Hormesis effects of sulfoxaflor on Aphis gossypii feeding, growth, reproduction behaviour and the related mechanisms.

Sulfoxaflor, an important alternative insecticide in integrated pest management (IPM) strategies, can effectively control sap-feeding insect pests such as Aphis gossypii. Although the side effects of sulfoxaflor have recently attracted widespread attention, its toxicological characteristics and mechanisms are still largely undefined. Therefore, the biological characteristics, life table and feeding behaviour of A. gossypii were studied to evaluate the hormesis effect of sulfoxaflor. Then, the potential mechanisms of induced fecundity associated with the vitellogenin (Ag. Vg) and vitellogenin receptor (Ag. VgR) genes were investigated. Although the LC10 and LC30 concentrations of sulfoxaflor significantly reduced the fecundity and net reproduction rate (R0) of the directly exposed sulfoxaflor-resistant and susceptible aphids, hormesis effects on fecundity and R0 were observed in the F1 generation of Sus A. gossypii when the parental generation was exposed to the LC10 of sulfoxaflor. Moreover, the hormesis effects of sulfoxaflor on phloem feeding were observed in both A. gossypii strains. Additionally, enhanced expression levels and protein content of Ag. Vg and Ag. VgR were observed in progeny generations when F0 was subjected to the trans- and multigenerational sublethal sulfoxaflor exposure. Therefore, sulfoxaflor-induced resurgence might occur in A. gossypii after exposure to sublethal concentrations. Our study could contribute to a comprehensive risk assessment and provide convincing reference to optimize sulfoxaflor in IPM strategies.

Sulfoxaflor adversely influences the biological characteristics of Coccinella septempunctata by suppressing vitellogenin expression and predation activity.

Sulfoxaflor is a widely used sulfoximine insecticide that has been regarded as an important alternative insecticide for IPM strategies, but a comprehensive study of its potential ecological toxicity is still lacking. In the present work, the growth, longevity, predation and reproduction toxicity of Coccinella septempunctata caused by sulfoxaflor were evaluated. In addition, the potential mechanisms of decreased fecundity in C. septempunctata were investigated by analyzing the transcriptional and protein levels of reproduction-related gene vitellogenin (Vg). In a 20-day acute contact toxicity test, decreased survival proportion, pupation rate, adult emergence ratio, and increased hazard quotient (HQ) values were observed. Moreover, sublethal dosages of sulfoxaflor significantly inhibited the predation, longevity, fecundity and net reproduction rate of progeny. In addition, LR30 of sulfoxaflor dramatically down-regulate the mRNA-expression (F0: 65.38-fold, F1: 2.24-fold) and protein content (F0: 1.35-fold, F1: 1.36-fold) of Vg in the F0 and F1 generations. These results suggested that sulfoxaflor could inhibit the gene and protein content of Vg, thereby reducing the fecundity of C. septempunctata. Our study indicated that sulfoxaflor has potential risks to parent and progeny generations of C. septempunctata. These results provide valuable reference for optimal usage of sulfoxaflor in IPM systems.

Seed treatment with chlorantraniliprole and carbaryl mixture for managing fall armyworm on maize: systemic synergism, control efficiency and synergistic mechanism.

