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1.
J Agric Food Chem ; 72(20): 11331-11340, 2024 May 22.
Artigo em Inglês | MEDLINE | ID: mdl-38721769

RESUMO

Research on mesoionic structures in pesticide design has gained significant attention in recent years. However, the 1-position of pyridino[1,2-a]pyrimidine is usually designed with 2-chlorothiazole, 2-chloropyridine, or cyano moieties commonly found in neonicotinoid insecticides. In order to enrich the available pharmacophore library, here, we disclose a series of new pyridino[1,2-a]pyrimidine mesoionics bearing indole-containing substituents at the 1-position. Most of these target compounds are confirmed to have good insecticidal activity against aphids through bioevaluation. In addition, a three-dimensional structure-activity relationship model is established to allow access to optimal compound F45 with an LC50 value of 2.97 mg/L. This value is comparable to the property achieved by the positive control triflumezopyrim (LC50 = 2.94 mg/L). Proteomics and molecular docking analysis suggest that compound F45 has the potential to modulate the functioning of the aphid nervous system through its interaction with neuronal nicotinic acetylcholine receptors. This study expands the existing pharmacophore library for the future development of new mesoionic insecticides based on 1-position modifications of the pyridino[1,2-a]pyrimidine scaffold.


Assuntos
Afídeos , Desenho de Fármacos , Indóis , Inseticidas , Simulação de Acoplamento Molecular , Pirimidinas , Inseticidas/química , Inseticidas/síntese química , Inseticidas/farmacologia , Animais , Pirimidinas/química , Pirimidinas/farmacologia , Pirimidinas/síntese química , Afídeos/efeitos dos fármacos , Indóis/química , Indóis/farmacologia , Indóis/síntese química , Relação Estrutura-Atividade , Estrutura Molecular , Receptores Nicotínicos/metabolismo , Receptores Nicotínicos/química , Receptores Nicotínicos/efeitos dos fármacos
2.
Int J Mol Sci ; 25(9)2024 Apr 28.
Artigo em Inglês | MEDLINE | ID: mdl-38732039

RESUMO

Hesperidin is a highly bioactive natural flavonoid whose role in ecological interactions is poorly known. In particular, the effects of hesperidin on herbivores are rarely reported. Flavonoids have been considered as prospective biopesticides; therefore, the aim of the present study was to examine the influence of hesperidin on the host plant selection behavior of three aphid (Hemiptera: Aphididae) species: Acyrthosiphon pisum Harrris, Rhopalosiphum padi (L.), and Myzus persicae (Sulz.). The aphid host plants were treated with 0.1% and 0.5% ethanolic solutions of hesperidin. Aphid probing behavior in the no-choice experiment was monitored using electropenetrography and aphid settling on plants in the choice experiment was recorded. The results demonstrated that hesperidin can be applied as a pre-ingestive, ingestive, and post-ingestive deterrent against A. pisum, as an ingestive deterrent against R. padi, and as a post-ingestive deterrent against M. persicae using the relatively low 0.1% concentration. While in A. pisum the deterrent effects of hesperidin were manifested as early as during aphid probing in peripheral plant tissues, in M. persicae, the avoidance of plants was probably the consequence of consuming the hesperidin-containing phloem sap.


Assuntos
Afídeos , Hesperidina , Afídeos/efeitos dos fármacos , Afídeos/fisiologia , Animais , Hesperidina/farmacologia , Hesperidina/química , Especificidade da Espécie , Comportamento Alimentar/efeitos dos fármacos , Herbivoria/efeitos dos fármacos , Comportamento Animal/efeitos dos fármacos
3.
Sci Rep ; 14(1): 9392, 2024 04 24.
Artigo em Inglês | MEDLINE | ID: mdl-38658769

RESUMO

A series of arecoline derivatives with amino acid moieties were designed and synthesised using an acylamide condensation strategy, taking arecoline as the foundational structure. The insecticidal efficacy of these compounds against Aphis craccivora and Tetranychus cinnabarinus was evaluated. Notably, derivatives 3h and 3i demonstrated superior insecticidal activity compared with arecoline. Additionally, 3h and 3i showed good fungicidal effectiveness against two types of plant fungi. Moreover, molecular docking analyses suggested that 3h and 3i could affect the nervous systems of A. craccivora and T. cinnabarinus by binding to neuronal nicotinic acetylcholine receptors. These findings suggest that compounds 3h and 3i represent promising leads for further development in insecticide and fungicide research.


