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At least 1,297 records · Page 72Linked to original sources
PubMed2005

Block of two subtypes of sodium channels in cockroach neurons by indoxacarb insecticides.

Indoxacarb, a novel insecticide, and its decarbomethoxyllated metabolite, DCJW, are known to block voltage-gated Na(+) channels in insects and mammals, but the mechanism of block is not yet well understood. The present study was undertaken to characterize the action of indoxacarb and DCJW on cockroach Na(+) channels. Na(+) currents were recorded using the whole-cell patch clamp technique from neurons acutely dissociated from thoracic ganglia of the American cockroach Periplaneta americana L. Two types of tetrodotoxin-sensitive Na(+) currents were observed, with different voltage dependencies of channel inactivation. Type-I Na(+) currents were inactivated at more negative potentials than type-II Na(+) currents. As a result, these two types of Na(+) channels responded to indoxacarb compounds differentially. At a holding potential of -100 mV, type-I Na(+) currents were inhibited reversibly by 1 microM indoxacarb and irreversibly by 1 microM DCJW in a voltage-dependent manner, whereas type-II Na(+) currents were not affected by either of the compound. However, type-II Na(+) currents were inhibited by indoxacarb or DCJW at more depolarizing membrane potentials, ranging from -60 to -40 mV. The slow inactivation curves of type-I and type-II Na(+) channels were significantly shifted in the hyperpolarizing direction by indoxacarb and DCJW, suggesting that these compounds have high affinities for the inactivated state of the Na(+) channels. It was concluded that the differential blocking actions of indoxacarb insecticides on type-I and type-II Na(+) currents resulted from their different voltage dependence of Na(+) channel inactivation. The irreversible nature of DCJW block may be partially responsible for its potent action in insects.

Animals↗
PubMed2005

Molecular basis of differential sensitivity of insect sodium channels to DCJW, a bioactive metabolite of the oxadiazine insecticide indoxacarb.

Indoxacarb (DPX-JW062) was recently developed as a new oxadiazine insecticide with high insecticidal activity and low mammalian toxicity. Previous studies showed that indoxacarb and its bioactive metabolite, N-decarbomethoxyllated JW062 (DCJW), block insect sodium channels in nerve preparations and isolated neurons. However, the molecular mechanism of indoxacarb/DCJW action on insect sodium channels is not well understood. In this study, we identified two cockroach sodium channel variants, BgNa(v)1-1 and BgNa(v)1-4, which differ in voltage dependence of fast and slow inactivation, and channel sensitivity to DCJW. The voltage dependence of fast inactivation and slow inactivation of BgNa(v)1-4 were shifted in the hyperpolarizing direction compared with those of BgNa(v)1-1 channels. At the holding potential of -90 mV, 20 microM of DCJW reduced the peak current of BgNa(v)1-4 by about 40%, but had no effect on BgNa(v)1-1. However, at the holding potential of -60 mV, DCJW also reduced the peak currents of BgNa(v)1-1 by about 50%. Furthermore, DCJW delayed the recovery from slow inactivation of both variants. Substitution of E1689 in segment 4 of domain four (IVS4) of BgNa(v)1-4 with a K, which is present in BgNa(v)1-1, was sufficient to shift the voltage dependence of fast and slow inactivation of BgNa(v)1-4 channels to the more depolarizing membrane potential close to that of BgNa(v)1-1 channels. The E1689K change also eliminated the DCJW inhibition of BgNa(v)1-4 at the hyperpolarizing holding potentials. These results show that the E1689K change is responsible for the difference in channel gating and sensitivity to DCJW between BgNa(v)1-4 and BgNa(v)1-1. Our results support the notion that DCJW preferably acts on the inactivated state of the sodium channel and demonstrate that K1689E is a major molecular determinant of the voltage-dependent inactivation and state-dependent action of DCJW.

Amino Acids↗
PubMed2006

Synergism between insecticides permethrin and propoxur occurs through activation of presynaptic muscarinic negative feedback of acetylcholine release in the insect central nervous system.

