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PubMed1998

Susceptibility status of malaria vectors to insecticides in India.

The use of chemical insecticides for control of malaria vector populations continues to be the mainstay of malaria control strategy in India. Monitoring vector susceptibility to chemical insecticides is an important activity under the National Malaria Eradication Programme to ensure judicious and effective use of chemical Insecticides. 72 entomological zones were established under NMEP in 1977 for undertaking entomological studies in the malaria problematic areas. These zones have been generating insecticide susceptibility data in respect of the various malaria vectors. In this paper the insecticide susceptibility data, in respect of major vectors of malaria as on 1997, is presented.

Animals↗

PubMed1994

What role for insecticides in vector control programs?

Vector-borne diseases including dengue, yellow fever, Japanese encephalitis, malaria, leishmaniasis, and filariasis remain severe public health problems in most of the countries in which they are endemic. In some cases, their incidence is increasing and they are spreading to new geographic areas. For a number of the infections, the most effective manner of controlling their transmission is through control of their vectors. However, in some instances, such as dengue and Chagas' disease, there is no alternative. Most countries that are endemic for vector-borne diseases maintain vector control services, and most large tropical and semitropical cities also have pest control programs, mainly against pest mosquitoes. Virtually all of the vector and pest control programs depend on the use of insecticides formulated as larvicides, adulticides, baits, or insecticide impregnated bed nets. For many years, the development of new insecticides for use in public health programs was encouraged and supported by multilateral and bilateral health agencies, including the implementation of field trials in endemic areas. Due to the development of insecticide resistance, toxicologic and environmental considerations, and the cost of development and of registration, the number of compounds available for use has declined while the number of new insecticides submitted for laboratory and field trials to the World Health Organization has dwindled even more. The recrudescence of vector-borne diseases, the rapid pace of urbanization, lagging development of environmental services in many tropical cities, and difficulties encountered in ensuring the community's cooperation in its own protection through environmental measures make imperative the continued availability of pesticides for public health use. Since only the pesticide manufacturing industry has the combination of technical and financial resources to promulgate the research and development of new pesticides and pesticide groups, it is suggested that governments, bilateral, and multilateral organizations explore the manner in which they can assist industry in the development of new compounds and guarantee the continued availability of effective and safe pesticides for vector-control programs.

Animals↗

PubMed2001

Multi-residue determination of 41 insecticides in garlic by gas chromatography and ion trap mass spectrometry using the selective ion storage technique.

A method is described for determining 41 insecticide residues in garlic (Allium sativum L.), including organophosphorus, organochlorine, carbamate, and synthetic pyrethroid insecticides. These insecticides were extracted from samples with acetone and dichloromethane, and co-extractives removed using a charcoal/Celite/alumina column. Analysis was performed by gas chromatography with ion trap mass spectrometry in selective ion storage (SIS) mode. Retention times and specific ions (m/z values) were used to confirm insecticides. Recoveries for most insecticides (blank samples spiked at 0.05, 0.2 and 1 microg mL(-1) levels) ranged from 70% to 110%, the coefficient of variation (CV) of the method was <20% for every case, and the limit of detection (LOD), defined in terms of 3 times baseline noise, varied between 0.01 and 0.16 mg kg(-1), depending on the compound.

Food Contamination↗

PubMed1993

Insecticide action at the GABA-gated chloride channel: recognition, progress, and prospects.

Three billion (3 x 10(9)) pounds of hexachlorocyclohexanes, polychlorobornanes, and chlorinated cyclodienes (such as lindane, toxaphene, and endosulfan, respectively) were used to control pest insects before their mode of action was established as blocking the GABA-gated chloride channel. With the restricted use or demise of these polychlorocycloalkanes (each approximately 50 to approximately 75% by weight of chlorine), the GABAergic system is for now an underutilized target of insecticide action. Newer compounds with outstanding potency at this receptor and as toxicants to houseflies are suitably-substituted 2,6,7-trioxabicyclo[2.2.2]-octanes, particularly the bicycloorthobenzoates, and 1,3-dithianes, including those with no halogenated substituents. Picrotoxinin analogs and alkynylphenyl-silatranes also act at this target but are of lower insecticidal activity. [3H]n-Propyl-ethynylbicycloorthobenzoate ([3H]EBOB) is for now the best radioligand for this insecticidally-relevant binding site in insects. Macrocyclic lactones such as the avermectins and moxidectin act at a different binding site to disrupt chloride flux and they have a different spectrum of insecticidal activity and no cross resistance with cyclodienes in houseflies. The search for new insecticides has provided the incentive and probes for a better understanding of the insect GABAergic system.

