sulfoxaflor and imidacloprid

In the southern United States, neonicotinoids are commonly applied as foliar insecticides to control sucking insect pests, such as the tarnished plant bug (TPB, Lygus lineolaris). In this study, spraying bioassays were conducted to determine the toxicity of five neonicotinoids and sulfoxaflor to susceptible and late fall field-collected TPB adults from Mississippi Delta region. Compared to a susceptible population, the field-collected TPBs exhibited the highest resistance to imidacloprid (up to 19.5-fold), a moderate resistance to acetamiprid (9.43-fold), clothianidin (13.68-fold), thiamethoxam (7.88-fold) and the least resistance to thiacloprid (4.61-fold) and sulfoxaflor (1.82-fold), respectively. A synergist study demonstrated that piperonyl butoxide (PBO) significantly increased the toxicity of imidacloprid and thiamethoxam by 22.2- and 15.3-fold, respectively, while triphenyl phosphate (TPP) and diethyl maleate (DEM) only showed 2-3-fold synergism to both neonicotinoids. In the field-collected TPBs, activities of the three detoxification enzymes esterase, glutathione S-transferase (GST) and CYP450 monooxygenase (P450) were significantly increased by 3.43-, 1.48- and 2.70-fold, respectively, when compared to the susceptible population. Additionally, after 48 h exposure to imidacloprid or thiamethoxam, resistant TPB adults exhibited elevated esterase activities, decreased GST activities, and no significant changes in P450 activities. Further examinations revealed that the expression of certain esterase and P450 detoxification genes were significantly elevated in resistant TPBs. Overall, these results suggest that elevated esterase and P450s expression and enzyme activity are key mechanisms for metabolic resistance in TPBs to neonicotinoids. Our findings also provide valuable information for selection and adoption of neonicotinoid insecticides for resistance management of TPBs and minimizing toxic risk to foraging bees.

Topics: Animals; Esterases; Heteroptera; Insecticide Resistance; Insecticides; Neonicotinoids; Nitro Compounds; Thiamethoxam

Insect pollinators are threatened worldwide, being the exposure to multiple pesticides one of the most important stressor. The herbicide Glyphosate and the insecticide Imidacloprid are among the most used pesticides worldwide, although different studies evidenced their detrimental effects on non-target organisms. The emergence of glyphosate-resistant weeds and the recent ban of imidacloprid in Europe due to safety concerns, has prompted their replacement by new molecules, such as glufosinate-ammonium (GA) and sulfoxaflor (S). GA is a broad-spectrum and non-selective herbicide that inhibits a key enzyme in the metabolism of nitrogen, causing accumulation of lethal levels of ammonia; while sulfoxaflor is an agonist at insect nicotinic acetylcholine receptors (nAChRs) and generates excitatory responses including tremors, paralysis and mortality. Although those molecules are being increasingly used for crop protection, little is known about their effects on non-target organisms. In this study we assessed the impact of chronic and acute exposure to sublethal doses of GA and S on honey bee gut microbiota, immunity and survival. We found GA significantly reduced the number of gut bacteria, and decreased the expression of glucose oxidase, a marker of social immunity. On the other hand, S significantly increased the number of gut bacteria altering the microbiota composition, decreased the expression of lysozyme and increased the expression of hymenoptaecin. These alterations in gut microbiota and immunocompetence may lead to an increased susceptibility to pathogens. Finally, both pesticides shortened honey bee survival and increased the risk of death. Those results evidence the negative impact of GA and S on honey bees, even at single exposition to a low dose, and provide useful information to the understanding of pollinators decline.

