Thus, many pyrethroids, particularly those without the α-cyano group, did not display their expected effects on the Na⁺ channel in rat brain. When assessed at 5 μM, pyrethroids inhibited, had no effect, or caused increases in the amount of Ca²⁺ incorporated in the presence of ATP. The effectiveness of the various pyrethroids to inhibit Ca²⁺ uptake again displayed a parabolic relationship with log P_opt being 6.4. It was concluded that the variations in pyrethroid effects on norepinephrine release and Ca²⁺ uptake are not solely related to their particular chemical structures, but to lipophilicity. The effects of many pyrethroids on Ca²⁺ metabolism, particularly displacement of bound Ca²⁺, better explain the transmitter release promoting properties in vitro rather than a direct effect on the Na⁺ channel. No direct relationship between known toxicity to mammals and Ca²⁺ inhibition by pyrethroids was established.     

昆虫对拟除虫菊酯类杀虫剂的代谢抗性机制研究进展

随着拟除虫菊酯类杀虫剂在卫生和农业害虫防治中的广泛应用,昆虫对此类杀虫剂产生抗性的报道越来越多。目前已明确昆虫对拟除虫菊酯类杀虫剂的抗性机制包括表皮穿透率下降、靶标抗性以及代谢抗性,其中代谢抗性机制较为普遍,而且其与昆虫对多种杀虫剂的交互抗性关系密切。目前,随着基因组、转录组以及蛋白质组学等新技术的发展及应用,昆虫对拟除虫菊酯类杀虫剂的代谢抗性机制研究也取得了很多新进展。昆虫体内细胞色素P450酶（P450s）、羧酸酯酶（CarE）及谷胱甘肽S-转移酶（GSTs）等重要解毒酶系的改变均与昆虫对拟除虫菊酯类杀虫剂的代谢抗性有关,其中这3类解毒酶的活性及相关基因表达量的变化是昆虫对此类杀虫剂产生代谢抗性的主要原因。明确昆虫对拟除虫菊酯类杀虫剂的代谢抗性机制,对合理使用此类杀虫剂及延缓抗药性的产生均具有重要意义。本文在总结拟除虫菊酯类杀虫剂代谢路径及相关生物酶研究概况的基础上,综述了近年来有关昆虫对此类杀虫剂代谢抗性机制研究的主要进展。     

Pyrethroid resistance in the cotton bollworm,Helicoverpa armigera (Hübner), in West Africa

The susceptibility of Helicoverpa armigera to pyrethroids has been investigated in West Africa by means of laboratory bioassays since 1985, the first year of widespread pyrethroid use. For some years, this survey has shown a tendency for the pest to become more tolerant to pyrethroids. During the 1996 growing season, farmers using calendar‐based spraying programmes reported control failures in various countries. The strong efficacy of cypermethrin on small larvae was confirmed in experimental plots, but the effect decreased quickly in successive instars. Bioassays performed on resistant strains revealed an increase in LD₅₀ that was related to different resistance mechanisms. Metabolic resistance (MFO) appears to be a possible primary mechanism of resistance to pyrethroids. Target modification (kdr) is involved to a small degree and esterases seem to appear only after additional selection pressure. © 2000 Society of Chemical Industry     

Mechanisms responsible for high levels of permethrin resistance in the house fly

The mechanisms responsible for > 6000-fold permethrin resistance in a pyrethroid-selected strain of house fly, Learn-PyR, were investigated. Through electrophysiological, in vitro metabolism, in vivo penetration and synergism studies it was demonstrated that the resistance mechanisms consisted of enhanced metabolic detoxification via the mixed-function oxidase (MFO) system, target-site insensitivity and decreased cuticular penetration. The major resistance mechanism was the MFO-mediated detoxification. The elevated MFO activity was correlated with higher levels of cytochrome P-450, cytochrome b₅ and NADPH-cytochrome c reductase activity. The kinetics of the latter showed similar K_m but greater V_max values in the Learn-PyR than in the susceptible strain, suggesting that the elevated activity was due to an altered amount, but not an altered form, of the enzyme. The Learn-PyR strain showed widely varying levels of resistance to the pyrethroids tested. Comparison of the pyrethroid structures with the resistance ratios revealed that resistance was highest in the presence of an unsubstituted phenoxybenzyl alcohol moiety. Substitution or certain modifications of the alcohol moiety reduced the level of resistance. Structure of the acid moiety or the presence or absence of an a-CN group did not affect the resistance level. These results are discussed with reference to the resistance mechanisms present.     

Time-dose-response relationships of pyrethroid insecticides with special reference to knockdown

The relationship between incoordination, knockdown and mortality was investigated by following the course of poisoning in Schistocerca gregaria of two synthetic pyrethroids, bioresmethrin and bioallethrin. Kinetics describing theonset of these responses as a function of dose are interpreted in terms of the dynamics of penetration and detoxication. The possibility of the same site of action for knockdown and kill is briefly discussed.     