BACKGROUND: Fall armyworm (Spodoptera frugiperda) is one of the major invasive pests in China, and has been widely controlled by labor-intensive foliar sprays of agrochemicals in maize (Zea mays L.). RESULTS: Systemic bioassay showed that mixtures of chlorantraniliprole (Chlor) and carbaryl (Carb) had dramatically synergistic effect on toxicity to S. frugiperda. Particularly, a mixture of Chlor with Carb at a mass ratio of 2:1 (MCC) exhibited the highest toxicity to S. frugiperda. Therefore, seed treatment of Chlor mixed with Carb was studied as a simple, accurate, efficient and low-cost control technology. Our results showed that MCC treatment shortened the median lethal time and 90% lethal time to S. frugiperda compared to Chlor- and Carb-alone treatments. Meanwhile, smaller leaf consumption by S. frugiperda was recorded under MCC treatment compared to Chlor- and Carb-alone treatments. In field trial, maize-seed treatment with MCC showed efficacy up to 39 days post-emergence in preventing S. frugiperda foliar damage at a low infestation pressure. Moreover, chemical quantification by ultrahigh-performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) showed that Chlor residues were more absorbed and concentrated in maize leaves of MCC treatment, compared to that of Chlor-alone treatment. CONCLUSION: These results suggested that seed treatment with MCC can be applied to increase the control efficacy and reduce the cost of Chlor-alone treatment for controlling S. frugiperda. The present study provided evidence of an enhanced translocation and accumulation of Chlor residues in maize leaves under MCC treatment, which likely contributed to a synergistic effect against S. frugiperda. © 2022 Society of Chemical Industry.

An insecticide phenotypic resistance diagnostic kit for cotton aphid Aphis gossypii Glover (Hemiptera Aphididae).

BACKGROUND: 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. RESULTS: 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/cm2 were finally identified as the actual diagnostic doses of imidacloprid, acetamiprid, thiamethoxam, nitenpyram, dinotefuran and sulfoxaflor, respectively. The regression equation between mortalities under diagnostic doses and actual resistance ratios tested by the leaf-dipping method were conducted in different strains of A. gossypii, and the diagnostic mortality of A. gossypii was negatively correlated with the resistance ratio to imidacloprid (r = -0.986, P = 0.002), acetamiprid (r = -0.964, P = 0.008), thiamethoxam (r = -0.930, P = 0.022), nitenpyram (r = -0.950, P = 0.013), dinotefuran (r = -0.976, P = 0.004) and sulfoxaflor (r = -0.937, P = 0.019). Moreover, four A. gossypii field populations were selected to apply the diagnostic kit in the field. CONCLUSIONS: 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.

Comparative Toxicity and Joint Effects of Chlorantraniliprole and Carbaryl Against the Invasive Spodioptera frugiperda (Lepidoptera: Noctuidae).

Fall armyworm, Spodoptera frugiperda, is one of the most devastating invasive pests in China. Chlorantraniliprole (CH) is currently the main agent for controlling S. frugiperda. Carbaryl (CA) has been widely used as a foliar treatment to control S. frugiperda, although the pest has become highly resistant to it. This study investigates the comparative toxicity and joint effects of CH and CA on S. frugiperda. Time-toxicity results showed that CH had high toxicity to 1st and 3rd instar larvae, whereas CA had very low toxicity to 1st and 3rd instar larvae. The mixtures of CH and CA at different mass ratios showed strong synergistic effects on toxicity, and the mass ratio of 2:1 exhibited the highest toxicity to S. frugiperda. Furthermore, the synergistic toxicity of CH and CA at the 2:1 mass ratio (CH+CA) was also verified in field populations of S. frugiperda. The life-history parameters showed that CH+CA dramatically decreased the survival rate and fecundity of the parent population (F0) compared with CH treatment at the same concentration. Besides, CH and CH+CA mixture showed induction effect on cytochrome P450s and glutathione-S-transferases (GSTs) activities in S. frugiperda, with cytochrome P450s enzyme responding the fastest. In conclusion, this research found CH+CA provided synergistic effects on the toxicity and the sublethal effect on larvae. The joint effects on the life-history parameters and the detoxifying enzymes in S. frugiperda, may be useful for implementing IPM programs against this Lepidoptera pest.

Field-evolved resistance to 11 insecticides and the mechanisms involved in Helicoverpa armigera (Lepidoptera: Noctuidae).