Topics: Animals; Bacteria; Bees; Herbicides; Insecticides; Neonicotinoids; Pesticides

Exposure to insecticides may contribute to global insect declines due to sublethal insecticide effects on non-target species. Thus far, much research on non-target insecticide effects has focused on neonicotinoids in a few bee species. Much less is known about effects on other insect taxa or newer insecticides, such as sulfoxaflor. Here, we studied the effects of an acute insecticide exposure on both olfactory and visual learning in free-moving Polistes fuscatus paper wasps. Wasps were exposed to a single, field-realistic oral dose of low-dose imidacloprid, high-dose imidacloprid or sulfoxaflor. Then, visual and olfactory learning and short-term memory were assessed. We found that acute insecticide exposure influenced performance, as sulfoxaflor- and high-dose imidacloprid-exposed wasps made fewer correct choices than control wasps. Notably, both visual and olfactory performance were similarly impaired. Wasps treated with high-dose imidacloprid were also less likely to complete the learning assay than wasps from the other treatment groups. Instead, wasps remained stationary and unmoving in the testing area, consistent with imidacloprid interfering with motor control. Finally, wasps treated with sulfoxaflor were more likely to die in the week after treatment than wasps in the other treatment groups. Our findings demonstrate that sublethal, field-realistic dosages of both neonicotinoid- and sulfoximine-based insecticides impair wasp learning and short-term memory, which may have additional effects on survival and motor functioning. Insecticides have broadly detrimental effects on diverse non-target insects that may influence foraging effectiveness, pollination services and ecosystem function.

Topics: Animals; Bees; Ecosystem; Insecticides; Neonicotinoids; Spatial Learning; Wasps

Aphis gossypii is a notorious pest worldwide, and evidence of resistance of A. gossypii to various insecticides has been documented. Diagnostic tools for the rapid and accurate assessment of insecticide resistance are urgently needed to implement effective pest control and insecticide resistance management strategies.. Using this diagnostic kit based on the glass vial bioassay, detection results can be obtained in 3 h and the values of 897.86, 133.57, 12 037.45, 2849.26, 19 457.33 and 215.60 ng/cm. A diagnostic kit based on the glass vial bioassay for the rapid detection of resistance to imidacloprid, acetamiprid, thiamethoxam, nitenpyram, dinotefuran and sulfoxaflor in A. gossypii was developed. The insecticide diagnostic kit for A. gossypii can be a useful screening tool to determine effective insecticides quickly and accurately. © 2022 Society of Chemical Industry.

Topics: Animals; Aphids; Insecticide Resistance; Insecticides; Neonicotinoids; Thiamethoxam

Sulfoxaflor (Isoclast™ active) is a sulfoximine insecticide that is active on a broad range of sap-feeding insects, including species that exhibit reduced susceptibility to currently available insecticides. Colonies of Myzus persicae (green peach aphid) were established from aphids collected in the field from peach (Prunus persica) and nectarine (Prunus persica var. nucipersica) orchards in France, Italy and Spain. The presence of the nicotinic acetylcholine receptor (nAChR) point mutation R81T was determined for all the colonies. Eight of the 35 colonies collected were susceptible relative to R81T (i.e., R81T absent), three of the colonies were found to be homozygous for R81T while 24 colonies had R81T present in some proportion (heterozygous). Sulfoxaflor and imidacloprid were tested in the laboratory against these M. persicae field colonies, which exhibited a wide range of susceptibilities (sulfoxaflor RR = 0.6 to 61, imidacloprid RR = 0.7 to 986) (resistance ratios, RR) to both insecticides. Although sulfoxaflor was consistently more active than imidacloprid against these field collected M. persicae, there was a statistically significant correlation across all colonies between the RRs for imidacloprid and sulfoxaflor (Pearson's r = 0.939, p < 0.0001). However, when a larger group of the colonies from Spain possessing R81T were analyzed, there was no correlation observed for the RRs between imidacloprid and sulfoxaflor (r = 0.2901, p = 0.3604). Thus, consistent with prior studies, the presence of R81T by itself is not well correlated with altered susceptibility to sulfoxaflor. In field trials, sulfoxaflor (24 and 36 gai/ha) was highly effective (~avg. 88-96% control) against M. persicae, demonstrating similar levels of efficacy as flonicamid (60-70 gai/ha) and spirotetramat (100-180 gai/ha) at 13-15 days after application, in contrast to imidacloprid (110-190 gai/ha) and acetamiprid (50-75 gai/ha) with lower levels of efficacy (~avg. 62-67% control). Consequently, sulfoxaflor is an effective tool for use in insect pest management programs for M. persicae. However, it is recommended that sulfoxaflor be used in the context of an insecticide resistance management program as advocated by the Insecticide Resistance Action Committee involving rotation with insecticides possessing other modes of action (i.e., avoiding rotation with other Group 4 insecticides) to minimize the chances for resistance development and to extend its future utility.