Animals↗

PubMed2001

Effects of organosilicon pyrethroid-like insecticides on nerve preparations of American cockroaches and crayfish.

Quaternary organosilicon pyrethroid-like ethers (five compounds) and alkanes (three compounds) were used for neurophysiological tests. Their activities in inducing repetitive firing in the central nervous cord of the American cockroach (Periplaneta americana) were evaluated by an extracellular recording method. The ethers were more active than the corresponding alkanes. The ability of the compounds to cause conduction blockage was also measured using the same nerve preparations, but the effects were too weak to allow definitive activity values to be determined. The compounds prolonged the sodium tail-current in the crayfish giant axon under voltage clamp conditions. The rate of decay of the tail-current changed in parallel with the reported insecticidal activity against P americana. These findings indicated that tail-current activity was the most useful nerve parameter in predicting insecticidal activity. Regression analysis of the numerical data together with those reported for other alkanes revealed that the higher the tail-current activity, the higher the insecticidal activity when a structural feature and the hydrophobicity were considered separately. The insecticidal activity of the ethers was about seven-fold higher than that of the alkanes with equivalent tail-current activity and hydrophobicity. Variations in insecticidal activity were parabolically correlated with the hydrophobicity [(log P)opt = 9.1] when other factors were similar.

Action Potentials↗

PubMed2001

Insecticidal and binding activities of N3-substituted imidacloprid derivatives against the housefly Musca domestica and the alpha-bungarotoxin binding sites of nicotinic acetylcholine receptors.

N3-substituted imidacloprid congeners containing C1-C6 alkyl groups or various analogous groups, and their corresponding nitromethylene analogues, were used in this study. Their insecticidal activity against the housefly, Musca domestica, and their binding activity toward the nicotinic acetylcholine receptor were determined. The insecticidal test was conducted using the synergists piperonyl butoxide and propargyl propyl phenylphosphonate. The binding assay was performed with housefly head membrane preparations using radio-labelled alpha-bungarotoxin. Both insecticidal and binding activities were drastically lowered by the introduction of alkyl/allyl groups at the imidazolidine NH sites of both nitroimino and nitromethylene compounds. The binding activity of N3-substituted nitromethylene analogues was much higher than that of the corresponding nitroimino analogues. However, the insecticidal activity of both series of compounds with a given substituent was nearly identical. The insecticidal activity correlated positively with the binding activity after taking into account the structural difference of the nitroimino and nitromethylene moieties and a structural feature of the N3-substituents.

Animals↗

PubMed1995

Relationship of aquatic natural organic material characteristics to the toxicity of selected insecticides.

Toxicities of the commercial insecticide formulations of azinphos methyl, chlorpyrifos, fenvalerate, and methyl parathion were evaluated in streamwater samples containing natural organic material (NOM) using a modification of a bacterial bioluminescence assay. Toxicity reduction of azinphos methyl was significantly (P < 0.05) correlated with water sample nonvolatile total solids (NVTS) concentration. Toxicity reductions of fenvalerate and of methyl parathion were significantly correlated to E4/E6 absorbance ratio of NOM, and to the proportion of NOM having molecular weight greater than 3700 Da. Toxicity reductions of fenvalerate and methyl parathion had significant correlations to the concentration of NVTS in water samples. Linear regressions of insecticide EC50 values to these NOM characteristics were used to mathematically model the effect of NOM on insecticide toxicity. Insecticide logKOW values were significantly correlated to the slopes of the EC50-total organic carbon (TOC) concentration regression lines. This confirms that the level of association of some nonionic organic contaminants with NOM is a function of the contaminant's water solubility. No single NOM characteristic was the best predictor of toxicity for all insecticides examined. However, these findings suggest that the influence of NOM on toxicity results primarily from differences in TOC content and abundance of larger molecular size NOM.