BACKGROUND: To understand the ongoing resistance of cotton bollworm, Helicoverpa armigera, the sensitivity of five field populations to commonly used insecticides, indoxacarb, abamectin, methoxyfenozide, chlorfenapyr, chlorantraniliprole, spinetoram, lambda-cyhalothrin, carbosulfan, metaflumizone, chlorpyrifos, and flufenoxuron, were evaluated. Furthermore, the biochemical and molecular mechanisms of field-evolved resistance in H. armigera were also investigated. RESULTS: Five field populations of H. armigera showed moderate resistance to indoxacarb, chlorantraniliprole, metaflumizone, methoxyfenozide, carbosulfan and lambda-cyhalothrin. The resistance ratio (RR) of indoxacarb was significantly correlated with glutathione-S-transferases (GSTs) activity (r = 0.913, P = 0.011). Methoxyfenozide RR was largely correlated with cytochrome P450s activity (r = 0.860, P = 0.028). Besides, six cytochrome P450s genes of CYP4L5 in AQP, CYP6B7 and CYP9A14 in HDP and BDP, CYP9A17V2 in HDP and YSP, CYP332A1 in HDP, LFP, AQP and YSP, CYP337B1 in YSP, and two GSTs genes of GSTd1 and GSTs1 in HDP were overexpressed (>5-fold). Moreover, indoxacarb RR was positively correlated with the overexpression of GSTs1, GSTd1 and CYP9A14 genes (r = 0.880, 0.98 and 0.86, P = 0.021, 0.001 and 0.028, respectively). The transcript of CYP9A17V2 and CYP337B1 were found to be correlated with metaflumizone RR (r = 0.950, P = 0.004) and carbosulfan RR (r = 0.850, P = 0.033), respectively. CONCLUSION: H. armigera can be effectively controlled using abamectin, chlorfenapyr, chlorpyrifos and spinetoram in Hebei and Shandong provinces. The present study demonstrated that the relative expression level of GSTs1, GSTd1, CYP9A14, CYP9A17V2 and CYP337B1 genes were significantly correlated with the resistance ratio to indoxacarb, metaflumizone and carbosulfan in field H. armigera.

Overexpression of Multiple UDP-Glycosyltransferase Genes Involved in Sulfoxaflor Resistance in Aphis gossypii Glover.

UDP-glycosyltransferases (UGTs) are major phase II enzymes involved in the metabolic detoxification of xenobiotics. In this study, two UGT-inhibitors, 5-nitrouracil and sulfinpyrazone, significantly increased sulfoxaflor toxicity against sulfoxaflor-resistant (Sul-R) Aphis gossypii, whereas there were no synergistic effects in susceptible (Sus) A. gossypii. The activity of UGTs in the Sul-R strain was significantly higher (1.35-fold) than that in the Sus strain. Further, gene expression determination demonstrated that 11 of 23 UGT genes were significantly upregulated (1.40- to 5.46-fold) in the Sul-R strain, among which the expression levels of UGT350A2, UGT351A4, UGT350B2, UGT342C2, and UGT343C2 could be induced by sulfoxaflor. Additionally, knockdown of UGT350A2, UGT351A4, UGT350B2, and UGT343C2 using RNA interference (RNAi) significantly increased sensitivity (1.57- to 1.76-fold) to sulfoxaflor in the Sul-R strain. These results suggested that UGTs might be involved in sulfoxaflor resistance in A. gossypii. These findings will facilitate further work to validate the functional roles of these UGT genes in sulfoxaflor resistance.

Overexpression of ATP-binding cassette transporters associated with sulfoxaflor resistance in Aphis gossypii glover.