Topics: Animals; Aphids; Insecticides; Mutation; Neonicotinoids; Nitro Compounds; Pyridines; Receptors, Nicotinic; Sulfur Compounds

Unintentional environmental consequences caused by neonicotinoids reinforce the development of safer alternatives. Sulfoxaflor is considered such an alternative. However, ecological risk of sulfoxaflor remains largely unknown. Here, we investigated the acute and chronic toxicity of sulfoxaflor to a benthic invertebrate, Chironomus kiinensis. Sulfoxaflor showed lower lethality than imidacloprid to midges, with LC50 values of 84.1 (81.5-87.3), 66.3 (34.8-259), and 47.5 (29.5-306) μg/L for 96-h, 10-d, and 23-d exposures, respectively. Conversely, sulfoxaflor significantly inhibited C. kiinensis growth and emergence in chronic exposures when concentrations were above 20 μg/L. Effects on energy production were assessed through in vitro tests using mitochondria isolated from C. kiinensis. Sulfoxaflor disrupted mitochondrial state-3 respiration, meanwhile, adenosine triphosphatase (ATPase) activity and adenosine triphosphate (ATP) production were both inhibited in a dose-dependent manner. The observed mitochondrial dysfunction may be related to the decreased organismal growth and emergence, which could further influence biodiversity. Interestingly, sulfoxaflor uptake in C. kiinensis was detected even after emergence, implying its potential to be transported along food webs and among environmental compartments. This study provides thorough investigations on the toxicity of an emerging neonicotinoid alternative to Chironomidae. Data derived from the current study are useful to inform future ecological risk assessment and benefit problem-solving to the overall agriculture-environment nexus.

Topics: Animals; Chironomidae; Insecticides; Invertebrates; Mitochondria; Neonicotinoids; Nitro Compounds; Pyridines; Risk Assessment; Sulfur Compounds; Water Pollutants, Chemical

Systemic insecticides are used to control agricultural pests globally and their non-target impact at non-lethal doses on beneficial arthropods has been recognized. We assessed the baseline toxicity of imidacloprid, thiamethoxam and sulfoxaflor-based insecticides on the polyphagous aphid pest, Aphis gossypii (Hemiptera: Aphididae), and their non-target effects on its main parasitoid, Aphidius colemani (Hymenoptera: Braconidae), evaluated by residual contact exposure to the median lethal (LC

Topics: Animals; Aphids; Biological Control Agents; Hymenoptera; Insecticides; Neonicotinoids; Nitro Compounds; Pyridines; Sulfur Compounds; Thiamethoxam

Insect nervous systems offer unique advantages for studying interactions between sensory systems and behavior, given their complexity with high tractability. By examining the neural coding of salient environmental stimuli and resulting behavioral output in the context of environmental stressors, we gain an understanding of the effects of these stressors on brain and behavior and provide insight into normal function. The implication of neonicotinoid (neonic) pesticides in contributing to declines of nontarget species, such as bees, has motivated the development of new compounds that can potentially mitigate putative resistance in target species and declines of nontarget species. We used a neuroethologic approach, including behavioral assays and multineuronal recording techniques, to investigate effects of imidacloprid (IMD) and the novel insecticide sulfoxaflor (SFX) on visual motion-detection circuits and related escape behavior in the tractable locust system. Despite similar LD

Topics: Animals; Environmental Exposure; Escape Reaction; Habituation, Psychophysiologic; Insecticides; Lethal Dose 50; Locusta migratoria; Motion; Motor Neurons; Neonicotinoids; Nitro Compounds; Pyridines; Sulfur Compounds