Although synergism between pesticides has been widely documented, the physiological mechanisms by which an insecticide synergizes another remains unclear. Toxicological and electrophysiological studies were carried out on two susceptible pest species (the mosquito Culex quinquefasciatus and the cockroach Periplaneta americana) to understand better the physiological process involved in pyrethroid and carbamate interactions. Larval bioassays were conducted with the susceptible reference strain SLAB of C. quinquefasciatus to assess the implication of multi-function oxidases and non-specific esterases in insecticide detoxification and synergism. Results showed that the general theory of synergism (competition between pesticides for a common detoxification enzyme) was unlikely to occur in the SLAB strain since the level of synergy recorded between permethrin and propoxur was unchanged in the presence of piperonyl butoxide and tribufos, two inhibitors of oxidases and esterases, respectively (synergism ratios were similar with and without synergists). We also showed that addition of a sub-lethal concentration of nicotine significantly increased the toxicity of permethrin and propoxur at the lower range of the dose-mortality regression lines, suggesting the manifestation of important physiological disruptions at synaptic level. The effects of both permethrin and propoxur were studied on the cercal-afferent giant-interneuron synapses in the terminal abdominal ganglion of the cockroach P. americana using the single-fibre oil-gap method. We demonstrated that permethrin and propoxur increased drastically the ACh concentration within the synaptic cleft, which thereby stimulated a negative feedback of ACh release. Atropine, a muscarinic receptor antagonist, reversed the effect of permethrin and propoxur mixtures. This demonstrates the implication of the presynaptic muscarinic receptors in the negative feedback regulation process and in synergism. Based on these findings, we propose a cascade of molecular events explaining the occurrence of synergistic effects between pyrethroid and carbamate on many susceptible insects including C. quinquefasciatus, a mosquito of medical importance.

Acetylcholine↗
PubMed2005

Extrapyramidal parkinsonism complicating acute organophosphate insecticide poisoning.

The aim of this study is to report our experience with a child who developed extrapyramidal perturbations complicating acute organophosphate insecticides poisoning and to review the literature reporting on basal ganglia impairment associated with this poisoning. Our patient had developed overt parkinsonism presenting with a resting tremor, expressionless face, and lack of blinking along with marked cogwheel rigidity and a stooped, slow gait. He was alert, coherent, and cooperative, yet agitated. The parkinsonian perturbations developed 5 days after an accidental ingestion of a raw eggplant sprayed with the organophosphate dimethoate (Rogor) when he had already recovered from the acute cholinergic crisis, the first stage of organophosphate poisoning. Such a presentation was initially perceived by his caregivers as severe reactive depression or even psychosis. Once a parkinsonian syndrome was diagnosed, he was begun on amantadine and completely recovered within 1 week with no relapse of symptoms. Basal ganglia impairment should be considered in any patient who develops extrapyramidal symptoms such as marked rigidity and bradykinesia or choreoathetosis while recovering from the acute cholinergic phase of organophosphate insecticide poisoning. Thus, administration of a drug such as amantadine, which probably enhances neurotransmission, may hasten the rate of recovery and prevent long-term neurologic and emotional sequelae.

Acute Disease↗
PubMed2004

Male-specific insecticide resistance and mosquito transgene dispersal.

There is a need to develop methods to spread disease-blocking transgenes through mosquito populations. This article discusses the possibility of linking transgenes to insecticide-resistant alleles engineered to be expressed only in males. The resulting increase in mean longevity of males carrying the construct under insecticide treatment could easily outweigh any fitness costs in females, so that the construct would spread rapidly. It should be possible to produce constructs where any potential risk of loss of male-specific expression would be negligible.

Animals↗
PubMed2004

Interactive toxicity of the organophosphorus insecticides chlorpyrifos and methyl parathion in adult rats.

