In-Depth Structural Simplification of Celangulin V: Design, Synthesis, and Biological Activity.

Celangulin V is a novel botanical insecticide with significant bioactivity and a unique molecular target, but its complex polyol ester structure hinders its broader application in agriculture. To discover new analogues of celangulin V with a simpler structure and enhanced biological activities, we initiated a research project aimed at simplifying its structure and assessing insecticidal efficacy. In this study, a series of novel 1-tetralone derivatives were designed via a structure-based rational design approach and synthesized by a facile method. The biological activities of the target compounds were determined against Mythimna separata (M. separata), Plutella xylostella, and Rhopalosiphum padi. The results revealed that most of the synthesized compounds exhibited superior activities compared to celangulin V. Remarkably, the insecticidal activity of compound 6.16 demonstrated 102-fold greater stomach toxicity than celangulin V against M. separata. In addition, certain compounds showed significant contact toxicity against M. separata, a finding not reported previously in the structural optimization studies of celangulin V. Molecular docking analysis illustrated that the binding pocket of compound 6.16 with the H subunit of V-ATPase was the same as celangulin V. This study presents novel insights into the structural optimization of botanical pesticides.

Laboratory evaluation of a bio-insecticide candidate from tangerine peel extracts against Trialeurodes vaporariorum (Homoptera: Aleyrodidae).

Background: The excessive use of synthetic insecticides in modern agriculture has led to environmental contamination and the development of insect resistance. Also, the prolonged use of chemical insecticides in producing flowers and tomatoes in greenhouses has caused health problems for workers and their offspring. In this study, we analyzed the efficacy of mandarin peel (Citrus reticulata L.) essential oil (EO) as a natural insecticide against greenhouse whitefly (Trieurodes vaporariorum W., Homoptera: Aleyrodidae), a common pest in greenhouse production of different crops. Methods: Petroleum ether (PET) and n-hexane (HEX) were used as solvents to extract essential oil (EO) from tangerine peels. Results: The yield of EO was 1.59% and 2.00% (m/m) for PET and HEX, respectively. Additionally, the insect-killing power of EO was tested by checking how many greenhouse whiteflies died at different times. The results showed that PET and HEX extracts of tangerine EO effectively controlled greenhouse whiteflies. Furthermore, with both solvents, a 12.5% (v/v) application was as practical as the commercial insecticide imidacloprid. Further characterization tests with the polarimeter, FTIR, HPLC-RP, and GC-MS showed that the essential oil (EO) contained about 41% (v/v) of d-limonene and that this compound may be responsible for the observed insecticidal properties. Conclusion: Therefore, tangerine peel essential oil is an excellent botanical insecticide candidate for controlling greenhouse whiteflies.

Copaiba oil and Neem extract can be a potential alternative for the behavioral control of Sitophilus zeamais

Abstract Insects' ethology is an important factor when it is desired to carry out pest management. This knowledge makes it possible to manipulate behavioral activities, repel, or attract insects according to needs and interests. The maize weevil Sitophilus zeamais (Mots., 1855) (Coleoptera: Curculionidae), one of the main stored grain pests, has been the target of studies of behavioral changes studies through natural substances due to its resistance to different insecticidal classes. Thus, this study aimed to evaluate the effect of sublethal concentrations of neem extract and copaiba oil on the locomotor behavior of S. zeamais. The behavioral characteristic considered were walking activity, the frequency of contact of insects with the treated grain mass, and the time spent for this behavior. The walking activity of the S. zeamais increased with exposure to Neem extract and Copaiba oil. In general, the Neem extract and Copaiba oil-induced more contact with grain mass than the control, suggesting an attractive effect on the insect, however more significant for the Neem oil. The insect's behavior was altered, presenting a specific path due to Copaiba oil and Neem extract stimuli. These results indicate that Copaiba oil and Neem extract can be a potential alternative for controlling S. zeamais on stored products since changes in this pests' behavior can reduce qualitative and quantitative grain damage. Thus, the development of products based on Copaiba oil and Neem extract may be helpful for storage pest management.