BACKGROUND: Sulfoxaflor is a new insecticide for controlling against Aphis gossypii in the field. ATP-binding cassette (ABC) transporters belong to a large superfamily of proteins and play an important role in the detoxification process. However, the potential role of ABC transporters in sulfoxaflor resistance in A. gossypii is unknown. RESULTS: In this study, an ABC transporter inhibitor, verapamil, dramatically increased the toxicity of sulfoxaflor in the resistant population with a synergistic ratio of 8.55. However, verapamil did not synergize sulfoxaflor toxicity in the susceptible population. The contents of ABC transporters were significantly increased in the Sul-R population. Based on RT-qPCR analysis, 10 of 23 ABC transcripts, ABCA1, ABCA2, ABCB1, ABCB5, ABCD1, ABCG7, ABCG16, ABCG26, ABCG27, and MRP7, were up-regulated in the Sul-R population compared to the Sus population. Meanwhile, inductive effects of ABCA1, ABCD1, ABCG7 and ABCG26 by sulfoxaflor were found in A. gossypii. Furthermore, knockdown of ABCA1 and ABCD1 using RNAi significantly increased the sulfoxaflor sensitivity in Sul-R aphids. CONCLUSION: These results suggested that ABC transporters, especially the ABCA1 and ABCD1 genes, might be related with sulfoxaflor resistance in A. gossypii. This study will promote further work to validate the functional roles of these ABCs in sulfoxaflor resistance and might be helpful for the management of sulfoxaflor-resistant A. gossypii.

Mechanisms of Increased Indoxacarb Toxicity in Methoxyfenozide-Resistant Cotton Bollworm Helicoverpa armigera (Lepidoptera: Noctuidae).

Indoxacarb is an important insecticide for the selective control of Helicoverpa armigera. It can be bioactivated to the more effective N-decarbomethoxylated indoxacarb (DCJW) by esterases in pests. It was observed that both field and laboratory selected populations of H. armigera showed negative cross-resistance between indoxacarb and methoxyfenozide. The Handan population exhibited moderate resistance to indoxacarb, but was susceptible to methoxyfenozide; the Baoding and Yishui populations exhibited moderate resistance to methoxyfenozide, but they were susceptible to indoxacarb. Moreover, the toxicity of indoxacarb was enhanced 1.83-fold in the laboratory methoxyfenozide-resistant H. armigera, and susceptibility to methoxyfenozide was increased 2.81-fold in the laboratory indoxacarb-resistant H. armigera. In vivo, DCJW concentrations in the susceptible and methoxyfenozide-selected (laboratory methoxyfenozide-resistant) populations were 4.59- and 4.31-fold greater than in the indoxacarb-resistant Handan population 1 h after dosing. After 2 h, the highest concentrations of DCJW and indoxacarb appeared in the methoxyfenozide-selected population. Meanwhile, increased carboxyl esterase (CarE) and decreased glutathione S-transferase (GST) activities were observed in the methoxyfenozide-selected population. However, the indoxacarb-selected (laboratory indoxacarb-resistant) and Handan populations showed a higher disappearance of indoxacarb and DCJW, and the activity of cytochrome P450 mono-oxygenase in these populations were significantly increased. This study showed that the improved toxicity of indoxacarb, as observed in the methoxyfenozide-selected H. armigera, was correlated with increased CarE activity, decreased GST activity, and the in vivo accumulation of indoxacarb and DCJW. The significantly increased cytochrome P450 activity and higher disappearance of indoxacarb and DCJW in indoxacarb-resistant H. armigera resulted in the decreased toxicity of indoxacarb.

Biocidal radiuses of cycloxaprid, imidacloprid and lambda-cyhalothrin droplets controlling against cotton aphid (Aphis gossypii) using an unmanned aerial vehicle.

BACKGROUND: Unmanned aerial vehicles (UAVs) are a recently advanced aerial spraying technology. However, the median lethal number of droplets (LN50 ) and biocidal radiuses (r50 ) of insecticides droplets sprayed by UAVs are still unknown. Therefore, we evaluated the LN50 and r50 of cycloxaprid, imidacloprid and lambda-cyhalothrin droplets associated with adjuvant controlling against Aphis gossypii. RESULTS: A small UAV and Potter spray tower (PST) were used to generate different size of droplets (Dv0.5 = 185 ± 5 and 43 ± 2 µm). The mortality of A. gossypii showed a droplet density-dependent process. At the concentration of 5 g L-1 , the LN50 of lambda-cyhalothrin, imidacloprid and cycloxaprid droplets sprayed by the UAV were only 49.2, 34.6 and 19.7 droplets cm-2 , respectively, and the r50 were 0.57, 0.68 and 0.90 mm, respectively. The LN50 values were negatively correlated with insecticide concentrations, but the r50 values increased with the increasing concentrations. Although cycloxaprid is less toxic to A. gossypii than lambda-cyhalothrin, cycloxaprid had a larger r50 than lambda-cyhalothrin due to its translocation ability. Furthermore, cycloxaprid had a relatively larger r50 than imidacloprid because it is more toxic to A. gossypii. Moreover, adjuvant silwet DRS-60 can significantly increase the r50 of droplets. CONCLUSION: Our results revealed that the r50 of a droplet was higher than its droplet size at tested concentrations. Smaller droplets generated by the PST had relatively higher insecticidal potential. The median lethal dose (LD50 ) and translocation ability of insecticides and spray adjuvant contributed to their r50 . Therefore, ultra-low-volume spray with UAVs is feasible to control cotton aphids. © 2020 Society of Chemical Industry.