Systemic neurotoxic insecticides are widely used to control aphid pests worldwide and their potential non-target effects on aphid predators are often unknown. Behavioral responses linked to biological control services are crucial when assessing the compatibility of chemicals with biocontrol organisms. This is particularly relevant for insecticides at low and sublethal concentrations. We studied the acute toxicity and the sublethal effect on the voracity of the generalist predator Harmonia axyridis (Coleoptera: Coccinellidae) caused by the exposure to three systemic insecticides routinely used against aphids. The tested insecticide concentrations were the Lethal Concentration 50% (LC

Topics: Animals; Aphids; Coleoptera; Insecticides; Lethal Dose 50; Neonicotinoids; Nitro Compounds; Predatory Behavior; Pyridines; Sulfur Compounds; Thiamethoxam

A key to effective insect pest management and insecticide resistance management is to provide growers with a range of new tools as potential alternatives to existing compounds or approaches. Sulfoxaflor (Isoclast™ active) is a new sulfoximine insecticide which is active on a broad range of sap-feeding insects, including species that have reduced susceptibility to currently used insecticides, such as imidacloprid from the neonicotinoid class. Sulfoxaflor (SFX) and imidacloprid (IMI) were tested in laboratory bioassays to compare the susceptibility of field populations of green peach aphid, Myzus persicae (Sulzer), exhibiting varying degrees of resistance involving an alteration (R81T) to the insect nicotinic acetylcholine receptor. The LC

Topics: Animals; Aphids; Mutation; Neonicotinoids; Nitro Compounds; Prunus persica; Pyridines; Receptors, Nicotinic; Spain; Sulfur Compounds

Systemic insecticides, such as neonicotinoids, are a major contributor towards beneficial insect declines. This has led to bans and restrictions on neonicotinoid use globally, most noticeably in the European Union, where four commonly used neonicotinoids (imidacloprid, thiamethoxam, clothianidin and thiacloprid) are banned from outside agricultural use. While this might seem like a victory for conservation, restrictions on neonicotinoid use will only benefit insect populations if newly emerging insecticides do not have similar negative impacts on beneficial insects. Flupyradifurone and sulfoxaflor are two novel insecticides that have been registered for use globally, including within the European Union. These novel insecticides differ in their chemical class, but share the same mode of action as neonicotinoids, raising the question as to whether they have similar sub-lethal impacts on beneficial insects. Here, we conducted a systematic literature search of the potential sub-lethal impacts of these novel insecticides on beneficial insects, quantifying these effects with a meta-analysis. We demonstrate that both flupyradifurone and sulfoxaflor have significant sub-lethal impacts on beneficial insects at field-realistic levels of exposure. These results confirm that bans on neonicotinoid use will only protect beneficial insects if paired with significant changes to the agrochemical regulatory process. A failure to modify the regulatory process will result in a continued decline of beneficial insects and the ecosystem services on which global food production relies.

Topics: 4-Butyrolactone; Animals; Ecosystem; Guanidines; Insecta; Insecticides; Neonicotinoids; Nitro Compounds; Pyridines; Sulfur Compounds; Thiamethoxam; Thiazines; Thiazoles

External feather rinses and homogenized whole-carcass tissue matrix from two hummingbird species found in California (Calypte anna and Archilochus alexandri) were analyzed for the presence of nine insecticides commonly used in urban settings. Using a liquid chromatography-high-resolution mass spectrometry (LC-HRMS) analytical method, samples were quantitatively tested for the following neonicotinoids: dinotefuran, nitenpyram, thiamethoxam, acetamiprid, thiacloprid, clothianidin, imidacloprid, and sulfoxaflor. This analytical method was also used to qualitatively screen for the presence of approximately 150 other pesticides, drugs, and natural products. Feather rinsates from both hummingbird species had detectable concentrations of carbamate and neonicotinoid classes of insecticides. Combined results of the rinsate and homogenized samples (n = 64 individual hummingbirds) showed that 44 individuals (68.75%) were positive for one to four target compounds. This study documented that hummingbirds found in California are exposed to insecticides. Furthermore, feather rinsates and carcass homogenates are matrices that can be used for assessing pesticide exposure in small bird species. The small body size of hummingbirds limits traditional sampling methods for tissues and whole blood to evaluate for pesticide exposure. Thus, utilization of this analytical method may facilitate future research on small-sized avian species, provide insight into pesticide exposure, and ultimately lead to improved conservation of hummingbirds.