Assuntos
Aminoácidos , Antifúngicos , Desenho de Fármacos , Inseticidas , Simulação de Acoplamento Molecular , Inseticidas/farmacologia , Inseticidas/síntese química , Inseticidas/química , Animais , Antifúngicos/farmacologia , Antifúngicos/síntese química , Antifúngicos/química , Aminoácidos/química , Afídeos/efeitos dos fármacos , Tetranychidae/efeitos dos fármacos , Relação Estrutura-Atividade , Receptores Nicotínicos/metabolismo , Receptores Nicotínicos/química , Testes de Sensibilidade Microbiana
4.
Ecotoxicol Environ Saf ; 276: 116291, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38581910

RESUMO

Myzus persicae is an important pest that has developed resistance to nearly all currently used insecticidal products. The employment of insecticide synergists is one of the effective strategies that need to be developed for the management of this resistance. Our study showed that treatment with a combination of the antibiotic, rifampicin, with imidacloprid, cyantraniliprole, or clothianidin significantly increased their toxicities against M. persicae, by 2.72, 3.59, and 2.41 folds, respectively. Rifampicin treatment led to a noteworthy reduction in the activities of multifunctional oxidases (by 32.64%) and esterases (by 23.80%), along with a decrease in the expression of the CYP6CY3 gene (by 58.57%) in M. persicae. It also negatively impacted the fitness of the aphids, including weight, life span, number of offspring, and elongation of developmental duration. In addition, bioassays showed that the combination of rifampicin and a detoxification enzyme inhibitor, piperonyl butoxide, or dsRNA of CYP6CY3 further significantly improved the toxicity of imidacloprid against M. persicae, by 6.19- and 7.55-fold, respectively. The present study suggests that development of active ingredients such as rifampicin as candidate synergists, show promise to overcome metabolic resistance to insecticides in aphids.


Assuntos
Afídeos , Guanidinas , Inseticidas , Neonicotinoides , Nitrocompostos , Butóxido de Piperonila , Rifampina , Tiazóis , Animais , Rifampina/toxicidade , Rifampina/farmacologia , Afídeos/efeitos dos fármacos , Inseticidas/toxicidade , Neonicotinoides/toxicidade , Nitrocompostos/toxicidade , Tiazóis/toxicidade , Guanidinas/toxicidade , Butóxido de Piperonila/toxicidade , Pirazóis/toxicidade , Sinergismo Farmacológico , Resistência a Inseticidas/genética , Sinergistas de Praguicidas/toxicidade , ortoaminobenzoatos/toxicidade , Esterases/metabolismo
5.
Arch Insect Biochem Physiol ; 115(4): e22112, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38605672

RESUMO

Insect trehalases have been identified as promising new targets for pest control. These key enzymes are involved in trehalose hydrolysis and plays an important role in insect growth and development. In this contribution, plant and microbial compounds, namely validamycin A, amygdalin, and phloridzin, were evaluated for their effect, through trehalase inhibition, on Acyrthosiphon pisum aphid. The latter is part of the Aphididae family, main pests as phytovirus vectors and being very harmful for crops. Validamycin A was confirmed as an excellent trehalase inhibitor with an half maximal inhibitory concentration and inhibitor constant of 2.2 × 10-7 and 5 × 10-8 M, respectively, with a mortality rate of ~80% on a A. pisum population. Unlike validamycin A, the insect lethal efficacy of amygdalin and phloridzin did not correspond to their trehalase inhibition, probably due to their hydrolysis by insect ß-glucosidases. Our docking studies showed that none of the three compounds can bind to the trehalase active site, unlike their hydrolyzed counterparts, that is, validoxylamine A, phloretin, and prunasin. Validoxylamine A would be by far the best trehalase binder, followed by phloretin and prunasin.


Assuntos
Afídeos , Trealase , Animais , Amigdalina , Afídeos/efeitos dos fármacos , Afídeos/enzimologia , Inositol/análogos & derivados , Nitrilas , Floretina , Florizina , Trealase/antagonistas & inibidores
6.
Pestic Biochem Physiol ; 201: 105894, 2024 May.
Artigo em Inglês | MEDLINE | ID: mdl-38685221

RESUMO

Rhopalosiphum padi is a global pest that poses a significant threat to wheat crops and has developed resistance to various insecticides. G protein-coupled receptors (GPCRs), known for their crucial role in signaling and biological processes across insect species, have recently gained attention as a potential target for insecticides. GPCR has the potential to contribute to insect resistance through the regulation of P450 gene expression. However, GPCRs in R. padi remained unexplored until this study. We identified a total of 102 GPCRs in R. padi, including 81 receptors from family A, 10 receptors from family B, 8 receptors from family C, and 3 receptors from family D. Among these GPCR genes, 16 were up-regulated in both lambda-cyhalothrin and bifenthrin-resistant strains of R. padi (LC-R and BIF-R). A relaxin receptor gene, RpGPCR41, showed the highest up-regulated expression in both the resistant strains, with a significant increase of 14.3-fold and 22.7-fold compared to the susceptible strain (SS). RNA interference (RNAi) experiments targeting the relaxin receptor significantly increase the mortality of R. padi when exposed to the LC50 concentration of lambda-cyhalothrin and bifenthrin. The expression levels of five P450 genes (RpCYP6CY8, RpCYP6DC1, RpCYP380B1, RpCYP4CH2, and RpCYP4C1) were significantly down-regulated following knockdown of RpGPCR41 in LC-R and BIF-R strains. Our results highlight the involvement of GPCR gene overexpression in the resistance of R. padi to pyrethroids, providing valuable insights into the mechanisms underlying aphid resistance and a potential target for aphid control.