Cycloxaprid: a novel cis-nitromethylene neonicotinoid insecticide to control Bemisia tabaci.

BACKGROUND: Bemisia tabaci is a worldwide insect pest with high ability to develop resistance to many insecticides. Cycloxaprid is a novel cis-configuration neonicotinoid insecticide that is effective against a wide range of imidacloprid-resistant pests. RESULTS: The lethal and sublethal effects of cycloxaprid on B. tabaci B were estimated. Cycloxaprid showed higher toxicity against adult, nymph and egg of B. tabaci B than imidacloprid. And cycloxaprid provided better efficacies against B. tabaci than imidacloprid in fields. Moreover, cycloxaprid was similarly toxic to the relatively susceptible and imidacloprid-resistant populations. The LC50 of cycloxaprid against the resistant adult, nymph and egg were 6.2, 11.5 and 111.3 mg L-1 , respectively, while they were 5.7, 8.9 and 129.4 mg L-1 for the susceptible population. In addition, when resistant adult of B. tabaci B was treated with LC30 of cycloxaprid (3.2 mg L-1 ), the net reproductive rate and female ratio of F1 generation B. tabaci were reduced. Moreover, the age-specific fecundity demonstrated the highest fecundity sharply decreased in cycloxaprid (7.0 offspring/ day) treated group compared with the control (26.0 offspring/ day). CONCLUSIONS: Our results indicated that cycloxaprid is a promising insecticide for the management of B. tabaci and insecticide-induced resurgence might not occur after exposure of B. tabaci to low sublethal concentrations of cycloxaprid. © 2019 Society of Chemical Industry.

The feeding behavior and life history changes in imidacloprid-resistant Aphis gossypii glover (Homoptera: Aphididae).

BACKGROUND: Imidacloprid (IMI) is a major neonicotinoid insecticide used to control Aphis gossypii Glover. However, resistance to IMI developed rapidly in A. gossypii. The feeding behavior and life history changes associated with IMI resistance were studied in A. gossypii. RESULTS: The resistant population with a point mutation (R81T) in the nAChR ß1 subunit showed an IMI resistance ratio of 58.12. This IMI-resistant A. gossypii became more active in finding an appropriate position for feeding. They made more intercellular apoplastic stylet pathway events (C) than the susceptible population. Moreover, the probing and feeding behavior of two aphid populations were dramatically altered by IMI. The phloem ingestion (E2) duration was significantly longer for IMI-resistant aphids on IMI-treated plants (WDI: 208.70 ± 17.38 min) than on control plants (WDI: 133.80 ± 16.37 min). However, IMI statistically reduced the ability of susceptible aphids to find and feed from the phloem. The number and duration of phloem-related activities were sharply decreased for the susceptible aphids treated with IMI. In addition, the resistant population showed an increased relative fitness of 1.36. The fecundity of IMI-resistant adults was dramatically higher than that of the susceptible population. This difference also led to an increase in the net reproductive rate (R0 ) for the IMI-resistant A. gossypii. CONCLUSIONS: Imidacloprid provoked phloem-feeding more rapidly and effectively in IMI-resistant A. gossypii, but significantly suppressed the feeding of susceptible A. gossypii. Therefore, the resistance to IMI can result in stimulated feeding and fecundity and subsequent population outbreaks, which make the control of IMI-resistant A. gossypii more challenging. © 2019 Society of Chemical Industry.