The acute interactive toxicity following exposure to two common organophosphorus (OP) insecticides, chlorpyrifos (CPF) and methyl parathion (MPS), was investigated in adult male rats. Oral LD1 values were estimated by dose-response studies (CPF = 80 mg/kg; MPS = 4 mg/kg, in peanut oil, 1 ml/kg). Rats were treated with both toxicants (0.5 or 1 x LD1) either concurrently or sequentially, with 4-h intervals between dosing. Functional signs of toxicity (1-96 h) and cumulative lethality (96 h) were recorded. Rats treated with CPF (1 x LD1) did not show any signs of toxicity although MPS (1 x LD1) elicited slight to moderate signs (involuntary movements) within 1-2 h. Concurrent exposure (LD1 dosages of both CPF and MPS) caused slight signs of toxicity only apparent between 24 and 48 h after dosing. When rats were treated sequentially with MPS first followed by CPF 4 h later, slight signs of toxicity were noted between 6 and 24 h, whereas reversing the sequence resulted in 100% lethality within 1 h of the second dosage. Following exposure to lower dosages (0.5 x LD1), the CPF first group showed higher signs of cholinergic toxicity compared with MPS first or concurrent groups. Cholinesterase inhibition in plasma, diaphragm, and frontal cortex was generally higher in rats treated sequentially with CPF first than in those treated initially with MPS from 4 to 24 h after dosing. Plasma and liver carboxylesterase inhibition at 4 h was also significantly higher in the CPF first (62-90%) compared with MPS first (22-43%) group, while at 8 and 24 h, there was no significant difference between any of the treatment groups. ChE inhibition assays to evaluate in vitro hepatic detoxification of oxons indicated that carboxylesterase (CE)- and A-esterase-mediated pathways are markedly less important for methyl paraoxon (MPO) than chlorpyrifos oxon (CPO) detoxification. CPF pretreatment blocked hepatic detoxification of methyl paraoxon while MPS pretreatment had minimal effect on hepatic CPO detoxification ex vivo. These findings suggest that the sequence of exposure to two insecticides that elicit toxicity through a common mechanism can markedly influence the cumulative action at the target site (acetylcholinesterase, AChE) and consequent functional toxicity.

Acetylcholinesterase↗
PubMed2005

Developmental exposure to terbutaline alters cell signaling in mature rat brain regions and augments the effects of subsequent neonatal exposure to the organophosphorus insecticide chlorpyrifos.

Exposure to apparently unrelated neurotoxicants can nevertheless converge on common neurodevelopmental events. We examined the long-term effects of developmental exposure of rats to terbutaline, a beta-adrenoceptor agonist used to arrest preterm labor, and the organophosphorus insecticide chlorpyrifos (CPF) separately and together. Treatments mimicked the appropriate neurodevelopmental stages for human exposures: terbutaline on postnatal days (PN) 2-5 and CPF on PN11-14, with assessments conducted on PN45. Although neither treatment affected growth or viability, each elicited alterations in CNS cell signaling mediated by adenylyl cyclase (AC), a transduction pathway shared by numerous neuronal and hormonal signals. Terbutaline altered signaling in the brainstem and cerebellum, with gender differences particularly notable in the cerebellum (enhanced AC in males, suppressed in females). By itself, CPF exposure elicited deficits in AC signaling in the midbrain, brainstem, and striatum. However, sequential exposure to terbutaline followed by CPF produced larger alterations and involved a wider spectrum of brain regions than were obtained with either agent alone. In the cerebral cortex, adverse effects of the combined treatment intensified between PN45 and PN60, suggesting that exposures alter the long-term program for development of synaptic communication, leading to alterations in AC signaling that emerge even after adolescence. These findings indicate that terbutaline, like CPF, is a developmental neurotoxicant, and reinforce the idea that its use in preterm labor may create a subpopulation that is sensitized to long-term CNS effects of organophosphorus insecticides.

Adenylyl Cyclases↗
PubMed2005

Structure-activity relationships for the action of 11 pyrethroid insecticides on rat Na v 1.8 sodium channels expressed in Xenopus oocytes.