Assuntos
Afídeos , Resistência a Inseticidas , Inseticidas , Piretrinas , Receptores Acoplados a Proteínas G , Piretrinas/farmacologia , Piretrinas/toxicidade , Animais , Resistência a Inseticidas/genética , Inseticidas/farmacologia , Inseticidas/toxicidade , Receptores Acoplados a Proteínas G/genética , Receptores Acoplados a Proteínas G/metabolismo , Afídeos/efeitos dos fármacos , Afídeos/genética , Proteínas de Insetos/genética , Proteínas de Insetos/metabolismo , Interferência de RNA , Nitrilas/farmacologia , Nitrilas/toxicidade
7.
Pest Manag Sci ; 80(6): 2773-2784, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38298140

RESUMO

BACKGROUND: Pheromones have unique advantages for pest control. Current aphid pheromone research focuses on alarm and sex pheromones. However, practical applications are limited so far, as (E)-ß-farnesene has only been investigated to a small extent as an alarm pheromone and only male aphids are targeted by sex pheromones. Previous literature reports electrophysiological responses and repellent behavior of asexual aphids to nepetalactone (1B), therefore our objective was to modify nepetalactone's structure to identify key fragments responsible for repellent effects, as guidance for subsequent modifications and further investigation. RESULTS: In this study, seven derivatives were designed and synthesized based on nepetalactol (1A) and nepetalactone (1B) as lead compounds. Free-choice tests, conducted using cowpea aphids (Aphis craccivora), revealed that the lactone moiety was crucial for the repellent activity, and the removal of the carbonyl group eliminated the repelling effect. Compound (±)1I, an analogue of nepetalactone (1B), demonstrated a significantly higher repellent value than nepetalactone (1B) at three different concentrations, and even at 0.1 mg/mL it maintained a considerable repellent effect (26.5%). Electrostatic potential and density functional theory calculations supported the importance of the carbonyl group for the repellent effects. CONCLUSION: The newly discovered para-pheromone (±)1I shows improved repellent effects and potential for development as a novel biological control agent. Based on our innovative findings, analogues with improved efficacy and properties can be designed and prepared. Our research contributes to understanding the effects of structural modifications on pheromone activity and properties, which is crucial for exploring novel pheromone-based products for crop protection. © 2024 Society of Chemical Industry.


Assuntos
Afídeos , Feromônios , Animais , Afídeos/efeitos dos fármacos , Feromônios/farmacologia , Masculino , Repelentes de Insetos/farmacologia , Repelentes de Insetos/química , Pironas/farmacologia , Pironas/química , Lactonas/farmacologia , Lactonas/química , Monoterpenos Ciclopentânicos , Feminino , Norbornanos/química , Norbornanos/farmacologia , Compostos Bicíclicos Heterocíclicos com Pontes
8.
Pest Manag Sci ; 80(6): 2991-2999, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38312069

RESUMO

BACKGROUND: Fusarium species are responsible for Fusarium head blight (FHB) in wheat, resulting in yield losses and mycotoxin contamination. Deoxynivalenol (DON) and enniatins (ENNs) are common mycotoxins produced by Fusarium, affecting plant, animal and human health. Although DON's effects have been widely studied, limited research has explored the impact of ENNs on insects. This study examines the influence of DON and enniatin B (ENB), both singularly and in combination, on the wheat aphid Sitobion avenae and one of its predators, the lacewing Chrysoperla carnea. RESULTS: When exposed to DON (100 mg L-1) or DON + ENB (100 mg L-1), S. avenae exhibited significantly increased mortality compared to the negative control. ENB (100 mg L-1) had no significant effect on aphid mortality. DON-treated aphids showed increasing mortality from 48 to 96 h. A dose-response relationship with DON revealed significant cumulative mortality starting at 25 mg L-1. By contrast, C. carnea larvae exposed to mycotoxins via cuticular application did not show significant differences in mortality when mycotoxins were dissolved in water but exhibited increased mortality with acetone-solubilized DON + ENB (100 mg L-1). Feeding C. carnea with aphids exposed to mycotoxins (indirect exposure) did not impact their survival or predatory activity. Additionally, the impact of mycotoxins on C. carnea was observed only with acetone-solubilized DON + ENB. CONCLUSIONS: These findings shed light on the complex interactions involving mycotoxins, aphids and their predators, offering valuable insights for integrated pest management strategies. Further research should explore broader ecological consequences of mycotoxin contamination in agroecosystems. © 2024 Society of Chemical Industry.