Topics: Animals; Birds; California; Chromatography, Liquid; Feathers; Guanidines; Insecticides; Neonicotinoids; Nitro Compounds; Pyridines; Sulfur Compounds; Tandem Mass Spectrometry; Thiamethoxam; Thiazines; Thiazoles

Sulfoxaflor is the first commercially available sulfoximine insecticide, which exhibits highly efficacy against many sap-feeding insect pests and has been applied as an alternative insecticide against cotton aphid in China. This study was conducted to investigate the risk of resistance development, the cross-resistance pattern and the potential resistance mechanisms of sulfoxaflor in Aphis gossypii. A colony (SulR strain) of A. gossypii with 245-fold resistance, originated from Xinjiang field population, was established by continuous selection using sulfoxaflor. The SulR strain has developed cross-resistance to imidacloprid (80.8-fold), acetamiprid (19.3-fold), thiamethoxam (10.0-fold), and flupyradifurone (107.5-fold), while no cross-resistance was detected to malathion, omethoate, bifenthrin, methomyl, and carbosulfan. Piperonyl butoxide and S, S, S-tributyl phosphorotrithioate could significantly increase the toxicity of sulfoxaflor to the SulR strain by 5.99- and 4.18-fold, respectively, whereas no synergistic effect with diethyl maleate was observed. The activities of P450s and carboxylesterase were significantly higher in the SulR strain than that in the SS strain. Further gene expression determination demonstrated that nine P450 genes were significantly increased in SulR strain and suppression the expression of CYP6CY13 and CYP6CY19 by RNAi significantly increased the susceptibility of SulR adult aphids to sulfoxaflor. These results demonstrated that the enhancing detoxification by cytochrome P450 monooxygenase may be involved in A.gossypii resistance to sulfoxaflor.

Topics: 4-Butyrolactone; Animals; Aphids; Cytochrome P-450 Enzyme System; Insecticide Resistance; Insecticides; Neonicotinoids; Nitro Compounds; Pyrethrins; Pyridines; Sulfur Compounds

Cockroach neurosecretory cells, dorsal unpaired median (DUM) neurons, express two distinct α-bungarotoxin-insensitive nicotinic acetylcholine receptor subtypes, nAChR1 and nAChR2 which are differently sensitive to the neonicotinoid insecticides and intracellular calcium pathways. The aim of this study is to determine whether sulfoxaflor acts as an agonist of nAChR1 and nAChR2 subtypes. We demonstrated that 1 mM sulfoxaflor induced high current amplitudes, compared to acetylcholine, suggesting that it was a full agonist of DUM neuron nAChR subtypes. Sulfoxaflor evoked currents were not inhibited by the nicotinic acetylcholine receptor antagonist d-tubocurarine (dTC) which reduced nAChR1. But, sulfoxaflor evoked currents were reduced in the presence of 5 μM mecamylamine which is known to reduce nAChR2 subtype. Interestingly, when 1 μM imidacloprid was added in the extracellular solution, sulfoxaflor-induced currents were significantly suppressed. Moreover, when extracellular calcium concentration was increased, bath application of 1 μM imidacloprid partially reduced sulfoxaflor activated currents when nAChR1 was inhibited with 20 μM dTC and completely suppressed sulfoxaflor currents when nAChR2 was inhibited with 5 μM mecamylamine. Our data demonstrated therefore that sulfoxaflor activates both nAChR1 and nAChR2 subtypes.