Resumo A etologia dos insetos é um fator importante quando se deseja relizar manejo de pragas. Através deste conhecimento, é possível manipular atividades comportamentais, repelir, ou atrair os insetos de acordo com as necessidades e interesses. O gorgulho do milho Sitophilus zeamais (Mots., 1855) (Coleoptera: Curculionidae), uma das principais pragas de grãos armazenados tem sido alvo de estudos de alterações comportamentais através de substâncias naturais devido à sua resistência a diferentes classes de insecticidas. Assim, este estudo teve como objetivo avaliar o efeito de concentrações subletais de extrato de neem e do óleo de copaíba sobre o comportamento de movimentação de S. zeamais. As características comportamentais consideradas foram: a atividade de caminhamento, a frequência do contato dos insetos com a massa de grãos tratada, e o tempo gasto para realização destes comportamentos. A atividade de caminhamento do S. zeamais aumentou quando os insetos foram expostos ao extrato de Neem e ao óleo de copaíba. Em geral, o extrato de Neem e o óleo de Copaíba induziram mais contato com a massa de grãos do que o controle, sugerindo um efeito atrativo sobre o inseto, contudo este efeito foi mais significativo para o óleo de Neem. O comportamento do inseto foi alterado, apresentando um caminhamento específico devido aos estímulos do óleo de copaíba e do extrato de Neem. Estes resultados indicam que o óleo de copaíba e o extrato de Neem podem ser alternativas potenciais para o controle do S. zeamais em produtos armazenados, uma vez que alterações no comportamento desta praga podem reduzir os danos qualitativos e quantitativos nos grãos. Assim, o desenvolvimento de produtos baseados no óleo de copaíba e no extrato de Neem pode ser útil para o manejo de pragas de armazenamento.

α-Terpineol affects social immunity, increasing the pathogenicity of entomopathogenic nematodes to subterranean termites (Isoptera).

Biocontrol of subterranean termites is largely impeded by their social immune responses. Studies on biocontrol agents combined with natural insecticides and their possible effects on the immune defense mechanisms of termites are limited. In this study, we investigated the effects of a combined biocontrol strategy using a plant-derived insect ATPase inhibitor, α-terpineol, with the entomopathogenic nematodes (EPNs) Steinernema carpocapsae against the subterranean termite Coptotermes formosanus Shiraki. Survival assays showed that even a low lethal concentration of α-terpineol significantly increased the EPNs-induced virulence in C. formosanus. α-terpineol treatment majorly inhibited the activity of Na+- K+- ATPase, which disturbed the EPNs-induced enhancement of locomotor activity and grooming behavior in termites treated with the combined strategy. Furthermore, the combination treatment had a synergistic inhibitory effect on innate immune responses in C. formosanus, which were measured as changes in the expression of immune-related genes and activities of immune system enzymes. In conclusion, α-terpineol can weaken the immune defense of termites against EPNs at low lethal concentrations, and is a suitable non-synthetic insecticide to prove the biocontrol efficiency of EPNs on C. formosanus. This study provides a theoretical basis and technical reference for a novel biocontrol strategy that promises to overcome the problems of host immune defense in termites.

Assessment of cytisine as an insecticide candidate for Hyphantria cunea management: Toxicological, biochemical, and control potential insights.