Assuntos
Afídeos , Depsipeptídeos , Tricotecenos , Animais , Afídeos/efeitos dos fármacos , Afídeos/crescimento & desenvolvimento , Tricotecenos/toxicidade , Depsipeptídeos/farmacologia , Comportamento Predatório/efeitos dos fármacos , Larva/crescimento & desenvolvimento , Larva/efeitos dos fármacos , Triticum , Insetos/efeitos dos fármacos , Cadeia Alimentar , Fusarium/efeitos dos fármacos
9.
Pest Manag Sci ; 80(6): 3000-3009, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38312101

RESUMO

BACKGROUND: To improve integrated pest management (IPM) performance it is essential to assess pesticide side effects on host plants, insect pests, and natural enemies. The green peach aphid (Myzus persicae Sulzer) is a major insect pest that attacks various crops. Aphidius gifuensis is an essential natural enemy of M. persicae that has been applied effectively in controlling M. persicae. Thiamethoxam is a neonicotinoid pesticide widely used against insect pests. RESULTS: The current study showed the effect of thiamethoxam against Solanum tuberosum, M. persicae, and A. gefiuensis and the physiological and molecular response of the plants, aphids, and parasitoids after thiamethoxam application. Thiamethoxam affected the physical parameters of S. tuberosum and generated a variety of sublethal effects on M. persicae and A. gefiuensis, including nymph development time, adult longevity, and fertility. Our results showed that different thiamethoxam concentrations [0.1, 0.5, and 0.9 µm active ingredient (a.i.)/L] on different time durations (2, 6, and 10 days) increased the antioxidant enzyme activities SOD, POD, and CAT of S. tuberosum, M. persicae, and A. gefiuensis significantly compared with the control. Our results also showed that different thiamethoxam concentrations (0.1, 0.5, and 0.9 µm a.i./L) on different time durations (2, 6, and 10 days) increased the expression of superoxide dismutase (SOD), peroxidase (POD), catalase (CAT), acetylcholinesterase (AChE), carboxylesterase (CarE) and glutathione-S-transferase (GST) genes of S. tuberosum, M. persicae, and A. gefiuensis compared with the control. CONCLUSION: Our findings reveal that using thiamethoxam at suitable concentrations and time durations for host plants and natural enemies may enhance natural control through the conservation of natural enemies by overcoming any fitness disadvantages. © 2024 Society of Chemical Industry.


Assuntos
Afídeos , Inseticidas , Neonicotinoides , Solanum tuberosum , Tiametoxam , Tiazóis , Animais , Afídeos/efeitos dos fármacos , Afídeos/genética , Solanum tuberosum/parasitologia , Inseticidas/farmacologia , Neonicotinoides/farmacologia , Tiazóis/farmacologia , Vespas/efeitos dos fármacos , Vespas/fisiologia , Oxazinas/farmacologia , Nitrocompostos/farmacologia , Ninfa/efeitos dos fármacos , Ninfa/crescimento & desenvolvimento , Ninfa/parasitologia
10.
Pest Manag Sci ; 80(6): 2929-2936, 2024 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-38285453

RESUMO

BACKGROUND: Alternatives to neonicotinoids against cereal aphids are needed to mitigate aphid resistance and non-target effects. The emulsifiable oil formulations of two Beauveria bassiana strains, namely Bb registered as a mycoinsecticide and TBb overexpressing an endogenous virulence factor, were tested for seasonal control of cereal aphids at the elongating (April 7) to milk ripening (May 12) stages of winter wheat crop in Yuhang, Zhejiang. Each of three field trials consisted of blank control and the treatments (three randomized 100-m2 plots per capita) of each fungal strain sprayed biweekly at rates of 1.0 × 1013 and 1.5 × 1013 conidia ha-1 and 10% imidacloprid WP sprayed biweekly at a label rate. RESULTS: Tiller infestation percentage and aphid density in the 5-week field trials after the first spray were reduced to 18.7-22.4% and 9.1-12.4 aphids per tiller in the fungal treatments, and 12.8-25.3% and 2.8-20.9 aphids per tiller in the chemical treatment, contrasting with 49.2-60.3% and 37.1-108.5 aphids per tiller in the control. Percent control efficacies (±SD) computed with weekly aphid densities over the period averaged 84.0 ± 1.6 and 85.3 ± 1.8 versus 78.0 ± 4.0 and 79.9 ± 3.2 in the high-rate versus low-rate treatments of Bb and TBb, respectively, and 84.5 ± 7.8 in the chemical treatment. Imidacloprid showed faster kill action but more variable efficacy than the fungal treatments throughout the trials. CONCLUSION: Either Bb or TBb formulation competes with imidacloprid in reducing percent infestation and aphid density. The overall efficacy was significantly higher in the treatments of TBb than of Bb. © 2024 Society of Chemical Industry.