Topics: Acetylcholine; Animals; Bungarotoxins; Calcium; Cholinergic Agents; Cockroaches; Mecamylamine; Neonicotinoids; Nicotinic Agonists; Nicotinic Antagonists; Nitro Compounds; Patch-Clamp Techniques; Pyridines; Receptors, Nicotinic; Sulfur Compounds; Tubocurarine

Control of Bemisia tabaci has depended primarily and heavily on insecticides, especially neonicotinoids. The novel sulfoximine insecticide sulfoxaflor exhibits high potency against a broad range of sap-feeding insect species, including those resistant to neonicotinoids. The resistance levels of Q-biotype B. tabaci field strains collected from 8 locations in eastern China to neonicotinoids and sulfoxaflor were investigated, and single nucleotide polymorphisms (SNPs) of nicotinic acetylcholine receptor β1 subunit gene (Btβ1) were detected. Compared with the reference strain, the field strains had developed low to moderate levels of resistance to imidacloprid and nitenpyram with the resistance ratios (RR) ranging between 4.07 and 21.75-fold and 3.37 and 16.14-fold, respectively. While YZ strain exhibited high resistance (RF 40.38) to thiamethoxam, only low levels of resistance to thiamethoxam (RF 3.50-8.58) was observed in other strains. All strains were relatively susceptible to both dinotefuran (RF 0.50-2.55) and sulfoxaflor (RF 0.40-3.07). Sequence analysis of Btβ1 cDNA fragments revealed 23 SNPs representing 19 amino acid replacements in these strains. Notably, a 45bp fragment deletion was detected in JY strain, which encodes 15 amino acid residues (positions 66-80) containing arginine at position 79 (R79) corresponding to the R81T mutation in Loop D of nAChR β1 subunit in Myzus persicae resistant to neonicotinoids. The lack of cross-resistance indicates that both dinotefuran and sulfoxaflor could play an important role in the control of B. tabaci already resistant to the first and second generation neonicotinoids.

Topics: Amino Acid Sequence; Animals; Base Sequence; China; Cloning, Molecular; DNA, Complementary; Female; Guanidines; Hemiptera; Imidazoles; Insect Proteins; Insecticide Resistance; Insecticides; Male; Neonicotinoids; Nitro Compounds; Oxazines; Polymorphism, Single Nucleotide; Protein Subunits; Pyridines; Receptors, Nicotinic; Sequence Analysis, DNA; Sulfur Compounds; Thiamethoxam; Thiazoles

Sulfoxaflor, a new insecticide from the sulfoximine chemical family, and imidacloprid, a widely used neonicotinoid insecticide, were tested to assess the susceptibility and feeding behaviour of two populations of Myzus persicae: Mp61, which exhibited target-site R81T resistance to neonicotinoids, and Mp1989, a laboratory clone maintained since 1989 as a susceptible reference.. The imidacloprid LC50 value for Mp61 was 16 times higher than for Mp1989, showing a moderate level of resistance. Sulfoxaflor LC50 values for Mp61 and Mp1989 were much closer. The probing behaviour, as assessed by electrical penetration graphs (EPGs), of both populations was clearly altered by sulfoxaflor, which reduced the ability of aphids to find and feed from the phloem. The feeding behaviour of the susceptible Mp1989 population was much more severely affected than the moderately resistant Mp61 population on imidacloprid-treated plants. PCR assays of both aphid populations followed by DNA sequencing identified differences between populations in the point mutation in the β-subunit of the nicotinic acetylcholine receptor linked to the resistant gene against the neonicotinoid insecticide.. Sulfoxaflor provoked feeding cessation more rapidly than imidacloprid in both aphid populations. Sharp differences in feeding behaviour were detected between the susceptible and the moderately resistant neonicotinoid-resistant aphid populations. The EPG technique can be used as a useful tool to give new insights into the functional effects of new chemical compounds and for early detection of low to moderate levels of resistance of sap-feeding insects to insecticides. The potential of this technique was validated by molecular analysis of the R81T mutation target site.

