Background: This study investigated the behavioral responses and toxicity of three basic amines: 1-methylpiperazine, 1-methylpyrrolidine, and triethylamine (TEA), compounds suggested previously to be anosmic in vapor exposures to caged mosquitoes.
Results: These compounds showed repellency of Aedes aegypti mosquitoes, followed by flightlessness, knockdown, and paralysis, all increasing with exposure time and dosage. Electrophysiological experiments showed a blocking effect on nerve discharge of the Drosophila melanogaster larval central nervous system (CNS) with little evidence of hyperexcitation.
The dinoflagellate Karenia brevis is a causative agent of red tides in the Gulf of Mexico and generates a potent family of structurally related brevetoxins that act via the voltage-sensitive Na channel. This project was undertaken to better understand the neurotoxicology and kdr cross-resistance to brevetoxins in house flies by comparing the susceptible aabys strain to ALkdr (kdr) and JPskdr (super-kdr). When injected directly into the hemocoel, larvae exhibited rigid, non-convulsive paralysis consistent with prolongation of sodium channel currents, the known mechanism of action of brevetoxins.
View Article and Find Full Text PDFVolatile pyrethroids are effective in reducing mosquito populations and repelling vectors away from hosts. However, many gaps in knowledge exist for the sublethal impacts of volatile pyrethroids on mosquitoes. To that end, transfluthrin exposures were conducted on a field strain of Aedes albopictus (Skuse) held as a laboratory colony.
View Article and Find Full Text PDFChemical screening efforts recently found that 3-phenoxybenzaldehyde, a breakdown product of alpha-cyano pyrethroids, was a potent spatial repellent against mosquitoes in a glass tube repellency assay. In order to characterize this molecule further and identify structure-activity relationships, a set of 12 benzaldehyde analogues were screened for their repellency and toxicity in vapor phase exposures at 100 μg/cm. Dose-response analyses were performed for the most active compounds in order to better characterize their repellent potency and toxicity compared to those of other commercially available toxicants.
View Article and Find Full Text PDFBecause of the increased interest in plant essential oils (PEO) for both home pest control and personal bite protection, the ability of fir needle (Abies balsamea) oil to synergize the 1-h knockdown and 24-h toxicity of 9 different synthetic insecticides was evaluated. Fir needle oil strongly synergized knockdown of the neonicotinoids, clothianidin, and thiamethoxam (between 16- and 24-fold), as well as natural pyrethrins (12-fold), but had less effect with organophosphates and fipronil. For 24-h mortality, only pirimiphos-methyl was strongly synergized by fir needle oil pretreatment (18-fold).
View Article and Find Full Text PDFThe emergence of pyrethroid-resistant mosquitoes is a worldwide problem that necessitates further research into the development of new repellents and insecticides. This study explored the modification of existing pyrethroid acids to identify structural motifs that might not be affected by active site mutations that elicit pyrethroid resistance. Because synthetic pyrethroids almost always contain activity-dependent chiral centers, we chose to focus our efforts on exploring alkoxy moieties of esters obtained with 1--permethrinic and related acids, which we showed in previous studies to have repellent and/or repellent synergistic properties.
View Article and Find Full Text PDFBackground: An important component of the biological activity of pyrethroids, when used in disease vector control, is excito-repellency. In this study, behavioral differences between insecticide susceptible (Orlando) and pyrethroid resistant (Puerto Rican) strains of Aedes aegypti were explored in a round glass arena using fabrics treated with permethrin, etofenprox, deltamethrin, or DDT. Repellency was evaluated across several variables, including the time to first flight (TFF), number of landings (NOL), total flight time (TFT), and maximum surface contact (MSC), all by video analysis.
View Article and Find Full Text PDFWe explored the potential of two sodium channel activators, veratrine and aconitine, as both insecticides and synergists of natural pyrethrins (NP) on Aedes aegypti adults and larvae. Aconitine was more toxic than veratrine, with an LD of 157 ng/mg compared to 376 ng/mg, on the pyrethroid-susceptible Orlando strain, but only aconitine showed significant resistance in the pyrethroid-resistant Puerto Rico strain (RR = 14.6 in topical application and 8.