In the present study, the toxicological effects of cytisine on the H. cunea larvae were investigated, and the potential of cytisine as a botanical insecticide through field simulation experiments was evaluated. The results showed that cytisine treatment (0.25-2.5%) exerted significant biotoxic effects on the H. cunea larvae, including diminished weight, disruption of both positive (HcCKS1, HcPLK, HcCCNA) and negative (HcGADD and HcCDKN) regulatory genes associated with larval growth, increased mortality, and heightened oxidative damage (H2O2 and MDA). Cytisine treatment significantly reduced glucose content and inhibited the expression of key rate-limiting enzyme genes (HcPFK, HcPK, HcHK1, HcCS, and HcIDH2) within glycolysis and the tricarboxylic acid cycle pathways. Under cytisine treatment, detoxification enzyme activities (CarE and GST) and expression of detoxification genes (HcCarE1, HcCarE2, HcCarE3, HcGST1, and HcGST3) were inhibited in H. cunea larvae. An increased contents of SOD, CAT, ASA and T-AOC, as well as expression of antioxidant enzyme genes HcSOD1 and HcCAT2, was found in cytisine-treated H. cunea larvae. Simultaneously, this is accompanied by a significant reduction in the expression of four antioxidant enzyme genes (e.g., HcPOD1 and HcPOD2). In the field experiment, a cytisine aqueous solution (25 g/L) with pre-sprayed and directly sprayed ways demonstrated potent insecticidal activity against H. cunea larvae, achieving a mortality rate of 53.75% and 100% at 24 h, respectively. Taken together, cytisine has significantly weight inhibition and lethal toxicity on the H. cunea larvae, and can be developed as a botanical insecticide for H. cunea control.

Rotenone nanoparticles based on mesoporous silica to improve the stability, translocation and insecticidal activity of rotenone.

Nanotechnology has been widely applied for pesticide carriers, which is an important way to improve the utilization, stability, and sustained release of pesticides. Mesoporous silica nanoparticles (MSNs) are a nanomaterial with adjustable particle and pore sizes, with a high specific surface area and good biocompatibility. Rotenone is a non-systemic botanical insecticide that is easily degraded in the environment. We used a modified soft-template method to prepare MSNs, in which rotenone was loaded using the solvent evaporation method. The prepared rotenone nanopesticide based on mesoporous silica showed considerable drug loading rates of 33.2%. Moreover, the prepared rotenone nanoparticles showed improved photostability and sustained release behavior, which improved the translocation of rotenone in tomato plants. Finally, the rotenone nanoparticles displayed superior insecticidal activity compared to traditional preparations. In summary, the rotenone nanopesticide improved the persistence and utilization rates of rotenone. These findings are of significance in reducing pesticide usage, mitigating environmental pollution, and ensuring food safety.

Research status of ginger insecticidal components in botanical insecticides.

The development and application of botanical insecticides is important for the sustainable development of green agriculture. The abuse of chemical pesticides has caused serious problems of environment and human health. Botanical insecticides have become an environment-friendly insecticides due to their nature, low toxicity, easy degradation and other advantages, which are an important field of insecticide development in the future. Although botanical insecticides have lots of advantages, there are still problems needed to be resolved, such as insecticidal plant species, impact assessment of botanical pesticide and separation and purification of active components. To excavate the resources of highly effective insecticidal plants and understand the mechanism of botanical insecticides, here we reviewed the progress of resources and active components of botanical insecticides, the mechanisms of action of botanical insecticides, the main active components and insecticidal properties of Zingiber officinale. Finally, we analyzed the difficulties faced in the research and development of botanical insecticides, prospected future directions, and discussed the active components of ginger. This review would provide reference for the deve-lopment of new botanical insecticides.

Life-table parameters, functional response, flight ability, and cross-generational effects of matrine demonstrate its safety to Hippodamia variegata (Coleoptera: Coccinellidae).

In Xinjiang's cotton growing area of China, previous studies have shown that matrine is a selective botanical insecticide, with high toxicity to Aphis gossypii Glover (Hemiptera: Aphididae) and low toxicity to its dominant natural enemy, Hippodamia variegata Goeze (Coleoptera: Coccinellidae). However, lethal effects alone are not sufficient evidence to justify introducing matrine into local IPM strategies. In this context, we systematically evaluated the safety of matrine to H. variegata by investigating the effects of contact and stomach toxicity of matrine on the lady beetle's life-table parameters, predatory ability, flight ability of parental adults, and cross-generational effects on life-table parameters of the predator's offspring. We found that matrine at 2,000 mg/l did not have any significant negative effects to adult fecundity, longevity, or the predatory capacity of parental adults of H. variegata. Moreover, it is the same for cross-generational effects of matrine on H. variegate. The contact toxicity of matrine significantly reduced the flight time of H. variegata males, but did not significantly affect flight time and average velocity. Our results support the view that matrine is safe to H. variegata and can be recommended for use in the local IPM strategy for control of A. gossipii.