Animals↗

PubMed2001

Acute toxicity of locust insecticides to two indigenous invertebrates from Sahelian temporary ponds.

During desert locust plagues large amounts of insecticides are used for control operations. Drift from these treatments and accidental overspraying may contaminate small surface waters such as temporary ponds. The present study describes methods for static acute toxicity tests with two abundant organisms that occur in temporary ponds in the African Sahel region: the fairy shrimp Streptocephalus sudanicus Daday (Branchiopoda, Anostraca, Streptocephalidae) and the backswimmer Anisops sardeus Herrich-Schåffer (Hemiptera, Notonectidae). The organisms were captured in the field and 48-h static toxicity tests were conducted in the laboratory. The assays were used to screen the toxicity of 11 formulated synthetic insecticides used in desert locust control and of spores of the mycopesticide Metarhizium anisopliae var. acridum. Most of the synthetic insecticides tested were highly toxic to both organisms (LC50 or EC50<1 mg/L). Exceptions were the toxicity of diflubenzuron to A. sardeus (moderately toxic: 1<LC50<10 mg/L), and that of fenitrothion (moderately toxic) and malathion (slightly toxic: 10<EC50<100 mg/L) to S. sudanicus. M. anisopliae var. acridum was moderately toxic to S. sudanicus and only slightly toxic to A. sardeus. EC50 values of the insecticides for S. sudanicus were not significantly correlated with L(E)C50 values for Daphnia magna collected from the literature. For A. sardeus a significant correlation with D. magna was found, but even in this data set the two species had widely differing sensitivities to some insecticides.

Animals↗

PubMed2001

Role of human GABA(A) receptor beta3 subunit in insecticide toxicity.

The gamma-aminobutyric acid type A (GABA(A)) receptor is the target for the major insecticides alpha-endosulfan, lindane, and fipronil and for many analogs. Their action as chloride channel blockers is directly measured by binding studies with [(3)H]ethynylbicycloorthobenzoate ([(3)H]EBOB). This study tests the hypothesis that GABA(A) receptor subunit composition determines the sensitivity and selectivity of insecticide toxicity. Human receptor subtypes were expressed individually (alpha1, alpha6, beta1, beta3, and gamma2) and in combination in insect Sf9 cells. Binding parameters were similar for [(3)H]EBOB in the beta3 homooligomer, alpha1beta3gamma2 heterooligomer, and native brain membranes, but toxicological profiles were very different. Surprisingly, alpha-endosulfan, lindane, and fipronil were all remarkably potent on the recombinant beta3 homooligomeric receptor (IC50 values of 0.5-2.4 nM), whereas they were similar in potency on the alpha1beta3gamma2 subtype (IC50 values of 16-33 nM) and highly selective on the native receptor (IC50 values of 7.3, 306, and 2470 nM, respectively). The selectivity order for 29 insecticides and convulsants as IC50 ratios for native/beta3 or alpha1beta3gamma2/beta3 was as follows: fipronil > lindane > 19 other insecticides including alpha-endosulfan and picrotoxinin > 4 trioxabicyclooctanes and dithianes (almost nonselective) > tetramethylenedisulfotetramine, 4-chlorophenylsilatrane, or alpha-thujone. Specificity between mammals and insects at the target site (fipronil > lindane > alpha-endosulfan) paralleled that for toxicity. Potency at the native receptor is more predictive for inhibition of GABA-stimulated chloride uptake than that at the beta3 or alpha1beta3gamma2 receptors. Therefore, the beta3 subunit contains the insecticide target and other subunits differentially modulate the binding to confer compound-dependent specificity and selective toxicity.