View Article and Find Full Text PDFNootkatone, a sesquiterpenoid isolated from Alaskan yellow cedar (Cupressus nootkatensis), is known to possess insect repellent and acaricidal properties and has recently been registered for commercial use by the Environmental Protection Agency. Previous studies failed to elucidate the mechanism of action of nootkatone, but we found a molecular overlay of picrotoxinin and nootkatone indicated a high degree of structural and electrostatic similarity. We therefore tested the hypothesis that nootkatone was a GABA-gated chloride channel antagonist, similar to picrotoxinin.
View Article and Find Full Text PDFCurr Res Parasitol Vector Borne Dis
November 2021
It is important to identify repellents that can provide reliable protection from arthropod biting and prevent arthropod-borne diseases, such as malaria. In the present study, the spatial repellent activity and toxicity of two novel pyridinyl amides ( and ) were evaluated against , , and . In vapor repellency bioassays, compound was generally more effective than DEET and 2-undecanone, while compound was about as active as these standards.
View Article and Find Full Text PDFThe risk of honey bee (Apis mellifera L.) exposure to pesticide residues while foraging for nectar and pollen is commonly explored in the context of agroecosystems. However, pesticides are also used in urban and suburban areas for vegetation management, vector control, and the management of ornamental plants in public and private landscapes.
View Article and Find Full Text PDFTo discover new natural materials for insect management, commercially available stored sheep wool was investigated for attractancy to female adult mosquitoes. The volatiles from sheep wool were collected by various techniques of headspace (HS) extractions and hydrodistillation. These extracts were analyzed using gas chromatography-mass spectrometry (GC-MS) and gas chromatography-flame ionization detector (GC-FID) coupled with GC-MS.
View Article and Find Full Text PDFPrevious studies have shown that insect cell cultures stop dividing, form clumps, and can be induced to grow processes reminiscent of axons, when the culture medium is supplemented with 20-hydroxyecdysone, insulin, or an agent that mimics their action, such as the ecdysone agonist, methoxyfenozide. Those cell growing processes resemble nerve cells, and the present study evaluates the ultrastructure of these cultures by transmission electron microscopy. 21 cells treated with 20-hydroxyecdysone (with or without veratridine amendment) and subjected to ultrastructural analysis had a similar somatic appearance to control cells, with slight changes in organelles and organization, such as a greater number of cytoplasmic vacuoles and mitochondrial granules.
View Article and Find Full Text PDFBackground: The CDC Bottle Bioassay serves as an inexpensive and effective way to screen field-caught mosquitoes against a wide variety of insecticidal active ingredients and commercial formulations, with the goal of detecting resistant individuals. For this study, we assessed how sucrose-water (10% w/v) feeding status impacted the response of Aedes aegypti mosquitoes to select insecticides.
Results: Starvation for 24 or 48 h decreased permethrin and malathion mean survival time by about 40%, with little difference in the two starvation times.
Resistance to currently utilized chemical insecticidal agents represents a significant threat to public health and food security worldwide. Better understanding the neurophysiological effects of available and candidate insecticidal molecules is valuable for characterizing the mechanisms of insecticide resistance, as well as the design and study of novel control chemistries. In this paper, we describe a method of recording nerve firing from the central nervous system of Aedes aegypti fourth instar larvae.
View Article and Find Full Text PDFLiriodenine is a biologically active plant alkaloid with multiple effects on mammals, fungi, and bacteria, but has never been evaluated for insecticidal activity. Accordingly, liriodenine was applied topically in ethanolic solutions to adult female Anopheles gambiae, and found to be mildly toxic. Its lethality was synergized in mixtures with dimethyl sulfoxide and piperonyl butoxide.