Toxicity, baseline of susceptibility, detoxifying mechanism and sublethal effects of chlorogenic acid, a potential botanical insecticide, on Bemisia tabaci.

Bemisia tabaci is a threat to agriculture worldwide because of its potential to cause devastating damage to crops. Chlorogenic acid is a bioactive pesticidal phytochemical agent against various insect pests. We here determined the susceptibility of a laboratory strain of B. tabaci to chlorogenic acid and other popular insecticides, and the susceptibility of several field-collected populations to chlorogenic acid. Also, cross-resistance to four common insecticides was measured. Chlorogenic acid had the highest toxicity of all tested insecticides, and all the field-collected populations were susceptible to chlorogenic acid, and little cross-resistance was detected between chlorogenic acid and the other tested insecticides. Furthermore, analysis of enzyme activities and expression of P450 genes in B. tabaci after treatment with LC50 of chlorogenic acid suggested that enhanced P450 activity could be involved in chlorogenic acid detoxification. We subsequently evaluated sublethal effects of chlorogenic acid, and found that treatment with LC25 of chlorogenic acid prolonged duration of two developmental stages, reduced fecundity, and decreased survival rates of treated B. tabaci compared to untreated insects. Overall, these findings demonstrate strong toxicity and significant sublethal effects of chlorogenic acid on B. tabaci, and suggest that overexpression of P450 genes may be associated with chlorogenic acid detoxification.

Role of DSC1 in Drosophila melanogaster synaptic activities in response to haedoxan A.

Drosophila sodium channel 1 (DSC1) encodes a voltage-gated divalent cation channel that mediates neuronal excitability in insects. Previous research revealed that DSC1 knockout Drosophila melanogaster conferred different susceptibility to insecticides, which indicated the vital regulation role of DSC1 under insecticide stress. Haedoxan A (HA) is a lignan compound isolated from Phryma leptostachya, and we found that HA has excellent insecticidal activity and is worthy of further study as a botanical insecticide. Herein, we performed bioassay and electrophysiological experiments to test the biological and neural changes in the larval Drosophila with/without DSC1 knockout in response to HA. Bioassay results showed that knockout of DSC1 reduced the sensitivity to HA in both w1118 (a common wild-type strain in the laboratory) and parats1 (a pyrethroid-resistant strain) larvae. Except for parats1 /DSC1-/- , electrophysiology results implicated that HA delayed the decay rate and increased the frequency of miniature excitatory junctional potentials of Drosophila from w1118 , parats1 , and DSC1-/- strains. Moreover, the neuromuscular synapse excitatory activities of parats1 /DSC1-/- larvae were more sensitive to HA than DSC1-/- larvae, which further confirmed the functional contribution of DSC1 to neuronal excitability. Collectively, these results indicated that the DSC1 channel not only regulated the insecticidal activity of HA, but also maintained the stability of neural circuits through functional interaction with voltage-gated sodium channels. Therefore, our study provides useful information for elucidating the regulatory mechanism of DSC1 in the neural system of insects involving the action of HA derived from P. leptostachya.

Chemical Profiles and Lethal Toxicities of Native Botanical Insecticides for the Control of Musca domestica Linnaeus and Stomoxys indicus Picard (Diptera: Muscidae) in Songkhla Province, Thailand.