Design, Synthesis, and Biological Activities of Novel 1,3,5-Trimethylpyrazole-Containing Malonamide Derivatives.

New 1,3,5-trimethylpyrazole-containing malonamide derivatives based on pyflubumide were designed, synthesized, and characterized using ¹H-NMR, 13C-NMR, and high-resolution mass spectra (HRMS). The results of preliminary bioassays showed that the target compounds possessed good activities against Tetranychus cinnabarinus, Plutella xylostella, and Aphis craccivora. Most of the target compounds exhibited moderate to good acaricidal activity against Tetranychus cinnabarinus at a concentration of 400 µg/mL, and some showed moderate activity at a concentration of 200 µg/mL; in particular, compounds 8m and 8p exhibited 70.0% mortality. In addition, some of the target compounds exhibited good insecticidal activities against Plutella xylostella at a concentration of 200 µg/mL, especially compounds 8i and 8o, which achieved 100.0% mortality at a concentration of 100 µg/mL. Interestingly, some of the target compounds exhibited potent anti-aphid activity against Aphis craccivora at a concentration of 200 µg/mL; furthermore, compounds 8p and 8q demonstrated 100.0% anti-aphid activity at a concentration of 50 µg/mL. The preliminary analyses of the structure⁻activity relationships (SAR) indicated that the acaricidal and insecticidal activities varied significantly depending on the type of substituent and substitution pattern, which provides guidance for the further investigation of such structural modifications.

Sublethal effects of the novel cis-nitromethylene neonicotinoid cycloxaprid on the cotton aphid Aphis gossypii Glover (Hemiptera: Aphididae).

Cycloxaprid is a novel cis-configuration neonicotinoid insecticide that is effective against a wide range of insect pests, including those that are resistant to conventional neonicotinoids. In this study, life table parameters were applied to estimate the cycloxaprid-induced sublethal effects on Aphis gossypii. The results indicated that the LC20 (0.81 mg a.i. L-1) of cycloxaprid significantly decreased the pre-oviposition period in first-progeny adults. Additionally, the life expectancy of F1 generation adults was reduced. However, no significant differences were observed for the intrinsic rate of increase (r i ), finite rate of increase (λ), net reproductive rate (R0), or mean generation time (T) of F1 individuals. Therefore, resurgence in the A. gossypii population induced by a low concentration of cycloxaprid might not occur. Additionally, the response of the detoxification enzymes showed that cycloxaprid at the LC20 inhibited cytochrome P450 monooxygenase (P450) and glutathione S-transferase (GST) activities at 6 h after exposure. Such inhibition of P450 and GST activities could lead to a decrease in the metabolism of cycloxaprid, which would increase the efficacy of cycloxaprid. Therefore, our results contribute to the assessment of the overall effects of cycloxaprid on A. gossypii.

Resistance selection of indoxacarb in Helicoverpa armigera (Hübner) (Lepidoptera: Noctuidae): cross-resistance, biochemical mechanisms and associated fitness costs.

BACKGROUND: The cotton bollworm Helicoverpa armigera is a worldwide insect pest with the ability to develop resistance to many insecticides. Indoxacarb, a sodium channel blocker, is an important insecticide that is used to control H. armigera. Cross-resistance, metabolic mechanisms and life history traits were established for an indoxacarb-selected (IND-SEL) population of H. armigera. RESULTS: After 11 generations of selection, the susceptibility to indoxacarb was decreased by 4.43-fold and the estimated realized heritability (h2 ) was only 0.072. Interestingly, the IND-SEL population was more susceptible to methoxyfenozide and abamectin than the susceptible population. The activities of cytochrome P450 monooxygenase (P450) and carboxyl esterase (CarE) were significantly increased in IND-SEL H. armigera. Thus, susceptibility to indoxacarb was increased by piperonyl butoxide and S,S,S-tributyl phosphorothioate, showing synergistic ratios of 2.54- and 1.82-fold, respectively. Moreover, the IND-SEL population had a reduced relative fitness (0.67), with a lower growth rate and fecundity than the susceptible population. CONCLUSIONS: Evidence from this study suggests that decreased susceptibility to indoxacarb may be associated with fitness costs in H. armigera and enhanced activities of P450 and CarE may be important detoxification mechanisms in the development of indoxacarb resistance. Methoxyfenozide and abamectin can be rotationally used to manage indoxacarb resistance. © 2018 Society of Chemical Industry.