View Article and Find Full Text PDFBackground: Varroa destructor is among the greatest threats to honey bee health worldwide. Acaricides used to control Varroa are becoming increasingly ineffective due to resistance issues, prompting the need for new compounds that can be used for control purposes. Ideally, such compounds would exhibit high toxicity to Varroa while maintaining relatively low toxicity to bees and beekeepers.
View Article and Find Full Text PDFPrevious studies have shown that blockers of voltage-gated potassium (Kv) channels, such as 4-aminopyridine (4-AP) and 2-methoxy-N-((1-phenylcyclopentyl)methyl)benzamide (2-MPB) synergized pyrethroid toxicity as well, or better than, piperonyl butoxide. The present study assessed the involvement of different Kv channels as possible pyrethroid synergist targets in Drosophila melanogaster. Three Kv1 mutants (Sh, Sh, and Sh) and one Kv2 mutant (Shab) were tested.
View Article and Find Full Text PDFThe use of N-aryl amide derivatives as spatially acting insecticides remains relatively unexplored. To expand this knowledge, we synthesized eighty-nine N-aryl amide analogues and screened them for mortality against an insecticide-susceptible strain of mosquitoes, Orlando (OR), using a vapor exposure glass tube assay. Of the screened compounds, twenty-two produced >92% mortality at 24 h and warranted further investigation to determine LC values.
View Article and Find Full Text PDFDelivery of compounds to the brain is critical for the development of effective treatment therapies of multiple central nervous system diseases. Recently a novel insect-based brain uptake model was published utilizing a locust brain ex vivo system. The goal of our study was to develop a priori, in silico cheminformatic models to describe brain uptake in this insect model, as well as evaluate the predictive ability.
View Article and Find Full Text PDFWith insecticide-resistant mosquito populations becoming an ever-growing concern, new vector control technologies are needed. With the lack of new chemical classes of insecticides to control mosquito populations, the development of novel synergists may improve the performance of available insecticides. We screened a set of 20 plant essential oils alone and in combination with natural pyrethrins against (Orlando) female adult mosquitoes to assess their ability to synergize this natural insecticide.
View Article and Find Full Text PDFThe productivity and survival of managed honey bee colonies is negatively impacted by a diverse array of interacting factors, including exposure to agrochemicals, such as pesticides. This study investigated the use of volatile heterocyclic amine (HCA) compounds as potential short-term repellents that could be employed as feeding deterrents to reduce the exposure of bees to pesticide-treated plants. Parent and substituted HCAs were screened for efficacy relative to the repellent ,-diethyl-meta-toluamide (DEET) in laboratory and field experiments.
View Article and Find Full Text PDFA total of 115 aryl amides were synthesized and screened for vapor repellency against the Orlando (OR) strain of mosquitoes. Of these compounds, 29 had 1 h repellency EC values comparable to or better than ,-diethyl--toluamide (DEET, 1 h EC value of 35 μg/cm), with 2,2,3,3,3-pentafluoro--(4-fluorophenyl)propenamide () and 2,2,3,3,4,4,4-heptafluoro--(3,4,5-trifluorophenyl)butanamide () exhibiting the most potent EC values of 4.5 and 2.
View Article and Find Full Text PDFThe combined effect of global warming and insecticide exposure on the spread of mosquito-borne diseases is poorly studied. In our opinion, more resources should be diverted to this topic to further research efforts and deal with this increasing threat. It is particularly important to determine how Aedes, Anopheles, and Culex vector species cope with insecticide exposure under warming temperatures, as well as how both stressors may impact the activity of mosquito biocontrol agents.
View Article and Find Full Text PDFBackground: The purpose of this research was to explore the possibility of co-applying pyrethroids (agonists of voltage-sensitive sodium channels) with potassium channel blockers in order to potentiate the neurological effects of pyrethroids on Anopheles gambiae. We hypothesized that the toxicity of pyrethroids caused by persistent sodium currents would be augmented by blockage of outward potassium current flow, which normally repolarizes the membrane potential during a nerve membrane action potential.
Results: Topical treatments with LD s (10% mortality doses) of synergists were given with pyrethroids.