Livestock farming is currently reducing the use of synthetic insecticides because of the development of resistance in insect pests. Plant-based bioinsecticides are considered alternatives to synthetic pesticides. Therefore, the present study investigated the chemical composition and discriminating concentrations (DCs) of essential oils from Syzygium aromaticum (L.) Merr. and L. M. Perry (SA), Cinnamomum porrectum (Roxb.) Kosterm (CP), and Litsea cubeba (Loureiro) Persoon (LC) against laboratory-reared Musca domestica (larvae and adults) and field-derived Stomoxys indicus (adults) using larval dip and adult contact bioassays. All essential oils were analyzed using gas chromatography/mass spectroscopy. The most common components in the SA, CP, and LC oils were eugenol, safrole, and terpenoids, respectively. The results of a larval test indicated that CP was most effective against M. domestica with a DC of 6.134% v/v. In adult bioassays, CP was also the most toxic oil against M. domestica (DC = 30.644% v/v), whereas SA displayed the greatest toxicity against S. indicus (DC = 1.434% v/v). Moreover, in the larval bioassay results of oils tested at 1, 5, and 10% v/v in M. domestica, 1% and 5% v/v CP had the shortest median lethal times values of 68.88 and 19.44 min, respectively, whereas, at 10% v/v, SA displayed the shortest median lethal time (0.03 min), followed by CP (1.74 min) and LC (19.02 min). However, additional data are needed to further evaluate the semi-field and field effects of CP and SA on M. domestica and S. indicus under realistic operational conditions.

Toxicological and molecular adverse effect of Illicium verum fruit constituents toward Bradysia procera.

BACKGROUND: Bradysia procera, a ginseng stem fungus gnat, is one of the most serious insect pests of Korean ginseng (Panax ginseng), causing significant damage to plant growth. The goal of this study was to determine the toxicity and mechanism of action of phenylpropanoids (trans-anethole and estragole) isolated from the methanol extract and hydrodistillate of Illicium verum fruit against third-instar larvae and eggs of Bradysia procera. RESULTS: The filter-paper mortality bioassay revealed that estragole [median lethal concentration (LC50 ) = 4.68 g/cm2 ] has a significant fumigant effect, followed by trans-anethole (LC50 = 43.92 g/cm2 ). However, estragole had the lowest toxic effect when compared to commercially available insecticides. After 7 days, estragole and trans-anethole at 75 g/cm2 inhibited egg hatchability up to 97% and 93%, respectively. At 0.09 g/cm2 , insecticides had an inhibitory effect on egg-hatching ability ranging from 88% to 94%. Furthermore, in both closed and open containers, these active constituents were able to consistently induce vapor-phased toxicity. Both estragole and trans-anethole have the ability to inhibit acetylcholinesterase (AChE), which is involved in neurotransmitter function. However, the active constituent estragole from I. verum fruit acted as a potent AChE inhibitor and had a slightly lower effect on cyclic adenosine monophosphate (AMP) than octopamine alone. CONCLUSION: This finding suggests that estragole may influence Bradysia procera neurotransmitter function via both the AChE and octopaminergic receptors. More research is needed to demonstrate the potential applications of I. verum fruit-derived products as potential larvicides and ovicides for Bradysia procera population control. © 2022 Society of Chemical Industry.

Potent insecticidal activity of Eleocharis dulcis (Burm. f.) Trin peel extract and its main components against aphids.