Assuntos
Afídeos , Beauveria , Neonicotinoides , Nitrocompostos , Controle Biológico de Vetores , Animais , Afídeos/efeitos dos fármacos , Nitrocompostos/farmacologia , Beauveria/fisiologia , China , Inseticidas/farmacologia , Estações do Ano , Triticum , Óleos
11.
Pest Manag Sci ; 79(1): 55-67, 2023 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-36067067

RESUMO

BACKGROUND: Acyrthosiphon pisum Harris is the most destructive pest worldwide because of its ability to feed on plants directly and transmit plant viruses as a vector. This study aims to identify triterpenoid saponins from Oxytropis hirta Bunge as biopesticides to control aphids. RESULTS: Three new azukisapogenol triterpenoid saponins (1-3), a new pinoresinol lignan glycoside (8), and four known saponins (4-7) were identified from the root of O. hirta. Compounds 4-7 displayed significant aphicidal activities against A. pisum with oral toxicities (LC50  = 51.10-147.43 µg/mL, 72 h), deterrent effects (deterrence index = 1.00, 100-200 µg/mL, 24 h), and aphid reproduction inhibitory effects (inhibition rates = 75.91-86.73%, 400 µg/mL, 24 h), respectively. The carboxyl groups at C-3 GlcA and C-30 were functional groups for their aphicidal activities. The toxic symptoms caused by the optimal 5 involved insect body-color changes from light green to dark or gray-green, and then brown until death. The intestinal cavity, apical microvilli, nuclei, mitochondria, and electron dense granules in the midgut tissues of A. pisum were the target sites showing aphicidal activity. The suppression of pepsin and α-amylase, and the activation of lipase and trypsin could be the signs of organelle damage in the midgut tissues. CONCLUSION: Azukisapogenol triterpenoid saponins from O. hirta could be used as biopesticides to control aphids for their multiple efficacies, including oral toxicity, deterrent activity, and reproduction inhibitory activity. The toxic symptoms involved insect body-color changes. Midgut tissues and their related enzymes were the targets for saponins showing aphicidal activities. © 2022 Society of Chemical Industry.


Assuntos
Afídeos , Oxytropis , Saponinas , Animais , Afídeos/efeitos dos fármacos , Oxytropis/química , Triterpenos/química , Saponinas/química , Saponinas/farmacologia , Inseticidas/química , Inseticidas/farmacologia
12.
Sci Rep ; 12(1): 2827, 2022 02 18.
Artigo em Inglês | MEDLINE | ID: mdl-35181691

RESUMO

Afidopyropen, a novel insecticide, is a derivative of pyripyropene A, which is produced by the filamentous fungus Penicillium coprobium. Afidopyropen has strong insecticidal activity against aphids and is currently used as a control agent of sucking pests worldwide. In this study, we summarized the biological properties and field efficacies of its derivatives against agricultural pests using official field trials conducted in Japan. Afidopyropen showed good residual efficacies against a variety of aphids, whiteflies and other sucking pests under field conditions. Furthermore, toxicological studies revealed its safety profiles against nontarget organisms, such as the honeybee, natural enemies and other beneficial insects, as well as mammals. Thus, afidopyropen is a next-generation agrochemical for crop protection that has a low environmental impact.


Assuntos
Compostos Heterocíclicos de 4 ou mais Anéis/química , Inseticidas/química , Lactonas/química , Penicillium/metabolismo , Piridinas/metabolismo , Sesquiterpenos/metabolismo , Animais , Afídeos/efeitos dos fármacos , Compostos Heterocíclicos de 4 ou mais Anéis/farmacologia , Inseticidas/farmacologia , Japão , Lactonas/farmacologia , Penicillium/química , Piridinas/química , Sesquiterpenos/química
13.
Int J Mol Sci ; 23(4)2022 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-35216472

RESUMO

Chemosensory proteins (CSPs) are a class of transporters in arthropods. Deeper research on CSPs showed that CSPs may be involved in some physiological processes beyond chemoreception, such as insect resistance to pesticides. We identified two upregulated CSPs in two resistant strains of Aphis gossypii Glover. To understand their role in the resistance of aphids to pesticides, we performed the functional verification of CSP1 and CSP4 in vivo and in vitro. Results showed that the sensitivity of the thiamethoxam-resistant strain to thiamethoxam increased significantly with the silencing of CSP1 and CSP4 by RNAi (RNA interference), and the sensitivity of the spirotetramat-resistant strain to spirotetramat increased significantly with the silencing of CSP4. Transgenic Drosophila melanogaster expressing CSPs exhibited stronger resistance to thiamethoxam, spirotetramat, and alpha-cypermethrin than the control did. In the bioassay of transgenic Drosophila, CSPs showed different tolerance mechanisms for different pesticides, and the overexpressed CSPs may play a role in processes other than resistance to pesticides. In brief, the present results prove that CSPs are related to the resistance of cotton aphids to insecticides.