Binding Sites↗

PubMed1975

[Residues of organochlorine insecticides in sediments of a high estuary of Fleuve St-Laurent].

In order to determine the distribution and levels of organochlorine insecticide residues in sediments of the upper estuary of the St. Lawrence River, we have carried out the first analyses in Quebec of these compounds in samples from different parts of this region. The recovery of these residues was conducted by continuous Soxhlet extraction of the samples with 100 ml of a mixture of acetone and n-hexane (50:50). The insecticide-containing extract was cleaned up by column chromatography on activated florisil. Elution with 100 ml of n-hexane and then 150 ml of a mixture of n-hexane and ether (85:15) gave two fractions. The analyses were performed by gas liquid chromatography using an electron-capture detector with a radioactive 63Ni source. In the two series of samplings (June and July 1973), DDT and its metabolites were detected in appreciable amounts at nearly all sampling sites while the other insecticides: alpha-BHC, gamma-BHC, heptachlor and dieldrin, were found only in a few and at very low concentrations: beta-BHC, aldrin and heptachlor epoxide were absent at all sites. In general, the insecticide levels at the various sites show a slight variation in time. However, in some, the concentration of organochlorine insecticides is much lower than in others; in these cases it is presumed that this is due to a greater rate of sedimentation in the absence of current and also to local agriculture and sediment texture.

Canada↗

PubMed1996

Heterogeneity of the glutathione transferase genes encoding enzymes responsible for insecticide degradation in the housefly.

One of the four glutathione-S-transferases (GST) that is overproduced in the insecticide-resistant Cornell-R strain of the housefly (Musca domestica) produces an activity that degrades the insecticide dimethyl parathion and conjugates glutathione to lindane. In earlier work, it was shown that the resistant Cornell-R carries an amplification, probably a duplication, of one or more of its GST loci and that this amplification is directly related to resistance. Using polymerase chain reaction (PCR) amplification with genomic DNA, multiple copies of the gene encoding the parathion-degrading activity (called MdGst-3) were subcloned from both the ancestral, insecticide-susceptible strain BPM and from the insecticide-resistant Cornell-R. In BPM, three different MdGst-3 genes were identified while in Cornell-R, 12 different MdGst-3 sequences were found that, though closely related to ancestral genes, had diverged by a few nucleotides. This diversity in MdGst-3 genomic sequences in Cornell-R is reflected in the expressed sequences, as sampled through a cDNA bank. Population heterozygosity cannot account for these multiple GST genes. We suggest that selection for resistance to insecticides has resulted in not only amplification of the MdGst-3 genes but also in the divergence of sequence between the amplified copies.

Animals↗

PubMed1999

Multiple origins of cyclodiene insecticide resistance in Tribolium castaneum (Coleoptera: Tenebrionidae).

The number of origins of pesticide resistance-associated mutations is important not only to our understanding of the evolution of resistance but also in modeling its spread. Previous studies of amplified esterase genes in a highly dispersive Culex mosquito have suggested that insecticide resistance-associated mutations (specifically a single-gene duplication event) can occur a single time and then spread throughout global populations. In order to provide data for resistance-associated point mutations, which are more typical of pesticide mechanisms as a whole, we studied the number of independent origins of cyclodiene insecticide resistance in the red flour beetle Tribolium castaneum. Target-site insensitivity to cyclodienes is conferred by single point mutations in the gene Resistance to dieldrin (Rdl), which codes for a subunit of a gamma-aminobutyric acid (GABA) receptor. These point mutations are associated with replacements of alanine 302 which render the receptor insensitive to block by the insecticide. We collected 141 strains of Tribolium worldwide and screened them for resistance. Twenty-four strains contained resistant individuals. After homozygosing 23 of these resistance alleles we derived a nucleotide sequence phylogeny of the resistant strains from a 694-bp section of Rdl, encompassing exon 7 (which contains the resistance-associated mutation) and part of a flanking intron. The phylogeny also included six susceptible alleles chosen at random from a range of geographical locations. Resistance alleles fell into six clades and three clades contained both resistant and susceptible alleles. Although statistical analysis provided support at only the 5-6% level, the pattern of variation in resistance alleles is more readily explained by multiple independent origins of resistance than by spread of a single resistance-associated mutation. For example, two resistance alleles differed from two susceptible alleles only by the resistance-associated mutation itself, suggesting that they form the susceptible ancestors and that resistance arose independently in several susceptible backgrounds. This suggests that in Tribolium Rdl, de novo mutations for resistance have arisen independently in several populations. Identical alleles were found in geographically distant regions as well, also implying that some Rdl alleles have been exported in stored grain. These differences from the Culex study may stem both from differences in the population genetics of Tribolium versus that of mosquitoes and differences in mutation rates associated with point mutations versus gene duplication events. The Tribolium data therefore suggest that multiple origins of insecticide resistance (associated with specific point mutations) may be more common than the spread of single events. These findings have implications for the way in which we model the evolution and spread of insecticide resistance genes and also suggest that parallel adaptive substitutions may not be uncommon in phyletic evolution.