BACKGROUND: Aphids are significant pests of cash crops and food farm crops. Botanical insecticides are safe for aphid control, especially for organic farming. In this study, Eleocharis dulcis (Burm. f.) Trin. peel extract (EDPE), a new botanical insecticide, was investigated for its active compositions against several agricultural aphids. RESULTS: The results showed that the EDPE had high insecticidal activity against Sitobion avenae Fabricius, Aphis gossypii Glover, Megoura crassicauda Mordvilko, and Acyrthosiphon pisum Harris, with half-lethal concentration (LC50 ) values of 95.92, 81.04, 140.31, and 255.73 mg/L after 48 h of treatment. In the pot culture assay, the aphicidal effects of 25% EDPE soluble liquid (SL) at a concentration of 0.016% were 68.98 ± 5.61%, 79.33 ± 8.27%, and 88.82 ± 3.91% after the first, third, and seventh days of treatment, respectively. Nine compounds were identified by bioactivity-directed fractionation: 4',5'-dimethoxy-6,6-dimethylpyranoisoflavone (1), 3-methoxy-4-hydroxylonchocarpin (2), 4-hydroxylonchocarpin (3), 4-methoxylonchocarpin (4), barbigerone (5), lonchocarpusone (6), 6a,12a-dehydrodeguelin (7), 13-homo-13-oxa-6a, 12a-dehydrodeguelin (8) and deguelin (9). Among them, 4-hydroxylonchocarpin (3) showed the highest aphidicidal activity against M. crassicauda, S. avenae, and A. pisum, with LC50 values of 97.24, 140.63, and 112.31 mg/L, respectively. CONCLUSION: These data contribute to a better understanding of the aphicidal activity of EDPE and its main component, 4-hydroxylonchocarpin. This will help to develop new botanical insecticides to contro aphids. © 2022 Society of Chemical Industry.

Synergistic modes of interaction between the plant essential oils and the respiratory blocker chlorfenapyr.

Plant essential oils are widely acknowledged for their insecticidal activities and synergistic interaction with conventional insecticides, but their insecticidal modes of action and the mechanism of synergy remain less understood. In this study, electrophysiological screenings on the larval central nervous system (CNS) of the common fruit fly, Drosophila melanogaster, and the housefly, Musca domestica, were conducted to identify the neurophysiological effects of the oils and their major constituents. Several oils changed the firing rate of the central motor neurons, and four oils were selected to determine their major active compounds. Eugenol and thymol (87.2% and 31.1% in clove bud and thyme oils, respectively) were inhibitory to the nerve firing rates of the CNS, and exhibited synergistic toxicity to the housefly when blended with a respiratory blocking pyrrole insecticide, chlorfenapyr. On the other hand, trans-cinnamaldehyde and terpinen-4-ol (74.6% and 52.0% in cinnamon and teatree oils) seemed excitatory to the nerves, and displayed antagonistic interaction to chlorfenapyr in their insecticidal activity. Chlorfenapyr led to ATP depletion in the insects, and the inhibitory compounds accelerated the process. On the other hand, nerve-excitatory compounds seemed to nullify the depletion. This was further confirmed with the two CNS-excitatory synthetic insecticides, permethrin and chlorpyrifos, that they exhibited antagonistic toxicity when mixed with chlorfenapyr. Meanwhile, the synergy between the inhibitory compounds and chlorfenapyr was diminished when ATP was artificially injected, indicating that the bioenergetic effects of neuroinhibitors are responsible for their synergistic interactions.

Glutathione S-Transferase May Contribute to the Detoxification of (S)-(-)-Palasonin in Plutella xylostella (L.) via Direct Metabolism.

The control of P. xylostella primarily involves chemical insecticides, but overuse has brought about many negative effects. Our previous study reported that (S)-(-)-palasonin (PLN) is a plant-derived active substance with significant insecticidal activity against P. xylostella. However, we noticed a possible cross-resistance between (S)-(-)-palasonin and other insecticides which may be related to metabolic detoxification. In order to further explore the detoxification effect of detoxification enzymes on (S)-(-)-palasonin in P. xylostella, the effects of (S)-(-)-palasonin on enzyme activity and transcription level were determined, and the detoxification and metabolism of GSTs on (S)-(-)-palasonin were studied by in vitro inhibition and metabolism experiments. During this study, GST enzyme activity was significantly increased in P. xylostella after (S)-(-)-palasonin treatment. The expression levels of 19 GSTs genes were significantly increased whereas the expression levels of 1 gene decreased. Furthermore, (S)-(-)-palasonin is shown to be stabilized with GSTs and metabolized GSTs (GSTd1, GSTd2, GSTs1 and GSTs2) in vitro, with the highest metabolic rate of 80.59% for GSTs1. This study advances the beneficial utilization of (S)-(-)-palasonin as a botanical pesticide to control P. xylostella in the field.