Assuntos
Afídeos/metabolismo , Compostos Aza/metabolismo , Resistência a Inseticidas , Proteínas de Membrana Transportadoras/metabolismo , Compostos de Espiro/metabolismo , Tiametoxam/metabolismo , Animais , Animais Geneticamente Modificados , Afídeos/efeitos dos fármacos , Afídeos/fisiologia , Drosophila melanogaster/genética , Proteínas de Insetos/metabolismo , Inseticidas/metabolismo
14.
Toxins (Basel) ; 14(1)2022 01 14.
Artigo em Inglês | MEDLINE | ID: mdl-35051034

RESUMO

Linear cationic venom peptides are antimicrobial peptides (AMPs) that exert their effects by damaging cell membranes. These peptides can be highly specific, and for some, a significant therapeutic value was proposed, in particular for treatment of bacterial infections. A prolific source of novel AMPs are arthropod venoms, especially those of hitherto neglected groups such as pseudoscorpions. In this study, we describe for the first time pharmacological effects of AMPs discovered in pseudoscorpion venom. We examined the antimicrobial, cytotoxic, and insecticidal activity of full-length Checacin1, a major component of the Chelifer cancroides venom, and three truncated forms of this peptide. The antimicrobial tests revealed a potent inhibitory activity of Checacin1 against several bacteria and fungi, including methicillin resistant Staphylococcus aureus (MRSA) and even Gram-negative pathogens. All peptides reduced survival rates of aphids, with Checacin1 and the C-terminally truncated Checacin11-21 exhibiting effects comparable to Spinosad, a commercially used pesticide. Cytotoxic effects on mammalian cells were observed mainly for the full-length Checacin1. All tested peptides might be potential candidates for developing lead structures for aphid pest treatment. However, as these peptides were not yet tested on other insects, aphid specificity has not been proven. The N- and C-terminal fragments of Checacin1 are less potent against aphids but exhibit no cytotoxicity on mammalian cells at the tested concentration of 100 µM.


Assuntos
Anti-Infecciosos , Proteínas de Artrópodes , Venenos de Artrópodes , Citotoxinas , Inseticidas , Sequência de Aminoácidos , Animais , Anti-Infecciosos/química , Anti-Infecciosos/farmacologia , Anti-Infecciosos/toxicidade , Afídeos/efeitos dos fármacos , Aracnídeos , Proteínas de Artrópodes/química , Proteínas de Artrópodes/farmacologia , Proteínas de Artrópodes/toxicidade , Venenos de Artrópodes/química , Venenos de Artrópodes/farmacologia , Venenos de Artrópodes/toxicidade , Citotoxinas/química , Citotoxinas/farmacologia , Citotoxinas/toxicidade , Cães , Inseticidas/química , Inseticidas/farmacologia , Inseticidas/toxicidade , Células Madin Darby de Rim Canino , Alinhamento de Sequência
15.
J Insect Sci ; 22(1)2022 Jan 01.
Artigo em Inglês | MEDLINE | ID: mdl-34958664

RESUMO

Plant essential oils, with high bioactivity and biodegradability, provide promising alternatives to synthetic pesticides for pest control. Trans-anethole is the major component of essential oil from star anise, Illicium verum Hook. The compound has a strong contact toxicity against the green peach aphid, Myzus persicae (Sulzer) (Hemiptera: Aphididae), which is a major insect pest of many vegetables and crops. However, little information is known about how M. persicae responds to trans-anethole at the molecular level. We conducted a comparative transcriptome analysis of M. persicae in response to a LD50 dose of trans-anethole. A total of 559 differentially expressed genes were detected in the treated individuals, with 318 genes up-regulated, and 241 genes down-regulated. Gene ontology (GO) analysis revealed that these genes were classified into different biological processes and pathways. We also found that genes encoding ATP-binding cassette (ABC) transporters, DnaJ, and cuticle proteins were dramatically up-regulated in response to trans-anethole. To study the function of these genes, we performed RNA interference (RNAi) analysis. Knockdown of an ABC transporter gene (ABCG4) and a DnaJ gene (DnaJC1) resulted in a significantly increased mortality rate in M. persicae following trans-anethole exposure, indicating the involvement of these two genes in the toxicity response to trans-anethole. The findings provide new insights into the mechanisms of M. persicae in coping with plant essential oils.