Design, synthesis, and insecticidal activity of novel 1-alkoxy-2-nitroguanidines.

In searching for new insecticidal lead compounds, a series of novel 1-alkoxy-2-nitroguanidine, guadipyr analogues bearing alkoxy groups were designed, synthesized and confirmed by 1H NMR, 13C NMR, high-resolution mass spectrometry and X-ray diffraction. The primary bioassays showed that most of these compounds exhibited moderate to good insecticidal activity against Myzus persicae and Aphis gossypii. Especially, the precise insecticidal assay showed that compounds 4-02, 4-07 and 4-08 displayed excellent in vitro activity with IC50 values lower than 10 µg mL-1 to M. persicae which is comparable to guadipyr. On the other hand, the toxicity of compound 4-07 and guadipyr against honey bees was much lower than imidacloprid. The results indicated that the flexible chain on the nitrogen atom was the most crucial factor on honey bee toxicity, which existed in both neonicotinoids and guadipyr series.

The Mechanism by Which Dodecyl Dimethyl Benzyl Ammonium Chloride Increased the Toxicity of Chlorpyrifos to Spodoptera exigua.

Beet armyworm, Spodoptera exigua (Hübner) is one of the most destructive pests that causes significant losses in crops. Unfortunately, S. exigua have developed resistance toward the majority of insecticides. Synergists may provide an important choice to deal with the resistance problems. Dodecyl dimethyl benzyl ammonium chloride (DDBAC) is a cationic surfactant, which displayed enhancement effect when combined with chlorpyrifos against S. exigua, giving enhancement factors of 1.50 and 1.57 at the concentrations of 90 and 810 mg L-1. In order to clarify the possible mechanisms, we investigate the effects of DDBAC on detoxification enzymes. However, DDBAC showed no inhibition on these enzymes activities. Meanwhile, scanning electron microscope images indicated DDBAC did not affect the cuticle super micro structure of S. exigua. The alterations in cuticular penetration rate have also been observed; indeed, it has been suggested that synergism is obtained by an acceleration of insecticide penetration through the cuticle. The chlorpyrifos penetration increased sharply when combined with 90 and 810 mg L-1 DDBAC, with only 12.6 and 8.5% of the initial chlorpyrifos recovered by external rinsing after 8 h. In contrast, when there was no DDBAC, more than 23.3% of the initial dose was recovered after 8 h.

Design, synthesis and insecticidal activity of novel hydrocarbylidene nitrohydrazinecarboximidamides.

BACKGROUND: Neonicotinoids, among the most important pesticides in recent decades, have played pivotal roles in controlling agricultural pests. However, the toxicity to some environmentally beneficial insects is a cause of concern. The development of novel insecticides safer to these insects is increasingly urgent. RESULTS: A novel series of hydrocarbylidene nitrohydrazinecarboximidamides were designed and synthesised, starting from S-methylisothiourea sulphate. Preliminary bioassays showed that the target molecules exhibited good activities against Lipaphis erysimi (turnip aphid) and Myzus persicae. As shown by initial insecticidal activity data, most of the target compounds had moderate to excellent activities at a concentration of 600 mg L-1 against L. erysimi, and the lethal rate of most compounds exceeded 90%. They were also highly effective against M. persicae. Some of them have shown excellent insecticidal activities, for example, the LC50 values of compounds Ie-02 to Ie-07 were found to be 3.8, 3.0, 2.5, 3.1, 4.1 and 4.0 mg L-1 respectively. CONCLUSION: Structure-activity relationship analysis indicated that a suitable flexible alkyl chain at the imine point and a Cl-substituted pyridine ring are the most crucial factors affecting the activity. © 2017 Society of Chemical Industry.