Pyrethroid insecticides bind to voltage-sensitive sodium channels and modify their gating kinetics, thereby disrupting nerve function. This paper describes the action of 11 structurally diverse commercial pyrethroid insecticides on the rat Na v 1.8 sodium channel isoform, the principal carrier of the tetrodotoxin-resistant, pyrethroid-sensitive sodium current of sensory neurons, expressed in Xenopus laevis oocytes. All 11 compounds produced characteristic sodium tail currents following a depolarizing pulse that ranged from rapidly-decaying monoexponential currents (allethrin, cismethrin and permethrin) to persistent biexponential currents (cyfluthrin, cyhalothrin, cypermethrin and deltamethrin). Tail currents for the remaining compounds (bifenthrin, fenpropathrin, fenvalerate and tefluthrin) were monoexponential and decayed with kinetics intermediate between these extremes. Reconstruction of currents carried solely by the pyrethroid-modified subpopulation of channels revealed two types of pyrethroid-modified currents. The first type, found with cismethrin, allethrin, permethrin and tefluthrin, activated relatively rapidly and inactivated partially during a 40-ms depolarization. The second type, found with cypermethrin, cyfluthrin, cyhalothrin, deltamethrin, fenpropathrin and fenvalerate, activated more slowly and did not detectably inactivate during a 40-ms depolarization. Only bifenthrin did not produce modified currents that fit clearly into either of these categories. In all cases, the rate of activation of modified channels was strongly correlated with the rate of tail current decay following repolarization. Modification of Na v 1.8 sodium channels by cyfluthrin, cyhalothrin, cypermethrin and deltamethrin was enhanced 2.3- to 3.4-fold by repetitive stimulation; this effect appeared to result from the accumulation of persistently open channels rather than preferential binding to open channel states. Fenpropathrin was the most effective compound against Na v 1.8 sodium channels from the perspective of either resting or use-dependent modification. When use dependence is taken into account, cypermethrin, deltamethrin and tefluthrin approached the effectiveness of fenpropathrin. The selective expression of Na v 1.8 sodium channels in nociceptive neurons suggests that these channels may be important targets for pyrethroids in the production of paresthesia following dermal exposure.

Animals↗
PubMed2005

Organochlorine insecticides: impacts on human HepG2 cytochrome P4501A, 2B activities and glutathione levels.

This study examined the effects of the organochlorine (OC) insecticides chlordane, o,p'-DDT, dieldrin, endosulfan, kepone, methoxychlor, and toxaphene on human HepG2 cytochrome P450 (1A-EROD and 2B-PROD) activities and glutathione (GSH) levels. Cells were exposed for 24 h at high concentrations (1, 5 or 10 mM) and for 48 h at lower concentrations ranging from 0.01 to 1 mM to evaluate dose responses. Our results show that after 48 h all but dieldrin significantly induced both P4501A and 2B. P4502B responses were greater at all exposure concentrations and times. Mixed responses in GSH levels were observed. All OCs except dieldrin and MXC significantly depleted GSH after 24 h. At 48 h, chlordane, endosulfan and toxaphene significantly increased GSH at low levels and decreased GSH at high levels, while kepone and methoxychlor produced significant declines in GSH at all concentrations. These results support findings of OC insecticides inducing CYP1A, 2B in rats, with CYP2B responses more important. GSH levels declined when P4502B activity was significantly elevated and were significantly increased in the absence of significant P450 activity, suggesting that GSH levels influence the catalytic activity of the cytochrome P450s and the cytochrome P450s influence the cell's ability to regulate GSH.

Cell Line, Tumor↗
PubMed2006

Sea anemone venom as a source of insecticidal peptides acting on voltage-gated Na+ channels.

Sea anemones produce a myriad of toxic peptides and proteins of which a large group acts on voltage-gated Na+ channels. However, in comparison to other organisms, their venoms and toxins are poorly studied. Most of the known voltage-gated Na+ channel toxins isolated from sea anemone venoms act on neurotoxin receptor site 3 and inhibit the inactivation of these channels. Furthermore, it seems that most of these toxins have a distinct preference for crustaceans. Given the close evolutionary relationship between crustaceans and insects, it is not surprising that sea anemone toxins also profoundly affect insect voltage-gated Na+ channels, which constitutes the scope of this review. For this reason, these peptides can be considered as insecticidal lead compounds in the development of insecticides.