Assuntos
Derivados de Alilbenzenos , Anisóis , Afídeos , Proteínas de Insetos/genética , Óleos Voláteis , Derivados de Alilbenzenos/farmacologia , Animais , Anisóis/farmacologia , Afídeos/efeitos dos fármacos , Afídeos/genética , Expressão Gênica , Óleos Voláteis/farmacologia
16.
Anal Biochem ; 639: 114522, 2022 02 15.
Artigo em Inglês | MEDLINE | ID: mdl-34883071

RESUMO

Insect cytochrome P450 plays major roles in detoxification of phytotoxin and insecticides. However, determination of P450 activity in aphids has variable success and there is no reliable method yet. In this study, we found that homogenizing the green peach aphid, Myzus persicae, in the 96-well microplate resulted in significantly higher P450 activities than those in Eppendorf tube. Homogenizing aphids in Eppendorf tube released uncharacterized compounds that inhibited aphids and pig liver P450 activities, whereas aphids homogenized in the microplate may not be completely ground and thus released fewer such inhibitors. Then, the microplate homogenization method was optimized as follows: one or two aphids were placed in one well of the 96 well-microplate and ground in phosphate buffer using pipette tips for 20 cycles, followed by addition of 7-ethoxycoumarin, and then incubated for 1 h at room temperature, after which glycine buffer-ethanol mixture was added to stop the reaction. This method is also suitable for the pea aphid, Acyrthosiphon pisum, and the bird cherry-oat aphid, Rhopalosiphum padi. These results highlight the importance of considering inhibitory effects of endogenous compounds in insects on their P450 activities and provide one possible method to reduce these inhibitory effects.


Assuntos
Afídeos/metabolismo , Sistema Enzimático do Citocromo P-450/metabolismo , Ensaios Enzimáticos/métodos , Proteínas de Insetos/metabolismo , Animais , Afídeos/efeitos dos fármacos , Inseticidas/toxicidade
17.
PLoS One ; 16(9): e0250311, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34529690

RESUMO

The soybean aphid Aphis glycines Matsumura (Hemiptera: Aphididae) is a primary pest of soybeans and poses a serious threat to soybean production. Our studies were conducted to understand the effects of different concentrations of insecticides (imidacloprid and thiamethoxam) on A. glycines and provided critical information for its effective management. Here, we found that the mean generation time and adult and total pre-nymphiposition periods of the LC50 imidacloprid- and thiamethoxam-treatment groups were significantly longer than those of the control group, although the adult pre-nymphiposition period in LC30 imidacloprid and thiamethoxam treatment groups was significantly shorter than that of the control group. Additionally, the mean fecundity per female adult, net reproductive rate, intrinsic rate of increase, and finite rate of increase of the LC30 imidacloprid-treatment group were significantly lower than those of the control group and higher than those of the LC50 imidacloprid-treatment group (P < 0.05). Moreover, both insecticides exerted stress effects on A. glycines, and specimens treated with the two insecticides at the LC50 showed a significant decrease in their growth rates relative to those treated with the insecticides at LC30. These results provide a reference for exploring the effects of imidacloprid and thiamethoxam on A. glycines population dynamics in the field and offer insight to agricultural producers on the potential of low-lethal concentrations of insecticides to stimulate insect reproduction during insecticide application.


Assuntos
Afídeos/crescimento & desenvolvimento , Glycine max/parasitologia , Inseticidas/efeitos adversos , Neonicotinoides/efeitos adversos , Nitrocompostos/efeitos adversos , Tiametoxam/efeitos adversos , Animais , Afídeos/efeitos dos fármacos , Produtos Agrícolas/efeitos dos fármacos , Produtos Agrícolas/crescimento & desenvolvimento , Feminino , Fertilidade/efeitos dos fármacos , Dose Letal Mediana , Masculino , Dinâmica Populacional
18.
Molecules ; 26(12)2021 Jun 13.
Artigo em Inglês | MEDLINE | ID: mdl-34199264

RESUMO

Rutin and its aglycone quercetin occur in the fruits, leaves, seeds, and grains of many plant species and are involved in plant herbivore interactions. We studied the effect of the exogenous application of rutin and quercetin on the probing behavior (= stylet penetration activities in plant tissues) of Acyrthosiphon pisum on Pisum sativum, Myzus persicae on Brassica rapa ssp. pekinensis, and Rhopalosiphum padi on Avena sativa using the electrical penetration graph technique (EPG = electropenetrography). The reaction of aphids to quercetin and rutin and the potency of the effect depended on aphid species, the flavonol, and flavonol concentration. Quercetin promoted probing activities of A. pisum within non-phloem and phloem tissues, which was demonstrated in the longer duration of probes and a trend toward longer duration of sap ingestion, respectively. M. persicae reached phloem in a shorter time on quercetin-treated B. rapa than on the control. Rutin caused a delay in reaching sieve elements by A. pisum and deterred probing activities of M. persicae within non-phloem tissues. Probing of R. padi was not affected by quercetin or rutin. The potency of behavioral effects increased as the applied concentrations of flavonols increased. The prospects of using quercetin and rutin in plant protection are discussed.