Animals↗

PubMed2001

Modification, by the insecticide chlorpyrifos, of the behavioral response to kairomones of a parasitoid wasp, Leptopilina boulardi.

Parasitoids are key species involved in the regulation of natural populations. Host parasitization is realized via some important steps in which kairomone perception is essential. Due to the wide use of insecticides and their contribution to environmental pollution, the determination of their sublethal effects on behaviors involved in the reproduction of parasitoids becomes a necessity. In this work, we analyzed the effects of a lethal dose 20% of chlorpyrifos, an organophosphorus insecticide, on the behavior of L. boulardi toward the kairomone of its host. The insecticide significantly modified the kinetics of the residence time of parasitoids on a patch marked by kairomones. Females exposed to the insecticide were less efficient in finding the kairomone patch than control females, and they tended to stay on that patch, whereas control females rapidly left it. These effects are discussed considering the mode of action of the insecticide. Because search time allocation of host is an important component for parasitism efficiency, this modification of behavior could interfere with the reproduction capacity of parasitoids. Therefore, in a context of environmental pollution, the repercussions of such sublethal effects on the population biology of insects need to be considered.

Animals↗

PubMed1982

Interactions of chlorinated hydrocarbon insecticides with membranes.

Chlorinated hydrocarbon insecticides quench the fluorescence of N-alkyl derivatives of carbazole. We used phospholipids with covalently attached carbazole as probes for the interactions of chlorinated hydrocarbon insecticides with lipid bilayers, the object being to understand better the toxicities of chlorinated hydro-carbons. Fluorescence quenching measurements revealed the lipid-water partition coefficients of the chlorinated hydrocarbons, their diffusion coefficients in the membranes, and the binding capacities of the membranes for the chlorinated hydrocarbons. Active insecticides were compared with inactive analogues to test whether activities correlated with chlorinated hydrocarbon-membrane interactions. Thus DDT and methoxychlor were compared with inactive DDE, and insecticidal gamma-lindane was compared with three less active stereoisomers. The partition coefficients, diffusion coefficients and membrane saturation capacities did not correlate with insecticidal potency. The partition coefficients of these chlorinated hydrocarbons were larger in bilayers containing unsaturated fatty acyl chains as compared to bilayers containing saturated fatty acyl chains. Interestingly, neural membranes are known to contain a large percentage of unsaturated lipids. Our results indicate that the activities of chlorinated hydrocarbons are not a result of specific interactions of these compounds with the lipids of membranes. However, the neurotoxicity of chlorinated hydrocarbons may be amplified by selective partitioning in the unsaturated neural membranes.

Diffusion↗

PubMed1984

Interference by DDT and cyclodiene types of insecticides with chloroplast-associated reactions.