Topics: Animals; Aphids; Biological Assay; DNA Mutational Analysis; Electricity; Feeding Behavior; Imidazoles; Insecticide Resistance; Insecticides; Neonicotinoids; Nitro Compounds; Pyridines; Sulfur Compounds

The green peach aphid, Myzus persicae (Sulzer), is an important insect pest of many crops around the world. Pesticide-induced hormesis may be an alternative mechanism for pest resurgence. In this study, life table parameters were applied to the estimation of sulfoxaflor-induced hormesis of adult M. persicae following 2-d LC25 concentration exposure. Leaf-dip bioassays showed that the sulfoxaflor possessed high toxicity against M. persicae, with an LC50 of 0.059 mg/liter. The results indicated that the exposure of the parent generation of M. persicae to sublethal sulfoxaflor induced increase in reproduction and prolongation of immature development duration in the first progeny generation. Both R0 and GRR of aphids for treatment group were significantly higher than for the control in F1 generation, and the mean generation time was significantly postponed in treated group. These results suggest a hormesis induced by lower concentration of sulfoxaflor in M. persicae. It would be useful for assessing the overall effects of sulfoxaflor on M. persicae.

Topics: Animals; Aphids; Imidazoles; Insecticides; Neonicotinoids; Nitro Compounds; Pyridines; Reproduction; Sulfur Compounds

Insecticides are important tools for managing damaging insect pests. Compounds that are effective against pests such as the whiteflies Bemisia tabaci and Trialeurodes vaporariorum, which show resistance to a range of insecticidal modes of action (MOA), have particular value as components of resistance management programmes. The sulfoximine insecticides are chemically unique as the first to incorporate a sulfoximine functional group. Sulfoxaflor is the first sulfoximine compound under commercial development for the control of sap-feeding insects. Its cross-resistance relationships were investigated by comparing the responses of field-collected strains with those of insecticide-susceptible laboratory strains of B. tabaci and T. vaporariorum.. Sulfoxaflor exhibited very low (less than threefold) resistance ratios (RR) when tested against strains of B. tabaci that produced RR of up to 1000-fold to imidacloprid and cross-resistance to other neonicotinoid insecticides. Similarly, sulfoxaflor was not cross-resistant in a strain of B. tabaci exhibiting resistance to a pyrethroid (deltamethrin) and an organophosphate (profenophos). No cross-resistance was observed between sulfoxaflor and imidacloprid in T. vaporariorum. One population of the three field strains tested showed slightly reduced susceptibility to sufloxaflor with an RR of 4.17. By comparison, this same population exhibited an RR of more than 23.8-fold for imidacloprid relative to the susceptible population.. In spite of sharing a target site with neonicotinoids (the nicotinic acetylcholine receptor), sulfoxaflor was largely unaffected by existing cases of neonicotinoid resistance in B. tabaci and T. vaporariorum. Neonicotinoid resistance mechanisms in these whitefly species are known to be primarily based on enhanced detoxification of insecticide. This lack of cross-resistance indicates that sulfoxaflor is a valuable new tool for the management of sap-feeding pests already resistant to established insecticide groups.

Topics: Animals; Hemiptera; Imidazoles; Insecticide Resistance; Insecticides; Neonicotinoids; Nitro Compounds; Pyridines; Sulfur Compounds

The discovery of sulfoxaflor [N-[methyloxido[1-[6-(trifluoromethyl)-3-pyridinyl]ethyl]-λ(4)-sulfanylidene] cyanamide] resulted from an investigation of the sulfoximine functional group as a novel bioactive scaffold for insecticidal activity and a subsequent extensive structure-activity relationship study. Sulfoxaflor, the first product from this new class (the sulfoximines) of insect control agents, exhibits broad-spectrum efficacy against many sap-feeding insect pests, including aphids, whiteflies, hoppers, and Lygus, with levels of activity that are comparable to those of other classes of insecticides targeting sap-feeding insects, including the neonicotinoids. However, no cross-resistance has been observed between sulfoxaflor and neonicotinoids such as imidacloprid, apparently the result of differences in susceptibility to oxidative metabolism. Available data are consistent with sulfoxaflor acting via the insect nicotinic receptor in a complex manner. These observations reflect the unique structure of the sulfoximines compared with neonicotinoids.