Assuntos
Afídeos/efeitos dos fármacos , Comportamento Alimentar/fisiologia , Floema/fisiologia , Folhas de Planta/metabolismo , Quercetina/farmacologia , Rutina/farmacologia , Animais , Antioxidantes/farmacologia , Afídeos/fisiologia , Herbivoria
19.
Sci Rep ; 11(1): 14484, 2021 07 14.
Artigo em Inglês | MEDLINE | ID: mdl-34262071

RESUMO

The agricultural use of silica (SiO2) nanoparticles (NPs) has the potential to control insect pests while the safety and tritrophic effects on plants and beneficial natural enemies remains unknown. Here, we evaluate the effects of silica NPs on insect pests with different feeding niches, natural enemies, and a plant. Silica NPs were applied at different concentrations (75-425 mg/L) on field-cultivated faba bean and soybean for two growing seasons. The faba bean pests, the cowpea aphid Aphis craccivora and the American serpentine leafminer Liriomyza trifolii, and the soybean pest, the cotton leafworm Spodoptera littoralis, were monitored along with their associated predators. Additional laboratory experiments were performed to test the effects of silica NPs on the growth of faba bean seedlings and to determine whether the rove beetle Paederus fuscipes is attracted to cotton leafworm-infested soybean treated with silica NPs. In the field experiments, silica NPs reduced the populations of all three insect pests and their associated predators, including rove beetles, as the concentration of silica NPs increased. In soybean fields, however, the total number of predators initially increased after applying the lowest concentration. An olfactometer-based choice test found that rove beetles were more likely to move towards an herbivore-infested plant treated with silica NPs than to a water-treated control, suggesting that silica NPs enhance the attraction of natural enemies via herbivore-induced plant volatiles. In the laboratory, while silica NPs inhibited the development of faba bean roots at 400 mg/L, they did not affect germination percentage, germination time, shoot length, or vigor index compared to the control.


Assuntos
Insetos/efeitos dos fármacos , Insetos/fisiologia , Inseticidas/farmacologia , Nanopartículas , Animais , Afídeos/efeitos dos fármacos , Afídeos/fisiologia , Besouros/efeitos dos fármacos , Besouros/fisiologia , Relação Dose-Resposta a Droga , Egito , Germinação/efeitos dos fármacos , Inseticidas/química , Nanopartículas/química , Densidade Demográfica , Comportamento Predatório/efeitos dos fármacos , Dióxido de Silício , Glycine max , Spodoptera/efeitos dos fármacos , Spodoptera/fisiologia , Vicia faba/efeitos dos fármacos , Vicia faba/crescimento & desenvolvimento
20.
ACS Appl Mater Interfaces ; 13(30): 36350-36360, 2021 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-34283576

RESUMO

The application of botanical pesticides is a good choice in organic agriculture. However, most botanical pesticides have limitations of slow action and short persistence for pest and disease management, which constrain their further application. With the objective of exploring a green pesticide for controlling strawberry pests and diseases simultaneously, a star polymer (SPc) with a low production cost was synthesized as a pesticide nanocarrier through simple reactions. The SPc complexed with osthole quickly through electrostatic interaction and hydrophobic association, which decreased the particle size of osthole down to the nanoscale (17.66 nm). With the help of SPc, more nano-sized osthole was delivered into cytoplasm through endocytosis, leading to the enhanced cytotoxicity against insect cells. As a green botanical pesticide, the control efficacy of the osthole/SPc complex was improved against main strawberry pests (green peach aphid and two-spotted spider mite) and disease (powdery mildew), which fulfilled the need of both pest and disease management in sustainable production of strawberry. Meanwhile, the introduction of SPc not only improved plant-uptake but also decreased the residue of osthole due to the higher degradation rate. Furthermore, the application of the osthole/SPc complex exhibited no influence on the strawberry fruit quality and nontarget predators. To our knowledge, it is the first success to control plant pests and diseases simultaneously for sustainable agriculture by only one pesticidal formulation based on nanoparticle-delivered botanical pesticides.


Assuntos
Antifúngicos/toxicidade , Cumarínicos/toxicidade , Dendrímeros/química , Portadores de Fármacos/química , Fragaria/crescimento & desenvolvimento , Inseticidas/toxicidade , Animais , Afídeos/efeitos dos fármacos , Dendrímeros/síntese química , Dendrímeros/toxicidade , Portadores de Fármacos/síntese química , Portadores de Fármacos/toxicidade , Fragaria/efeitos dos fármacos , Células Sf9 , Spodoptera , Tetranychidae/efeitos dos fármacos
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