Amino Acid Sequence↗
PubMed2004

Future applications of phosphotriesterases in the prophylaxis and treatment of organophosporus insecticide and nerve agent poisonings.

Organophosphorus compounds (OPs) are being used as insecticides and warfare agents. OP insecticides represent an important problem of public health, causing around 200,000 deaths annually. The World Health Organization has pointed to the necessity to introduce new medical practices that improve the results of classical treatments. Many studies have shown that the administration of phosphotriesterases (enzymes that detoxify OPs through hydrolysis) is a promising treatment of persons poisoned with OPs. Such an enzyme-based treatment might introduce important improvements in the treatment of patients having ingested large amounts of OPs. Phosphotriesterases might also be suitable for prophylactic treatment of persons at risk to be severely exposed. The new experimental treatments do not exhibit the intrinsic neurotoxicity of the classical prophylaxis based on carbamates and antimuscarinic drugs. Experimental data suggest that might be time to initiate clinical trials in order to study the efficacy of phosphotriesterases in the therapy and prophylaxis of OP intoxication.

Animals↗
PubMed2006

Insecticide-treated bednets to prevent anthroponotic cutaneous leishmaniasis in Aleppo Governorate, Syria: results from two trials.

The increasing incidence of anthroponotic cutaneous leishmaniasis (ACL) in Syria, coupled with the inefficacy of residual insecticide spraying to control the disease, have led to the further evaluation of the preventive efficacy of insecticide-treated bednets (ITNs) through large-scale field studies. Two trials were performed in the historical ACL-endemic areas of the Aleppo Governorate. In 1997-1999, a matched-cluster randomized trial was conducted in five intervention (ITNs) and five control (untreated bednets) villages, which involved a population of 10354 in 1321 households. In 2001-2003, a second study was performed in four villages (a population of 9325 in 858 households), which allowed the evaluation of the impact of the interruption of ITN intervention on ACL incidence rates. Both studies not only confirmed the high efficacy of ITNs in preventing ACL during 1 year post-intervention [about 85% (95% CL 76-98%) in the 1997-1999 trial], but also suggested that the interruption of this control measure might restore the pre-intervention disease incidence within 1-2 years. These findings underline the need for a sustainable and durable implementation of ITN-based control of the disease.

Animals↗
PubMed2004

[Systemic insecticides: new risk for pollinator insects].

Imidacloprid, a new systemic insecticide used as seed-dressing, has been widely used in France since 1994. Its application mode and its efficiency allow a significant reduction in comparison with the usual quantity of chemicals used during pulverising treatment. But the insecticide imidacloprid is suspected to have harmful effects on the pollinators as many bees have died since its introduction. Recent studies have shown that imidacloprid has chronic and sub-lethal toxicities at levels of micro g/kg or less. It was therefore necessary to detect imidacloprid at these levels in soils, plants, flowers, and pollens. With this aim, we characterised the bio-availability of imidacloprid in the environment using a new quantitative analytical method, as a basis for the evaluation of the risk for bees.

Animals↗
PubMed2000

Stability of organophosphorus insecticides on graphitized carbon black extraction cartridges used for large volumes of surface water.

The stability of nine organophosphorus insecticides (azinphos-ethyl, azinphos-methyl, diazinon, EPN, ethion, fonofos, malathion, phosmet and parathion-methyl) was evaluated under a variety of storage conditions. Large volumes of surface water (4 l) were extracted using large-particle-size graphitized carbon black cartridges (Carbopack B 60-80 mesh). The effects of temperature, matrix type and drying of cartridges on the recovery of these contaminants, after different storage periods, were studied and compared to the conservation of surface water in bottles. After a 2-month period, all the chemicals stored on cartridges and kept at -20 degrees C remained stable, with recoveries ranging from 70 to 134%. By contrast, phosmet and EPN could no longer be recovered from the bottled surface water. Cartridges kept at -20 degrees C fared better than did those stored at 4 degrees C and 20 degrees C. The type of matrix water selected appears to have kept the target pesticides stored on cartridges from degrading, compared to the Milli-Q water, in which malathion and phosmet were unstable. The effect of the cartridges being either wet or dry made no difference in terms of improving the recovery of chemicals. After immediate surface water extraction, the most practical storage condition for the target insecticides was found to be storage on cartridges in the dark at -20 degrees C, with no drying or solvent washing of the Carbopack B material.