Evidence for different mechanisms of action of the three pyrethroids,deltamethrin, cypermethrin,and fenvalerate,on the excitation threshold of myelinated nerve

The effects of three α-cyano pyrethroids (deltamethrin, fenvalerate, and cypermethrin) on the electrophysiological function of single myelinated nerve fibers from Rana esculenta were investigated. The time course of pyrethroid-induced changes on the threshold interval, V_s − V_m (V_s: threshold voltage; V_m: membrane potential), as well as stationary membrane parameters determining this interval was measured on the same nerve preparation (membrane potential V_m, stationary transition voltage V_Tr, stationary sodium conductance). The results suggest that the mechanisms of changing the threshold interval are different for the three pyrethroids. Deltamethrin and cypermethrin increase this interval until inexcitability, deltamethrin by increasing the stationary sodium conductance and cypermethrin by blocking the sodium conductance. Fenvalerate, however, insignificantly affects the threshold interval because both V_m and V_s are shifted parallel by about the same amount in the same direction (depolarization). These qualitatively different effects of chemically related substances differentiate the pyrethroids from other classes of substances which are effective on the nerve function and suggests that the molecular mechanisms underlying the pyrethroid effects might have a unique quality.     

Characteristics of pyrethroids for insect pest control in agriculture

Pyrethroid insecticides are characterised by high knockdown and lethal activity, a wide spectrum, good residual activity, together with repellent and antifeeding activity. With these characteristics, pyrethroid insecticides have become widely used for plant protection. Their major use has been for the control of bollworms and leafworms in cotton but they have also achieved widespread use for controlling various species of lepidopterous pests in fruits and vegetables, aphids in cereals, and many other minor outlets. Although the early synthetic pyrethroids suffered from a lack of activity against mites and soil pests, later additions, such as fenpropathrin, have combined high acaricidal activity with insecticidal activity and further pyrethroids are being introduced for use in soil. The extent of pyrethroid use has increased progressively since the first of the ‘photostable’ pyrethroids was registered. In 1986, the market share of pyrethroids reached 25 % of the total insecticide market for plant protection; this figure can be increased in the future.     

增效混剂延缓棉铃虫对菊酯农药抗性机制的研究

用同位素标记体壁穿透测定法及不同种群神经敏感性电生理测定法,进行了增效混剂延缓棉铃虫对菊酯抗性机制的初步研究。结果表明,与抗性生物汰选相一致,显示出药剂对增效菊酯混剂汰选种群比对菊酯单剂汰选种群的棉铃虫体壁穿透率高、神经敏感性也高的特点。证明了混剂延缓棉铃虫抗药性确与体壁穿透率和神经敏感性有关,有机制存在,这就为使用增效混剂进行棉铃虫抗性治理的措施打下了部分理论基础。     

A comparative study of insecticide resistance assays with the German cockroach

Females of a diazinon-resistant strain of German cockroach exhibiting cross resistance to propoxur were evaluated for resistance to diazinon and propoxur by six assays: LD₅₀s for topical application and injection; LC₅₀, KT₅₀ and LT₅₀ for deposits on wood and KT₅₀ for deposits on glass. Also investigated were certain variables in the topical application technique and the experimental conditions for topical synergism studies. Among all assays, diazinon resistance ratios (resistant:susceptible) ranged from 3- to 145-fold; propoxur varied from 1- to 14-fold. Resistance ratios based on KT₅₀ data were consistently low (<4x) for both insecticides. Resistance to diazinon was 13x when applied topically and 6x when injected. Resistance to propoxur was 14x by injection compared to 8x for topical application. The LC₅₀ assay exhibited the greatest difference in resistance to the two insecticides: namely, 145x to diazinon and 1x(no resistance) to propoxur. By LT₅₀ analysis, resistance to propoxur was 10x compared with 100x resistance to diazinon. Thus, the method used had a significant effect on the final value of the resistance ratio. Even though resistance ratios may vary widely among different techniques, the final choice of a method depends upon many factors. The LT₅₀ method may provide a more realistic appraisal of resistance in wild populations of German cockroaches especially when experimental residues are similar to those used in control programmes.     

Cross-resistance to pyrethroids and other insecticides in Aedes aegypti

Two substrains of Aedes aegypti, already resistant to DDT and pyrethroids, were further selected using either DDT or permethrin by mass exposure of the females only. DDT selection over 14 generations raised the resistance to DDT so far that no accurate LC₅₀ values could be determined. Selection with permethrin raised the tolerance to an irregular plateau 7–10 times the original. DDT selection in the adults raised the DDT resistance of the larvae, but this could be partly overcome using a dehydrochlorinase inhibitor. The resistance to pyrethroids was increased but tolerance of dieldrin, malathion and propoxur compounds was little changed. Permethrin selection of the adults raised resistance to pyrethroids more than DDT selection but also increased DDT resistance. Similar patterns were found for the larval insects. A strain from Demerara in Guyana showed both DDT and pyrethroid resistance, including strong resistance to pyrethrins together with dieldrin and propoxur. It was concluded that two major independent resistance mechanisms existed in the selected strains, a dehydrochlorinase affecting DDT alone, and an unknown mechanism, probably nerve insensitivity (kdr) affecting both DDT and pyrethroids.