De novo transcriptome and expression profile analyses of the Asian corn borer (Ostrinia furnacalis) reveals relevant flubendiamide response genes.

BACKGROUND: The Asian corn borer (ACB), Ostrinia furnacalis (Guenée), has become the most damaging insect pest of corn in Asia. However, the lack of genome or transcriptome information heavily hinders our further understanding of ACB in every aspect at a molecular level and on a genome-wide scale. Here, we used the Ion Torrent Personal Genome Machine (PGM) Sequencer to explore the ACB transcriptome and to identify relevant genes in response to flubendiamide, showing high selective activity against ACB. RESULTS: We obtained 35,430 unigenes, with an average length of 716 bp, representing a dramatic expansion of existing cDNA sequences available for ACB. These sequences were annotated with Non-redundant Protein (Nr), Gene Ontology (GO), Clusters of Orthologous Groups (COG) and Kyoto Encyclopedia of Genes and Genomes (KEGG) to better understand their functions. A total of 31 cytochrome P450 monooxygenases (P450s), 27 carboxyl/cholinesterases (CCEs) and 19 glutathione S-transferases (GSTs) were manually curated to construct phylogenetic trees, and 25 unigenes encoding target proteins (acetylcholinesterase, nicotinic acetylcholine receptor, gamma-aminobutyric acid receptor, glutamate-gated chloride channel, voltage-gated sodium channel and ryanodine receptor) were identified. In addition, we compared and validated the differentially expressed unigenes upon flubendiamide treatment, revealing that the genes for detoxification enzymes (P450s and esterase), calcium signaling pathways and muscle control pathways (twitchin and tropomyosin), immunoglobulin (hemolin), chemosensory protein and heat shock protein 70 were significantly overexpressed in response to flubendiamide, while the genes for cuticular protein, protease and oxidoreductase showed much lower expression levels. CONCLUSION: The obtained transcriptome information provides large genomic resources available for further studies of ACB. The differentially expressed gene data will elucidate the molecular mechanisms of ACB in response to the novel diamide insecticide, flubendiamide. In particular, these findings will facilitate the identification of the genes involved in insecticide resistance and the development of new compounds to control the ACB.

Cycloxaprid: A novel cis-nitromethylene neonicotinoid insecticide to control imidacloprid-resistant cotton aphid (Aphis gossypii).

Imidacloprid is a nicotinic acetylcholine receptor (nAChR) agonist with potent insecticidal activity. However, resistance to imidacloprid is a significant threat and has been identified in several pest species. Cycloxaprid with cis-configuration is a novel neonicotinoid insecticide, which shows high activity against imidacloprid-resistant pests. The LC50 of imidacloprid against the resistant Aphis gossypii was 14.33mgL(-1) while it was only 0.70mgL(-1) for the susceptible population, giving a resistance ratio of 20.47. In this imidacloprid-resistant population, a point mutation (R81T) located in the loop D region of the nAChR ß1 subunit was found out. But this point mutation did not decrease the activity of cycloxaprid against A. gossypii. The LC50 of cycloxaprid was 1.05 and 1.36mgL(-1) for the imidacloprid-susceptible and imidacloprid-resistant populations, respectively. In addition, cycloxaprid provided better efficacies against resistant A. gossypii than imidacloprid in the fields. Although cycloxaprid was highly toxic to A. gossypii, it showed high selective activity between A. gossypii and its predominant natural enemies, Harmonia axyridis and Chrysoperla sinica. These results demonstrate that cycloxaprid is a promising insecticide against imidacloprid-resistant A. gossypii and suitable for the integrated pest management.