Plant volatile compound methyl benzoate is highly effective against Spodoptera frugiperda and safe to non-target organisms as an eco-friendly botanical-insecticide.

Recent studies have indicated that the plant volatile methyl benzoate (MB) exhibits significant insecticidal bioactivity against several common insects. However, the potential environmental hazards of MB and its safety to non-target organisms is poorly understood. In the present study, these characteristics were investigated through laboratory experiments and field investigations. The results revealed that MB was highly toxic to the agricultural pest, fall armyworm Spodoptera frugiperda. Compared with the commercial pesticide lambda-cyhalothrin, the toxicities of MB against S. frugiperda larvae and adults were comparable and 3.41 times higher, respectively. Behavioral bioassays showed that the percentage repellency of MB to S. frugiperda larvae was 56.72 %, and MB induced 69.40 % oviposition deterrence rate in S. frugiperda female adults. Furthermore, in terms of median lethal concentration (LC50) and median lethal doses (LD50), MB exhibited non-toxic effects on non-target animals with 3-d LC50 of > 1 % to natural predators (Coccinella septempunctata and Harmonia axyridis), 3-d LD50 of 467.86 µg/bee to the bumblebee Bombus terrestris, 14-d LC50 of 971.09 mg/kg to the earthworm Eisenia fetida, and 4-d LC50 of 47.30 mg/L to the zebrafish Brachydanio rerio. The accumulation of MB in the soil and earthworms was found to be extremely limited. Our comparative study clearly demonstrated that MB is effective as a selective botanical pesticide against S. frugiperda and it is safe to use in the tested environment, with no toxic effects on non-target animals and natural predators.

Insect repellent pellets - an application of botanicals against red flour beetle - their antifungal activity during storage and use as potential fumigants.

BACKGROUND: The protection of grains from insect infestation is critical during storage. Insect repellent pellets (IRPs) are a potential technique to repel insects by hindering insect movement toward the grains. The basic principle of IRPs is the use of active components found in the oils of lemongrass, eucalyptus, and neem leaves for the controlled release of fumes, thereby avoiding the need for reapplication after a few days. Here, we examined the antifungal activity, the lethal dose, and the repelling effect of IRPs against red flour beetle, Tribolium castaneum, over a 30 day period. RESULTS: We observed that IRPs possessed antifungal properties and were able to repel the adults of T. castaneum. These insects ultimately died from the fumes if they manage to stay near the IRPs (LD50 = 2 and LD99 = 7 days). The active components (phenol, 2,4-di-tert-butyl-, citral, neral, geraniol, n-hexadecanoic acid) present in IRP during the initial stage were also found after a storage period of 35 days. CONCLUSION: The active components present in IRPs have antifungal, repellent, and fumigant properties. The IRPs can thus be termed potent botanical insecticides and are an alternative to synthetic insecticides. © 2022 Society of Chemical Industry.

Aphicidal activity of farnesol against the green peach aphid - Myzus persicae.

BACKGROUND: Myzus persicae (Hemiptera: Aphididae) is considered one of most important agricultural pests in the world. It is one of the main pests in protected pepper crops under glasshouse conditions in Southeastern Spain, but its control is limited as a consequence of the few available authorized insecticides and their incompatibility with the natural enemies. Some essential oils and pure compounds such as anise (Pimpinella anisum) or farnesol are repellent and/or toxic to aphids. Their use as a botanical insecticides can be an alternative for aphid control in pepper. RESULTS: The effect of farnesol was evaluated against M. persicae in a new bioassay developed to test the contact effect (aqueous formulation of the products) on aphids in laboratory conditions. Aniseed essential oil, geraniol and (Z)-jasmone at 0.6% causes an aphid mortality of >50%; and farnesol was the most effective (93.67% mortality). Farnesol nanoemulsions between 0.2% and 0.6% were formulated with an IKA-Labor Pilot dispersing machine (7940 rpm for 10 min) using Tween 80 as a surfactant. These formulations were tested on field experiments (glasshouse conditions) on pepper crops for 2 years. Foliar applications of farnesol at a concentration of 0.4% in field conditions causes a high reduction in aphid populations, with efficacies of ≈70-80% with respect to the control, similar to or even higher than the efficacy of the reference pyrethrin insecticide. CONCLUSION: Farnesol showed a great aphicidal effect against M. persicae. The use of this molecule in integrated pest management programs combined with natural enemies is a good option for future control of M. persicae. © 2022 Society of Chemical Industry.