Carbon↗
PubMed2001

Separation of the insecticidal pyrethrin esters by capillary electrochromatography.

A simple, rapid technique for the direct separation and quantification of the six insecticidally active pyrethrin esters in typical extracts and commercial formulations by capillary electrochromatography (CEC) has been described. The separation of the pyrethrin esters was achieved by optimizing several parameters including the length of stationary phase, the mobile phase composition and column temperature. The mobile phase composition had the most pronounced effect toward resolving these structurally similar compounds. A ternary mobile phase composed of acetonitrile-aqueous buffer-tetrahydrofuran (55:35:10) provided the elutropic solvent strength needed to resolve the six esters from an extract mixture in under 16 min. A 25 cm packed bed of Hypersil 3 microm C18 stationary phase was used with the ternary mobile phase at 25 degrees C and 30 kV voltage. These conditions also yielded excellent separation of the pyrethrin esters in two different commercially available insecticidal formulations. In addition, the developed CEC method was shown to be a fast and easy way of quantifying the amount of these esters in typical pyrethrin formulations.

Chromatography, Micellar Electrokinetic Capillary↗
PubMed1976

Gas chromatographic analysis of heptafluorobutyryl derivatives of some carbamate insecticides.

The gas chromatography (GC) of a number of carbamate insecticides as their heptafluorobutyryl derivatives has been studied. The reaction makes use of heptafluorobutyric anhydride with trimethylamine in benzene as a catalyst. Conversion of the insecticides to their products is complete in 15-20 min at room temperature. The same reaction proved satisfactory for trifluoroacetylation. The excess reagent and trimethylamine are removed by partitioning with water in the reaction test tube. An aliquot of the organic phase is used for analysis. The heptafluorobutyryl derivatives are stable for several days on the lab bench without removal of the aqueous phase from the test tube. GC detection was carried out with a Coulson conductivity detector in the halogen (reductive) mode. About 1.0 ng produced a 50% full-scale response for most of the carbamates (3 min retention time) on 3% OV-1. This method was applied to the analysis of several carbamates spiked in corn, mustard greens, turnip greens, lettuce and cabbage.

Butyrates↗
PubMed2001

Optimization of headspace solid-phase microextraction conditions for the determination of organophosphorus insecticides in natural waters.

Headspace solid-phase microextraction (HS-SPME) has been developed for the analysis of seven organophosphorus insecticides, i.e. diazinon, fenitrothion, fenthion, ethyl parathion, methyl bromophos, ethyl bromophos and ethion in natural waters. Their determination was carried out using gas chromatography with flame thermionic and mass spectrometric detection. To perform the HS-SPME, two types of fibre have been assayed and compared: polyacrylate (PA 85 microm), and polydimethylsiloxane (PDMS 100 microm). The main parameters affecting the HS-SPME process such as temperature, salt additives, memory effect, stirring rate and adsorption-time profile were studied. The method was developed using spiked natural waters such as ground, sea, river and lake water in a concentration range of 0.05-1 microg/l. The HS-SPME conditions were optimized in order to obtain the maximum sensitivity. Detection limits varied from 0.01 to 0.04 microg/l and relative standard deviations (RSD <17%) were obtained showing that the precision of the method is reliable. The method showed also good linearity for the tested concentration range with regression coefficients ranging between 0.985 and 0.999. Recoveries were in relatively high levels for all the analytes and ranged from 80 to 120%. Water samples collected from different stations along the flow of Kalamas river (NW Greece) were analyzed using the optimized conditions in order to evaluate the potential of the proposed method to the trace-level screening determination of organophosphorus insecticides. The analysis with HS-SPME has less background interference and the advantage of its non-destructive nature reveal the possibility of the repetitive use of the SPME fibre.

Gas Chromatography-Mass Spectrometry↗