Topics: Animals; Aphids; Hemiptera; Imidazoles; Insecta; Insecticide Resistance; Insecticides; Neonicotinoids; Nitro Compounds; Pyridines; Receptors, Nicotinic; Structure-Activity Relationship; Sulfur Compounds

The novel sulfoximine insecticide sulfoxaflor is as potent or more effective than the neonicotinoids for toxicity to green peach aphids (GPA, Myzus persicae). The action of sulfoxaflor was characterized at insect nicotinic acetylcholine receptors (nAChRs) using electrophysiological and radioligand binding techniques. When tested for agonist properties on Drosophila melanogaster Dα2 nAChR subunit co-expressed in Xenopus laevis oocytes with the chicken β2 subunit, sulfoxaflor elicited very high amplitude (efficacy) currents. Sulfoximine analogs of sulfoxaflor were also agonists on Dα2/β2 nAChRs, but none produced maximal currents equivalent to sulfoxaflor nor were any as toxic to GPAs. Additionally, except for clothianidin, none of the neonicotinoids produced maximal currents as large as those produced by sulfoxaflor. These data suggest that the potent insecticidal activity of sulfoxaflor may be due to its very high efficacy at nAChRs. In contrast, sulfoxaflor displaced [(3)H]imidacloprid (IMI) from GPA nAChR membrane preparations with weak affinity compared to most of the neonicotinoids examined. The nature of the interaction of sulfoxaflor with nAChRs apparently differs from that of IMI and other neonicotinoids, and when coupled with other known characteristics (novel chemical structure, lack of cross-resistance, and metabolic stability), indicate that sulfoxaflor represents a significant new insecticide option for the control of sap-feeding insects.

Topics: Animals; Aphids; Binding, Competitive; Chickens; Drosophila melanogaster; Drosophila Proteins; Female; Imidazoles; Insect Control; Insect Proteins; Insecticides; Membrane Potentials; Neonicotinoids; Nicotinic Agonists; Nitro Compounds; Oocytes; Protein Subunits; Pyridines; Radioligand Assay; Receptors, Nicotinic; Recombinant Proteins; Sulfur Compounds; Transfection; Xenopus laevis

Imidacloprid, sulfoxaflor and two experimental sulfoximine insecticides caused generally depressive symptoms in stick insects, characterized by stillness and weakness, while also variably inducing postural changes such as persistent ovipositor opening, leg flexion or extension and abdomen bending that could indicate excitation of certain neural circuits. We examined the same compounds on nicotinic acetylcholine receptors in stick insect neurons, which have previously been shown to desensitize in the presence of ACh. Brief U-tube application of 10(-4) M solutions of insecticides for 1 s evoked currents that were much smaller than ACh-evoked currents, and depressed subsequent ACh-evoked currents for several minutes, indicating that the compounds are low-efficacy partial agonists that potently desensitize the receptors. Much lower concentrations of insecticides applied in the bath for longer periods did not activate currents, but inhibited ACh-evoked currents via desensitization of the receptors. Previously described fast- and slowly-desensitizing nACh currents, I(ACh1) and I(ACh2) respectively, were each found to consist of two components with differing sensitivities to the insecticides. Imidacloprid applied in the bath desensitized high-sensitivity components, I(ACh1H) and I(ACh2H) with IC(50)s of 0.18 and 0.13 pM, respectively. It desensitized the low-sensitivity slowly desensitizing component, I(ACh2L), with an IC(50) of 2.6 nM, while a component of the fast-desensitizing current, I(ACh1L), was least sensitive, with an IC(50) of 81 nM I(ACh1L) appeared to be insensitive to the three sulfoximines tested, whereas all three sulfoximines potently desensitized I(ACh1H) and both slowly desensitizing components, with IC(50)s between 2 and 7 nM. We conclude that selective desensitization of certain nAChR subtypes can account for the insecticidal actions of imidacloprid and sulfoximines in stick insects.

Topics: Animals; Central Nervous System; Female; Imidazoles; Insecta; Insecticides; Neonicotinoids; Nitro Compounds; Pyridines; Receptors, Nicotinic; Sulfur Compounds