The effects of DDT, some of its analogs, and selected cyclodiene insecticides on isolated spinach (Spinacea oleracea L.) thylakoids were identified, characterized, and compared to responses induced by selected herbicides. Except for endrin, the insecticides inhibited light-induced electron transport, altered chlorophyll fluorescence transients, and competitively displaced [14C]atrazine [2-chloro-4-(ethylamino)-6-(isopropylamino)-s-triazine], a known photosystem II inhibitor, from the membranes. The insecticides appeared to act at, or near B, the secondary electron acceptor of photo-system II. Binding of DDT and dieldrin was estimated at 900 and 2200 molecules, respectively, per photosynthetic unit (490 chlorophyll molecules). The insecticides also inhibited valinomycin-induced swelling of the thylakoid membrane. Whereas inhibition of electron transport can be attributed to interaction by the insecticides with a proteinaceous component of the thylakoid membrane, interference with the action of valinomycin may involve interaction with lipoidal constituents of the membrane.

Binding, Competitive↗

PubMed1983

Influence of pretreatment with various insecticides on the N-demethylation of dimethylnitrosamine.

The effects of various classes of insecticides were studied on the N-demethylation of dimethylnitrosamine (DMN) by mouse liver enzymes. Organochlorine insecticides, represented by lindane, DDT, and endrin, increased the activities of DMN demethylase I and II. The latter enzyme was more susceptible to the inducive action of the tested chlorinated insecticides. On the other hand, the synthetic pyrethroids, fenvalerate and flucythrinate, did not alter the activity of either enzyme. While pretreatment with carbaryl, a carbamate derivative, was without effect, moderate elevation in the activity of both demethylases was observed following administration of carbofuran. Dimethoate, representing organophosphorus compounds, was the only insecticide tested to inhibit the N-demethylation of DMN, with more pronounced effect on DMN demethylase I. Since DMN requires metabolic activation for its hepatotoxic and carcinogenic actions, alterations in the activities of its metabolizing enzymes as a sequela of exposure to certain insecticides may change susceptibility to its toxicity and/or carcinogenicity.

Animals↗

PubMed1977

Mutagenicity screening of five methyl carbamate insecticides and their nitroso derivatives using mutants of Salmonella typhimurium LT2.

The mutagenic activity of five methyl carbamate insecticides-carbaryl, baygon, BUX-Ten, landrin and methomyl-and their nitroso derivatives were investigated using histidine auxotrophs-his TA98, his TA100, his TA1535, his TA1537 and his TA1538--of Salmonella typhimurium LT2 derived by Ames. The methyl carbamate insecticides did not cause a signficant increase in the number of revertant colonies in any of the strains used. In contrast, the nitroso derivatives of the carbamate insecticides greatly increased the number of colonies on plates inoculated with strains his TA100 and his TA1535. We conclude that the nitroso derivatives of the tested methyl carbamate insecticides are potent mutagens; whereas, the parent insecticides are non-mutagenic.

Carbamates↗

PubMed1993

Evaluation of knit glove fabrics as barriers to dermal absorption of organophosphorus insecticides using an in vitro test system.

Cotton and synthetic knit glove fabrics in combination with an in vitro skin model were used to examine the capability of fabric to decrease the dermal absorption of the organophosphorus insecticides azinphos-methyl, paraoxon, and malathion. Capability for inhibition of acetylcholinesterase was determined in samples of media taken from under the skin barrier after the skin model, with or without fabric protection, had been exposed to the test compounds for 4 h. Acetylcholinesterase inhibitions caused by the direct addition of organophosphorus insecticide to the media were also included in the comparison. Results indicated that the skin model system alone had some capability to serve as a barrier to the transfer of organophosphates. Fabric covering used on the test model increased the barrier between insecticide application and resultant acetylcholinesterase inhibition. The all-cotton, 7-cut knit was especially effective in preventing the absorption of azinphos-methyl, as this organophosphorus insecticide had no capability to cause acetylcholinesterase inhibition when this fabric was used to protect the skin model. Knit glove materials of 100% cotton were demonstrated to be effective in preventing the absorption of paraoxon and malathion. These studies indicate that an in vitro model system can be used in combination with fabrics to study the relationship between clothing and skin as barriers to the absorption of organophosphorus insecticides.

Gloves, Protective↗