Negative cross-resistance of a pyrethroid-resistant Drosophila mutant to Phryma leptostachya-derived haedoxan A.

Voltage-gated sodium channels are the primary target of pyrethroid insecticides. Mutations in sodium channel confer knockdown resistance (kdr) to pyrethroids in various arthropod pests. Haedoxan A (HA) is the major insecticidal component from Phryma leptostachya. It has been shown that HA alters electrical responses at the Drosophila neuromuscular junction and modifies the gating properties of cockroach sodium channels expressed in Xenopus oocytes. However, whether sodium channel mutations that confer pyrethroid resistance also affect the action of HA is unknown. In this study, we conducted bioassays using HA and permethrin in two Drosophila melanogaster strains: w1118 , an insecticide-susceptible strain, and parats1 , a pyrethroid-resistant strain due to a I265N mutation in the sodium channel, and identified a new case of negative cross-resistance (NCR) between permethrin and HA. Both parats1 larvae and adults were more resistant to permethrin, as expected. However, both parats1 larvae and adults were more sensitive to HA compared to w1118 . We confirmed that the I265N mutation reduced the sensitivity to permethrin of a Drosophila sodium channel variant, DmNav 22, expressed in Xenopus oocytes. Interestingly, the I265N mutation also abolished the effect of HA on sodium channels. Further characterization showed that I265 on the sodium channels is critical for the action of both pyrethroids and HA on sodium channels, pointing to an overlapping mode of action between pyrethroids and HA on the sodium channel. Overall, our results suggest an I265N-independnt mechanism(s) in parats1 flies that is responsible for the NCR between permethrin and HA at the whole insect level.

Insecticidal activity of the essential oil of Piper corcovadensis leaves and its major compound (1-butyl-3,4-methylenedioxybenzene) against the maize weevil, Sitophilus zeamais.

BACKGROUND: Sitophilus zeamais is one of the most economically impactful pests, attacking various grains and processed foods. Control of this insect has been achieved using synthetic insecticides, exacerbated and careless use of which has led to the development of resistant insect populations, toxicity to non-target organisms and environmental contamination. In this study, Piper corcovadensis leaf essential oil (PcLEO) and its major compound, 1-butyl-3,4-methylenedioxybenzene (BMDB), were investigated as alternative insecticidal agents against S. zeamais. RESULTS: Characterization of PcLEO showed the presence of 40 compounds. The major components were the phenylpropanoid BMDB (35.77%) and the monoterpenes α-pinene (14.95%) and terpinolene (6.23%). PcLEO and BMDB were toxic by fumigation (half-maximal lethal concentration [LC50 ]: 9.46 and 0.85 µl L-1 of air, respectively), by contact (half-maximal lethal dose [LD50 ]: 9.38 and 6.16 µg g-1 of insect, respectively) and ingestion (LC50 : 16.04 and 14.30 mg g-1 , respectively). In the ingestion test, both PcLEO and BMDB promoted the loss of insect biomass and had a strong deterrent effect. In addition, both were able to inhibit trypsin and α-amylase activities. CONCLUSION: PcLEO and BMDB exhibited insecticidal activity against S. zeamais, with a toxic effect by fumigation, contact and ingestion, in addition to food deterrence and inhibiting trypsin and α-amylase activities, suggesting their potential for use in the control of this pest.